{"id":40356,"date":"2021-10-14T08:00:08","date_gmt":"2021-10-14T00:00:08","guid":{"rendered":"\/\/www.gsbet888.com\/?p=40356"},"modified":"2021-10-12T21:06:48","modified_gmt":"2021-10-12T13:06:48","slug":"jacs%ef%bc%9alewis%e7%a2%b1%e6%80%a7%e7%9b%90%e8%af%95%e5%89%82%e4%bf%83%e8%bf%9b%e7%9a%84%e6%9c%89%e6%9c%ba%e7%a1%85%e7%83%b7%e4%b8%8e%e8%8a%b3%e9%a6%99%e4%ba%b2%e7%94%b5%e5%ba%95%e7%89%a9%e4%b9%8b","status":"publish","type":"post","link":"\/\/www.gsbet888.com\/%e5%8c%96%e5%ad%a6%e6%9d%82%e8%ae%b0\/recentpaper\/2021\/10\/jacs%ef%bc%9alewis%e7%a2%b1%e6%80%a7%e7%9b%90%e8%af%95%e5%89%82%e4%bf%83%e8%bf%9b%e7%9a%84%e6%9c%89%e6%9c%ba%e7%a1%85%e7%83%b7%e4%b8%8e%e8%8a%b3%e9%a6%99%e4%ba%b2%e7%94%b5%e5%ba%95%e7%89%a9%e4%b9%8b.html","title":{"rendered":"JACS\uff1aLewis\u78b1\u6027\u76d0\u8bd5\u5242\u4fc3\u8fdb\u7684\u6709\u673a\u7845\u70f7\u4e0e\u82b3\u9999\u4eb2\u7535\u5e95\u7269\u4e4b\u95f4\u7684\u5076\u8054\u53cd\u5e94"},"content":{"rendered":"<p><strong>\u672c\u6587\u4f5c\u8005\uff1a\u6749\u6749<\/strong><\/p>\n<h4>\u5bfc\u8bfb<\/h4>\n<p>\u8fd1\u65e5\uff0c\u7f8e\u56fdColorado\u5dde\u7acb\u5927\u5b66 (Colorado State\u00a0University)\u7684J.\u00a0S. Bandar\u8bfe\u9898\u7ec4\u62a5\u9053\u4e00\u79cd\u901a\u8fc7Lewis\u78b1\u6027\u76d0\u8bd5\u5242\u4fc3\u8fdb\u7684\u82c4\u57fa\u4e09\u7532\u57fa\u7845\u70f7\u4e0e(\u6742)\u82b3\u57fa\u8148\u3001\u781c\u4ee5\u53ca\u6c2f\u4ee3\u4e4b\u95f4\u7684\u4ea4\u53c9\u5076\u8054\u53cd\u5e94\u65b9\u6cd5\u5b66\uff0c\u8fdb\u800c\u83b7\u5f97\u4e00\u7cfb\u52171,1-\u4e8c\u82b3\u57fa\u70f7\u70c3\u884d\u751f\u7269\u3002\u503c\u5f97\u6ce8\u610f\u7684\u662f\uff0c\u8fd9\u4e00\u5168\u65b0\u7684\u5076\u8054\u7b56\u7565\u4e2d\uff0c\u9009\u62e9\u7a33\u5b9a\u3001\u5ec9\u4ef7\u5e76\u6613\u4e8e\u5236\u5907\u7684\u6709\u673a\u7845\u70f7\u4f5c\u4e3a\u5076\u8054\u53c2\u4e0e\u7269\uff0c\u540c\u65f6\uff0c\u80fd\u591f\u5728\u9178\u6027\u5b98\u80fd\u56e2\u7684\u5b58\u5728\u4e0b\uff0c\u5b9e\u73b0\u9009\u62e9\u6027\u7684\u82b3\u57fa\u5316\u53cd\u5e94\u3002\u6b64\u5916\uff0c\u8be5\u5c0f\u7ec4\u901a\u8fc7\u5bf9\u8fd9\u4e00\u65b0\u578b\u7684\u5076\u8054\u7b56\u7565\u5728\u836f\u7269\u7c7b\u4f3c\u7269\u5206\u5b50\u7684\u5408\u6210\u4ee5\u53ca\u591a\u7ec4\u5206\u53cd\u5e94\u4e2d\u7684\u5e94\u7528\uff0c\u8fdb\u4e00\u6b65\u9610\u660e\u8fd9\u4e00\u5168\u65b0\u7684\u5076\u8054\u53cd\u5e94\u65b9\u6cd5\u5b66\u5177\u6709\u826f\u597d\u7684\u5408\u6210\u5e94\u7528\u4ef7\u503c\u3002<\/p>\n<blockquote><p>Lewis Basic Salt-Promoted Organosilane Coupling Reactions with Aromatic Electrophiles<br \/>\nT. W. Reidl, J. S. Bandar, J. Am. Chem. Soc. \u00a02021, 143, 11939. doi: <a href=\"https:\/\/pubs.acs.org\/doi\/10.1021\/jacs.1c05764\"><u>10.1021\/jacs.1c05764<\/u><\/a><u>.<\/u><\/p><\/blockquote>\n<p><a href=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/2-5.png\"><img loading=\"lazy\" decoding=\"async\" class=\"aligncenter wp-image-40346 size-large\" src=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/2-5-680x287.png\" alt=\"\" width=\"680\" height=\"287\" srcset=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/2-5-680x287.png 680w, https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/2-5-300x127.png 300w, https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/2-5.png 755w\" sizes=\"(max-width: 680px) 100vw, 680px\" \/><\/a><\/p>\n<h4>\u6b63\u6587<\/h4>\n<p>1,1-\u4e8c\u82b3\u57fa\u70f7\u70c3\u662f\u4e00\u7c7b\u5177\u6709\u8f83\u9ad8\u5e94\u7528\u4ef7\u503c\u7684\u6709\u673a\u5206\u5b50\uff0c\u901a\u5e38\u91c7\u7528\u5b98\u80fd\u56e2\u5316\u7684\u82c4\u57fa\u8bd5\u5242\u4e0e\u82b3\u9999\u4eb2\u7535\u5e95\u7269\u4e4b\u95f4\u7684\u5076\u8054\u53cd\u5e94\u7b56\u7565\uff0c\u5b8c\u6210\u4e0a\u8ff0\u5206\u5b50\u7684\u5236\u5907\u3002\u5176\u4e2d\uff0c\u8fc7\u6e21\u91d1\u5c5e\u50ac\u5316\u7684\u82b3\u5364\u6216\u82b3\u57fa\u62df\u5364\u4ee3\u7269\u4e0e\u82c4\u57fa\u9541\u3001\u950c\u4ee5\u53ca\u787c\u5316\u5408\u7269\u4e4b\u95f4\u7684\u5076\u8054\u53cd\u5e94\u65b9\u6cd5\u5b66\u5e94\u7528\u6700\u4e3a\u5e7f\u6cdb\u3002\u7136\u800c\uff0c\u4e0a\u8ff0\u7b56\u7565\u4e2d\uff0c\u901a\u5e38\u9700\u8981\u539f\u4f4d\u5236\u5907\u51fa\u5177\u6709\u8f83\u9ad8\u53cd\u5e94\u6d3b\u6027\u7684\u82c4\u57fa\u8bd5\u5242\uff0c\u56e0\u6b64\uff0c\u5b9e\u9a8c\u64cd\u4f5c\u8f83\u4e3a\u7e41\u7410\u3002\u7531\u6b64\uff0c\u6709\u673a\u5408\u6210\u5316\u5b66\u5bb6\u5f00\u59cb\u81f4\u529b\u4e8e\u8bbe\u8ba1\u5168\u65b0\u7684\u5076\u8054\u53cd\u5e94\u7b56\u7565\uff0c\u8fdb\u800c\u5b9e\u73b01,1-\u4e8c\u82b3\u57fa\u70f7\u70c3\u5206\u5b50\u7684\u9ad8\u6548\u6784\u5efa\u3002<\/p>\n<p>\u82c4\u57fa\u53bb\u8d28\u5b50\u5316\u53cd\u5e94\u65b9\u6cd5\u5b66<sup>[<\/sup><sup>1]<\/sup>\u4f5c\u4e3a\u4e00\u79cd\u6781\u5177\u5438\u5f15\u529b\u7684\u53cd\u5e94\u7b56\u7565\uff0c\u80fd\u591f\u901a\u8fc7\u78b3\u8d1f\u79bb\u5b50\u4e2d\u95f4\u4f53\u7684\u5f62\u6210\uff0c\u8fdb\u800c\u4e0e\u82b3\u57fa\u4eb2\u7535\u5e95\u7269\u5728\u91d1\u5c5e\u50ac\u5316\u5242\u5b58\u5728\u6216\u65e0\u50ac\u5316\u5242\u5b58\u5728\u7684\u6761\u4ef6\u4e0b\uff0c\u5b8c\u6210\u76f8\u5e94\u7684\u5076\u8054\u53cd\u5e94\u8fc7\u7a0b (Figure 1, left)\u3002\u7136\u800c\uff0c\u8fd9\u4e00\u7b56\u7565\u4e2d\uff0c\u5374\u4f34\u968f\u591a\u82b3\u57fa\u5316\u526f\u4ea7\u7269\u7684\u4ea7\u751f\uff0c\u5e76\u4e14\uff0c\u9700\u8981\u9009\u62e9\u5177\u6709\u4e00\u5b9a\u9178\u6027\u7684\u524d\u4eb2\u6838\u5e95\u7269\uff0c\u4f8b\u5982\u4e8c\u82b3\u57fa\u7532\u70f7\u3002\u540c\u65f6\uff0c\u4e0a\u8ff0\u53bb\u8d28\u5b50\u6d3b\u5316\u8fc7\u7a0b\u7684\u5e95\u7269\u5e94\u7528\u8303\u56f4\u540c\u6837\u8f83\u4e3a\u6709\u9650\u3002<\/p>\n<p>\u4e3a\u89e3\u51b3\u4e0a\u8ff0\u95ee\u9898\uff0c\u672c\u8bfe\u9898\u7ec4\u5f00\u59cb\u81f4\u529b\u4e8e\u8bbe\u8ba1\u4e00\u79cd\u91c7\u7528\u78b1\u4fc3\u8fdb\u7684\u5168\u65b0\u7684\u82c4\u4f4d\u82b3\u57fa\u5316\u7b56\u7565\uff0c\u53cd\u5e94\u8fc7\u7a0b\u4e2d\u6d89\u53caLewis\u78b1\u5bf9\u4e8e\u5177\u6709\u4e00\u5b9aLewis\u9178\u6027\u7684\u82c4\u57fa\u5316\u5408\u7269\u7684\u6d3b\u5316\uff0c\u8fdb\u800c\u5b9e\u73b0\u82b3\u57faCsp<sup>2<\/sup>-Csp<sup>3<\/sup>\u952e\u4e4b\u95f4\u7684\u5076\u8054\u8fc7\u7a0b<sup>[<\/sup><sup>2<\/sup><sup>]<\/sup>\u3002\u5176\u4e2d\uff0c\u7531\u4e8e\u82c4\u57fa\u4e09\u7532\u57fa\u7845\u70f7\u5177\u6709\u826f\u597d\u7684\u7a7a\u6c14\u7a33\u5b9a\u6027\u3001\u65e0\u5438\u6e7f\u6027\u4ee5\u53ca\u5ec9\u4ef7\u6613\u5f97\u7b49\u4f18\u52bf\uff0c\u7531\u6b64\u6210\u4e3a\u8f83\u4e3a\u7406\u60f3\u7684\u5076\u8054\u5e95\u7269\u3002\u4ee5\u6b64\u540c\u65f6\uff0c\u6d89\u53ca\u590d\u6742\u82c4\u57fa\u4e09\u7532\u57fa\u7845\u70f7\u5408\u6210<sup>[<\/sup><sup>3<\/sup><sup>]<\/sup>\u7684\u76f8\u5173\u53cd\u5e94\u7b56\u7565\u5df2\u6709\u6587\u732e\u62a5\u9053\u3002\u800c\u4e14\uff0c\u8fc4\u4eca\u4e3a\u6b62\uff0c\u7531\u4e8e\u82c4\u57fa\u4e09\u7532\u57fa\u7845\u70f7\u5206\u5b50\u6240\u5177\u6709\u7684\u9ad8\u5ea6\u7a33\u5b9a\u6027\uff0c\u81f4\u4f7f\u5176\u5728\u91d1\u5c5e\u50ac\u5316\u7684\u4ea4\u53c9\u5076\u8054\u53cd\u5e94\u8fc7\u7a0b\u4e2d\uff0c\u65e0\u6cd5\u8868\u73b0\u51fa\u826f\u597d\u7684\u53cd\u5e94\u6d3b\u6027\uff0c\u8fdb\u800c\u4f7f\u5176\u5728\u82b3\u57fa\u5316\u53cd\u5e94\u65b9\u6cd5\u5b66\u4e2d\u7684\u5e94\u7528\u53d7\u5230\u8f83\u5927\u9650\u5236<sup>[<\/sup><sup>4<\/sup><sup>]<\/sup>\u3002\u4e3a\u8fdb\u4e00\u6b65\u89e3\u51b3\u4e0a\u8ff0\u53cd\u5e94\u8fc7\u7a0b\u4e2d\u5b58\u5728\u7684\u5c40\u9650\uff0c\u540c\u6837\u6709\u6587\u732e\u62a5\u9053\u91c7\u7528\u94af\u50ac\u5316\u4ee5\u53ca\u91d1\u5c5e\u5149\u6c27\u5316\u8fd8\u539f\u50ac\u5316<sup>[<\/sup><sup>5<\/sup><sup>]<\/sup>\u7684\u76f8\u5173\u5076\u8054\u53cd\u5e94\u7b56\u7565 (Figure 1, right)\u3002<\/p>\n<p>\u8fd9\u91cc\uff0cJ. S. Bandar\u8bfe\u9898\u7ec4\u62a5\u9053\u4e00\u79cd\u5168\u65b0\u7684\uff0c\u901a\u8fc7Lewis\u78b1\u6027\u76d0\u8bd5\u5242\u4fc3\u8fdb\u7684\u82c4\u57fa\u4e09\u7532\u57fa\u7845\u70f7\u4e0e\u5404\u7c7b\u82b3\u9999\u4eb2\u7535\u5e95\u7269\u4e4b\u95f4\u7684\u76f4\u63a5\u5076\u8054\u53cd\u5e94\u65b9\u6cd5\u5b66\uff0c\u8fdb\u800c\u83b7\u5f97\u4e00\u7cfb\u5217\u76f8\u5e94\u76841,1-\u4e8c\u82b3\u57fa\u70f7\u70c3\u884d\u751f\u7269 (Figure 1, bottom)\u3002\u503c\u5f97\u6ce8\u610f\u7684\u662f\uff0c\u5728\u8fd9\u4e00\u5168\u65b0\u7684\u5076\u8054\u7b56\u7565\u4e2d\uff0c\u82c4\u4f4d\u7684\u82b3\u57fa\u5316\u80fd\u591f\u4e0e\u6f5c\u5728\u7684\u8d1f\u79bb\u5b50\u526f\u53cd\u5e94\u8fdb\u884c\u6709\u6548\u7684\u7ade\u4e89\uff0c\u8fdb\u800c\u4f7f\u8fd9\u4e00\u65b0\u578b\u7684\u5076\u8054\u53cd\u5e94\u8fc7\u7a0b\uff0c\u80fd\u591f\u4e0e\u5e95\u7269\u4e2d\u5b58\u5728\u7684\u9178\u6027\u4e0e\u4eb2\u7535\u5b98\u80fd\u56e2\u826f\u597d\u5730\u8fdb\u884c\u517c\u5bb9\u3002\u5e76\u4e14\uff0c\u540c\u6837\u80fd\u591f\u826f\u597d\u5730\u5e94\u7528\u4e8e\u5176\u5b83\u7845\u70f7\u5e95\u7269\u4ee5\u53ca\u5176\u5b83\u76f8\u5173\u7684\u53cd\u5e94\u5e8f\u5217\uff0c\u4f8b\u5982\u91c7\u7528\u70ef\u4e19\u57fa\u7845\u70f7\u53c2\u4e0e\u7684\u4e32\u8054\u82b3\u57fa\u5316\/\u5f02\u6784\u5316\u53cd\u5e94\u65b9\u6cd5\u5b66\uff0c\u80fd\u591f\u8f83\u597d\u5730\u5b8c\u6210\u5404\u7c7b\u82b3\u57fa\u70ef\u5206\u5b50\u7684\u6784\u5efa\u3002\u56e0\u6b64\uff0c\u91c7\u7528Lewis\u78b1\u4fc3\u8fdb\u7684\u82b3\u57fa\u5316\u53cd\u5e94\u65b9\u6cd5\u5b66\uff0c\u5177\u6709\u826f\u597d\u7684\u5408\u6210\u5b9e\u7528\u6027\u4ee5\u53ca\u8f83\u4e3a\u5e7f\u6cdb\u7684\u5e95\u7269\u9002\u7528\u8303\u56f4\u3002<\/p>\n<p><a href=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/3-5.png\"><img loading=\"lazy\" decoding=\"async\" class=\"aligncenter wp-image-40347 size-full\" src=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/3-5.png\" alt=\"\" width=\"551\" height=\"618\" srcset=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/3-5.png 551w, https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/3-5-267x300.png 267w\" sizes=\"(max-width: 551px) 100vw, 551px\" \/><\/a><\/p>\n<p>\u540c\u65f6\uff0c\u57282019\u5e74\uff0cJ.\u00a0S. Bandar\u56e2\u961f\u62a5\u9053\u4e00\u79cd\u901a\u8fc7\u6c1f\u79bb\u5b50\u6d3b\u5316\u7684\u70ef\u4e19\u57fa\u4e09\u7532\u57fa\u7845\u70f7\u4e0e\u4e09\u6c1f\u7532\u57fa\u82b3\u70c3\u4e4b\u95f4\u7684\u5355\u9009\u62e9\u6027\u53bb\u6c1f\u70ef\u4e19\u57fa\u5316\u53cd\u5e94\u65b9\u6cd5\u5b66 (monoselective defluoroallylation)<sup>[<\/sup><sup>6<\/sup><sup>]<\/sup>\u3002\u5176\u4e2d\uff0c\u53cd\u5e94\u8fc7\u7a0b\u6d89\u53ca\u8d1f\u79bb\u5b50\u70ef\u4e19\u57fa\u4e2d\u95f4\u4f53\u7684\u5f62\u6210\uff0c\u5e76\u8fdb\u4e00\u6b65\u4e0e\u4e09\u6c1f\u7532\u57fa\u82b3\u70c3\u7ecf\u5386\u5355\u7535\u5b50\u8f6c\u79fb\u8fc7\u7a0b\uff0c\u8fdb\u800c\u4f7fC-F\u952e\u65ad\u88c2\uff0c\u5e76\u901a\u8fc7\u5f62\u6210\u7684\u4e8c\u6c1f\u82c4\u57fa\u81ea\u7531\u57fa\uff0c\u8fdb\u884c\u540e\u7eed\u7684\u70ef\u4e19\u57fa\u5316\u8fc7\u7a0b (Scheme 1a)\u3002\u8fd9\u4e00\u7b56\u7565\u7c7b\u4f3c\u4e8e\u91c7\u7528\u70ef\u4e19\u57fa\u4e09\u7532\u57fa\u7845\u70f7\u8fdb\u884c\u76841,4-\u4e8c\u6c30\u57fa\u82b3\u70c3\u7684\u5149\u8bf1\u5bfc\u7535\u5b50\u8f6c\u79fb (PET)\u70ef\u4e19\u57fa\u5316\u8fc7\u7a0b\uff0c\u5373\u53cd\u5e94\u673a\u7406\u4e2d\uff0cSET\u8fc7\u7a0b\u5148\u4e8eC-C\u952e\u7684\u5f62\u6210\u8fc7\u7a0b<sup>\u00a0[<\/sup><sup>7<\/sup><sup>]<\/sup>\u3002\u540c\u65f6\uff0c\u5728PET\u8fc7\u7a0b\u7684\u7814\u7a76\u4e2d\uff0c\u8be5\u5c0f\u7ec4\u540c\u6837\u5bf9\u82c4\u57fa\u4e09\u7532\u57fa\u7845\u70f7\u7684\u5e94\u7528\u8fdb\u884c\u7814\u7a76\u3002\u7136\u800c\uff0c\u4e0a\u8ff0\u7684PET\u70ef\u4e19\u57fa\u5316\u8fc7\u7a0b\u5177\u6709\u8f83\u4f4e\u7a0b\u5ea6\u7684\u533a\u57df\u9009\u62e9\u6027\u4ee5\u53ca\u526f\u4ea7\u7269\u5f62\u6210\u7684\u95ee\u9898\uff0c\u540c\u65f6\uff0c\u53cd\u5e94\u8fc7\u7a0b\u4e2d\u9700\u8981\u8fdb\u4e00\u6b65\u91c7\u7528\u7d2b\u5916\u5149\u8f90\u5c04 (Scheme 1b)<sup>\u00a0[<\/sup><sup>8<\/sup><sup>]<\/sup>\u3002\u57fa\u4e8e\u4e0a\u8ff0\u7684\u7814\u7a76\u62a5\u9053\uff0c\u4f5c\u8005\u5047\u8bbe\uff0c\u6709\u673a\u4e09\u7532\u57fa\u7845\u70f7\u901a\u8fc7Lewis\u78b1\u7684\u6d3b\u5316\uff0c\u80fd\u591f\u826f\u597d\u5730\u4fc3\u8fdb\u5176\u4e0e\u5176\u5b83\u82b3\u9999\u4eb2\u7535\u5e95\u7269\u4e4b\u95f4\u7684\u76f4\u63a5\u5076\u8054\u8fc7\u7a0b\u3002<\/p>\n<p>\u4e3a\u8fdb\u4e00\u6b65\u9a8c\u8bc1\u8fd9\u4e00\u5047\u8bbe\uff0c\u4f5c\u8005\u9009\u62e94-\u6c30\u57fa\u5421\u5576 (<strong>1<\/strong>)\u4e0e\u82c4\u57fa\u4e09\u7532\u57fa\u7845\u70f7 (<strong>2<\/strong>) \u4f5c\u4e3a\u6a21\u578b\u5e95\u7269\uff0c\u5bf9\u76f8\u5e94\u7684Lewis\u78b1\u8fdb\u884c\u7b5b\u9009\u3002\u6700\u7ec8\uff0c\u8be5\u5c0f\u7ec4\u786e\u5b9a\u51fa\u6700\u4f73\u7684\u53cd\u5e94\u6761\u4ef6\u4e3a\uff1a\u91c7\u75281\u00a0eq.\u7684\u6c1f\u5316\u94ef\u4e3a\u78b1\uff0c\u540c\u65f6\u52a0\u51651.1\u00a0eq.18-crown-6\uff0c\u5728DMSO\u4f5c\u4e3a\u53cd\u5e94\u6eb6\u5242\u4ee5\u53ca\u5ba4\u6e29\u7684\u53cd\u5e94\u6761\u4ef6\u4e0b\uff0c\u53cd\u5e94\u65f6\u95f4\u4e3a3 h\uff0c\u8fdb\u800c\u83b7\u5f9795%\u6536\u7387\u7684\u5076\u8054\u4ea7\u7269<strong>3<\/strong>\u00a0(Scheme 1c)\u3002<\/p>\n<p><a href=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/4-5.png\"><img loading=\"lazy\" decoding=\"async\" class=\"aligncenter wp-image-40348 size-full\" src=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/4-5.png\" alt=\"\" width=\"557\" height=\"703\" srcset=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/4-5.png 557w, https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/4-5-238x300.png 238w\" sizes=\"(max-width: 557px) 100vw, 557px\" \/><\/a><\/p>\n<p>\u5728\u4e0a\u8ff0\u7684\u6700\u4f73\u53cd\u5e94\u6761\u4ef6\u4e0b\uff0c\u4f5c\u8005\u9996\u5148\u5bf9\u4e0a\u8ff0\u5076\u8054\u8fc7\u7a0b\u7684\u5e95\u7269\u5e94\u7528\u8303\u56f4\u8fdb\u884c\u8003\u5bdf (Table 1)\u3002\u7814\u7a76\u8868\u660e\uff0c\u7f3a\u7535\u5b50\u7684\u6c30\u57fa\u5421\u5576\u4e0e\u6c30\u57fa\u82ef\u5e95\u7269\u80fd\u591f\u4e0e\u4e00\u7cfb\u5217\u4e00\u7ea7\u3001\u4e8c\u7ea7\u4ee5\u53ca\u4e09\u7ea7\u82c4\u57fa\u7845\u70f7\u5728\u4e0a\u8ff0\u7684\u6807\u51c6\u53cd\u5e94\u6761\u4ef6\u4e0b\uff0c\u8fdb\u884c\u76f8\u5e94\u7684\u5076\u8054\u8fc7\u7a0b\uff0c\u5e76\u83b7\u5f97\u6700\u7ec8\u7684\u76ee\u6807\u4ea7\u7269<strong>4<\/strong>&#8211;<strong>24<\/strong>\uff0c\u6536\u7387\u4e3a50-94%\u3002\u540c\u65f6\uff0c\u53cd\u5e94\u8fc7\u7a0b\u4e2d\u8868\u73b0\u51fa\u4f18\u826f\u7684\u5b98\u80fd\u56e2\u517c\u5bb9\u6027\u3002\u4e4b\u540e\uff0c\u8be5\u5c0f\u7ec4\u89c2\u5bdf\u5230\uff0c\u5177\u6709<em>\u03b1<\/em>-\u6742\u539f\u5b50\u7684\u82c4\u57fa\u7845\u70f7\u5e95\u7269 (<strong>25<\/strong>&#8211;<strong>27<\/strong>)\u4ee5\u53ca\u836f\u7269\u5206\u5b50paroxetine\u00a0(<strong>28<\/strong>)\u4e0ebepotastine\u00a0(<strong>29<\/strong>)\uff0c\u5747\u80fd\u591f\u4e0e\u4e0a\u8ff0\u7684\u6807\u51c6\u53cd\u5e94\u6761\u4ef6\u826f\u597d\u5730\u8fdb\u884c\u517c\u5bb9\u3002<\/p>\n<p><a href=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/5-5.png\"><img loading=\"lazy\" decoding=\"async\" class=\"aligncenter wp-image-40349 size-large\" src=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/5-5-454x1024.png\" alt=\"\" width=\"454\" height=\"1024\" srcset=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/5-5-454x1024.png 454w, https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/5-5-133x300.png 133w, https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/5-5-681x1536.png 681w, https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/5-5.png 747w\" sizes=\"(max-width: 454px) 100vw, 454px\" \/><\/a><\/p>\n<p>\u4e4b\u540e\uff0c\u4f5c\u8005\u5bf9\u5404\u7c7b\u82b3\u57fa\u4eb2\u7535\u5e95\u7269\u7684\u5e94\u7528\u8303\u56f4\u8fdb\u884c\u8003\u5bdf (Scheme 2)\u3002\u7814\u7a76\u8868\u660e\uff0c2-\u6c2f-1,3-\u5511\u7c7b\u4e3a\u4e0a\u8ff0\u5076\u8054\u8fc7\u7a0b\u7684\u6709\u6548\u5e95\u7269 (<strong>30<\/strong>&#8211;<strong>32<\/strong>)\u3002\u5e76\u4e14\uff0c\u5177\u6709\u6269\u5f20<em>\u03c0-<\/em>\u4f53\u7cfb\u7684\u6c2f\u4ee3\u7269\uff0c\u4f8b\u59821,3-\u4e8c\u6c2f\u5f02\u55b9\u5549 (<strong>33<\/strong>)\u30019-\u6c2f\u5416\u5576(<strong>34<\/strong>)\u4ee5\u53ca\u6297\u80bf\u7624\u836f\u7269\u5206\u5b50imiquimod\u7684\u6c2f\u55b9\u5549\u884d\u751f\u7269 (<strong>35<\/strong>)\u540c\u6837\u80fd\u591f\u4e0e\u4e0a\u8ff0\u7684\u6700\u4f73\u53cd\u5e94\u6761\u4ef6\u826f\u597d\u5730\u517c\u5bb9\u3002\u540c\u65f6\uff0c\u4f5c\u8005\u53d1\u73b0\uff0c\u5c3d\u7ba14-\u5364\u5421\u5576\u5728\u4e0a\u8ff0\u7684\u6807\u51c6\u53cd\u5e94\u6761\u4ef6\u4e0b\uff0c\u65e0\u6cd5\u6709\u6548\u5730\u8fdb\u884c\u76f8\u5e94\u7684\u5076\u8054\u8fc7\u7a0b\uff0c\u7136\u800c\uff0c\u4e0a\u8ff0\u7684\u6807\u51c6\u53cd\u5e94\u4f53\u7cfb\u5bf9\u4e8e4-\u78fa\u9170\u57fa\u5421\u5576 (<strong>36<\/strong>)\u5e95\u7269\uff0c\u5219\u80fd\u591f\u83b7\u5f97\u5177\u6709\u826f\u597d\u6536\u7387\u7684\u5076\u8054\u4ea7\u7269 (Scheme 2b)\u3002\u6b64\u5916\uff0c\u4f5c\u8005\u89c2\u5bdf\u5230\uff0c\u5c064-\u6c2f\u5421\u5576<strong>37<\/strong>\u8f6c\u5316\u4e3a\u78fa\u9170\u5316\u4ea7\u7269<strong>38<\/strong><strong>\u00a0<\/strong>(Scheme 2c)\u4e4b\u540e\uff0c\u518d\u4e0e\u82c4\u57fa\u7845\u70f7\u8fdb\u884c\u4e0a\u8ff0\u7684\u5076\u8054\u8fc7\u7a0b\uff0c\u6700\u7ec8\u80fd\u591f\u987a\u5229\u83b7\u5f97\u76f8\u5e94\u7684\u4e8c\u82b3\u57fa\u70f7\u70c3\u4ea7\u7269<strong>39<\/strong>\u3002<\/p>\n<p><a href=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/6-4.png\"><img loading=\"lazy\" decoding=\"async\" class=\"aligncenter wp-image-40350 size-full\" src=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/6-4.png\" alt=\"\" width=\"480\" height=\"632\" srcset=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/6-4.png 480w, https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/6-4-228x300.png 228w\" sizes=\"(max-width: 480px) 100vw, 480px\" \/><\/a><\/p>\n<p>&nbsp;<\/p>\n<p><a href=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/7-4.png\"><img loading=\"lazy\" decoding=\"async\" class=\"aligncenter wp-image-40351 size-full\" src=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/7-4.png\" alt=\"\" width=\"490\" height=\"66\" srcset=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/7-4.png 490w, https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/7-4-300x40.png 300w\" sizes=\"(max-width: 490px) 100vw, 490px\" \/><\/a><\/p>\n<p>\u63a5\u4e0b\u6765\uff0c\u4f5c\u8005\u8fdb\u4e00\u6b65\u5bf9\u6709\u673a\u7845\u5316\u5408\u7269<strong>40<\/strong>\u4e0e\u5404\u7c7b\u82b3\u57fa\u4e0e\u6742\u82b3\u57fa\u4eb2\u7535\u5e95\u7269\u4e4b\u95f4\u7684\u5076\u8054\u8fc7\u7a0b\u8fdb\u884c\u8fdb\u4e00\u6b65\u7814\u7a76 (Figure 2)\u3002\u8be5\u5c0f\u7ec4\u89c2\u5bdf\u5230\uff0c\u901a\u8fc7\u5316\u5408\u7269<strong>40<\/strong>\u53c2\u4e0e\u7684\u5076\u8054\u8fc7\u7a0b\uff0c\u6700\u7ec8\u80fd\u591f\u83b7\u5f97\u4e00\u7cfb\u5217\u76f8\u5e94\u7684chlorpheniramine\u7c7b\u4f3c\u7269\uff0c\u4f8b\u5982<strong>41<\/strong>&#8211;<strong>48<\/strong>\uff0c\u6536\u7387\u4e3a45-95%\u3002<\/p>\n<p><a href=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/8-3.png\"><img loading=\"lazy\" decoding=\"async\" class=\"aligncenter wp-image-40352 size-large\" src=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/8-3-680x539.png\" alt=\"\" width=\"680\" height=\"539\" srcset=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/8-3-680x539.png 680w, https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/8-3-300x238.png 300w, https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/8-3.png 749w\" sizes=\"(max-width: 680px) 100vw, 680px\" \/><\/a><\/p>\n<p>\u6b64\u5916\uff0c\u4f5c\u8005\u8fd8\u540c\u6837\u5bf9\u4e0a\u8ff0\u5076\u8054\u8fc7\u7a0b\u7684\u9009\u62e9\u6027\u8fdb\u884c\u6df1\u5165\u7814\u7a76 (Scheme 3)\u3002\u9996\u5148\uff0c\u4f5c\u8005\u53d1\u73b0\uff0c\u82b3\u57fa\u4eb2\u7535\u5e95\u7269<strong>2<\/strong>\u5728\u4e0a\u8ff0\u7684\u6807\u51c6\u53cd\u5e94\u6761\u4ef6\u4e0b\uff0c\u80fd\u591f\u83b7\u5f9780%\u6536\u7387\u7684\u7532\u82ef\u4ea7\u7269 (Scheme 3a)\u3002\u8fdb\u800c\u8868\u660e\u82c4\u57fa\u7684\u8d28\u5b50\u5316\u8fc7\u7a0b\u4e0e\u82b3\u57fa\u5316\u8fc7\u7a0b\u4e4b\u95f4\u5b58\u5728\u7ade\u4e89\u3002\u7136\u800c\uff0c\u8f83\u4e3a\u6709\u8da3\u7684\u662f\uff0c\u5728\u9178\u6027\u663e\u8457\u9ad8\u4e8e\u7532\u82ef\u7684\u53cd\u5e94\u6eb6\u5242\u4e2d\uff0c4-\u6c30\u57fa\u5421\u5576\u7684\u82c4\u57fa\u5316\u8fc7\u7a0b\u540c\u6837\u80fd\u591f\u8f83\u597d\u5730\u8fdb\u884c (Scheme 3b)\u3002\u6b64\u5916\uff0c\u4f5c\u8005\u5728\u9009\u62e9\u82c4\u57fa\u7845\u70f7\u7684\u4e24\u79cd\u533a\u57df\u5f02\u6784\u4f53 (<strong>50<\/strong>\u4e0e<strong>52<\/strong>)\u00a0\u53c2\u4e0e\u7684\u5076\u8054\u8fc7\u7a0b\u4e2d\u53d1\u73b0\uff0c\u4e0a\u8ff0\u82c4\u57fa\u7845\u70f7\u7684\u82b3\u57fa\u5316\u8fc7\u7a0b\u80fd\u591f\u533a\u57df\u4e13\u4e00\u6027\u5730\u5728\u5177\u6709TMS\u57fa\u56e2\u7684\u4f4d\u7f6e\u8fdb\u884c (Scheme 3c)\u3002\u8fdb\u800c\u8868\u660e\uff0c\u82b3\u57fa\u5316\u8fc7\u7a0b\u5728\u8d28\u5b50\u8f6c\u79fb\u4e4b\u524d\u8fdb\u884c\u3002\u540c\u65f6\uff0c\u7814\u7a76\u53d1\u73b0\uff0c\u5177\u6709\u4e00\u5b9a\u9178\u6027\u7684\u4e8c\u82b3\u57fa\u70f7\u70c3\u4ea7\u7269\u7684\u53bb\u8d28\u5b50\u5316\u8fc7\u7a0b\u53d7\u5230\u6781\u5927\u7a0b\u5ea6\u7684\u6291\u5236\uff0c\u8fdb\u800c\u80fd\u591f\u8fdb\u4e00\u6b65\u6291\u5236\u591a\u82b3\u57fa\u5316\u526f\u53cd\u5e94\u8fc7\u7a0b\u7684\u8fdb\u884c\u3002\u4e0a\u8ff0\u4e8b\u5b9e\u540c\u6837\u8868\u660e\uff0cLewis\u78b1\u4fc3\u8fdb\u7684\u82b3\u57fa\u5316\u53cd\u5e94\u65b9\u6cd5\u5b66\u5177\u6709\u663e\u8457\u7684\u4f18\u52bf\uff0c\u800c\u5728Br\u00f8nsted\u78b1\u53c2\u4e0e\u7684\u82b3\u57fa\u5316\u8fc7\u7a0b\u4e2d\uff0c\u5219\u65e0\u6cd5\u5f62\u6210\u76f8\u5e94\u7684\u82c4\u57fa\u78b3\u8d1f\u79bb\u5b50\u3002\u540c\u65f6\uff0c\u53ef\u80fd\u51fa\u73b0\u591a\u91cd\u82b3\u57fa\u5316\u7684\u526f\u53cd\u5e94\u3002\u5e76\u4e14\uff0c\u5728\u5177\u6709\u591a\u91cd\u82c4\u57fa\u4f4d\u7f6e\u53d6\u4ee3\u7684\u76f8\u5173\u5e95\u7269\u4e2d\uff0c\u65e0\u6cd5\u83b7\u5f97\u8f83\u4e3a\u4f18\u826f\u7684\u9009\u62e9\u6027 (\u8be6\u89c1<a href=\"https:\/\/pubs.acs.org\/doi\/suppl\/10.1021\/jacs.1c05764\/suppl_file\/ja1c05764_si_001.pdf\"><u>Supporting Information<\/u><\/a>)\u3002<\/p>\n<p><a href=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/9-1.png\"><img loading=\"lazy\" decoding=\"async\" class=\"aligncenter wp-image-40353 size-full\" src=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/9-1.png\" alt=\"\" width=\"550\" height=\"597\" srcset=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/9-1.png 550w, https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/9-1-276x300.png 276w\" sizes=\"(max-width: 550px) 100vw, 550px\" \/><\/a><\/p>\n<p>\u4e3a\u89e3\u91ca\u4e0a\u8ff0\u82b3\u57fa\u5316\u8fc7\u7a0b\u4e2d\u7684\u9ad8\u5ea6\u9009\u62e9\u6027\uff0c\u4f5c\u8005\u5047\u8bbe\u82c4\u57fa\u8d1f\u79bb\u5b50\u4e2d\u95f4\u4f53\u901a\u8fc7\u6781\u6027\u6216SET\u673a\u7406\uff0c\u8fdb\u884c\u5feb\u901f\u7684\u82b3\u9999\u53d6\u4ee3\u8fc7\u7a0b (Figure 3)\u3002\u5176\u4e2d\uff0cSET\u673a\u7406\u8fc7\u7a0b\u901a\u8fc7\u78b1\u6027\u6761\u4ef6\u4fc3\u8fdb\uff0c\u5e76\u7c7b\u4f3c\u4e8e\u6709\u673a\u7845\u70f7\u4e0e1,4-\u4e8c\u6c30\u57fa\u82b3\u70c3\u4e4b\u95f4PET\u53cd\u5e94\u3002\u5e76\u4e14\uff0c\u6781\u6027\u673a\u7406\u540c\u6837\u5177\u6709\u5408\u7406\u6027\uff0c\u56e0\u4e3a\u6c30\u57fa\u82b3\u70c3\u4e0e\u78fa\u9170\u57fa\u82b3\u70c3\u5206\u5b50\u80fd\u591f\u53c2\u4e0e\u901a\u8fc7\u5178\u578b\u7684\u52a0\u6210-\u6d88\u9664\u8fc7\u7a0b\u8fdb\u884c\u7684\u53d6\u4ee3\u53cd\u5e94\u3002\u800c\u5728\u8d1f\u79bb\u5b50\u8bd5\u5242\u5bf9\u4e8e\u7c7b\u4f3c\u4eb2\u7535\u5e95\u7269\u7684\u52a0\u6210\u8fc7\u7a0b\u4e2d\uff0c\u51c6\u786e\u533a\u5206\u4e0a\u8ff0\u4e24\u79cd\u4e0d\u540c\u7684\u673a\u7406\u8def\u5f84\uff0c\u5219\u5177\u6709\u8f83\u5927\u7684\u6311\u6218\u6027\u3002\u5e76\u4e14\uff0c\u4e0a\u8ff0\u7684\u5076\u8054\u53cd\u5e94\u8fc7\u7a0b\u4e2d\u7684\u76f8\u5173\u5b9e\u9a8c\u7ed3\u8bba\uff0c\u5747\u80fd\u591f\u901a\u8fc7\u6781\u6027\u4e0eSET\u4e24\u79cd\u4e0d\u540c\u7684\u673a\u7406\u8def\u5f84\u8fdb\u884c\u5408\u7406\u7684\u89e3\u91ca\u3002\u540c\u65f6\uff0c\u4f5c\u8005\u53d1\u73b0\u4e0a\u8ff0\u7684\u5076\u8054\u53cd\u5e94\u65b9\u5f0f\u53ef\u80fd\u5177\u6709\u76f8\u5173\u7684\u5e95\u7269\u4f9d\u8d56\u6027\uff0c\u5c3d\u7ba1\u76f8\u5e94\u7684\u82b3\u57fa\u5316\u8fc7\u7a0b\u80fd\u591f\u4e0e\u5176\u5b83\u901a\u8fc7\u6f5c\u5728\u8d1f\u79bb\u5b50\u4e2d\u95f4\u4f53\u5f15\u53d1\u7684\u526f\u53cd\u5e94\u8fc7\u7a0b\u6709\u6548\u5730\u8fdb\u884c\u7ade\u4e89\u3002<\/p>\n<p><a href=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/10.png\"><img loading=\"lazy\" decoding=\"async\" class=\"aligncenter wp-image-40354 size-large\" src=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/10-680x315.png\" alt=\"\" width=\"680\" height=\"315\" srcset=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/10-680x315.png 680w, https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/10-300x139.png 300w, https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/10-370x170.png 370w, https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/10.png 762w\" sizes=\"(max-width: 680px) 100vw, 680px\" \/><\/a><\/p>\n<p>\u901a\u8fc7\u4e0a\u8ff0\u7814\u7a76\uff0c\u4f5c\u8005\u8bbe\u60f3\uff0c\u6709\u673a\u7845\u70f7\u7684\u82b3\u57fa\u5316\u8fc7\u7a0b\u540c\u6837\u80fd\u591f\u4e0e\u78b1\u4fc3\u8fdb\u7684\u5176\u5b83\u5408\u6210\u8f6c\u5316\u8fc7\u7a0b\u8fdb\u884c\u6709\u6548\u5730\u7ed3\u5408 (Scheme 4)\u3002\u9996\u5148\uff0c\u4f5c\u8005\u53d1\u73b0\uff0c\u901a\u8fc7\u70ef\u4e19\u57fa\u4e09\u7532\u57fa\u7845\u70f7\u5f62\u6210\u7684\u70ef\u4e19\u57fa\u82b3\u70c3\u4e2d\u95f4\u4f53\uff0c\u80fd\u591f\u8fdb\u4e00\u6b65\u7ecf\u5386\u540e\u7eed\u7684\u7acb\u4f53\u9009\u62e9\u6027\u5f02\u6784\u5316\u8fc7\u7a0b\uff0c\u5e76\u83b7\u5f97\u76f8\u5e94\u7684\u70ef\u4ea7\u7269<strong>54<\/strong>\u3001<strong>55<\/strong>\u4e0e<strong>56<\/strong><strong>\u00a0<\/strong>(Scheme 4a)\u3002\u4e4b\u540e\uff0c\u8be5\u5c0f\u7ec4\u8fdb\u4e00\u6b65\u8bbe\u8ba1\u51fa\u4e00\u79cd\u6709\u673a\u7845\u70f7\u3001\u82b3\u57fa\u4eb2\u7535\u5e95\u7269\u4e0eMichael\u53d7\u4f53\u4e4b\u95f4\u7684\u4e09\u7ec4\u5206\u5076\u8054\u7b56\u7565\u3002\u4f5c\u8005\u5047\u8bbe\u53cd\u5e94\u8fc7\u7a0b\u4e2d\uff0c\u9996\u5148\u8fdb\u884c\u6709\u673a\u7845\u70f7\u4e0e\u82b3\u57fa\u4eb2\u7535\u5e95\u7269\u4e4b\u95f4\u9009\u62e9\u6027\u7684\u82c4\u57fa\u82b3\u57fa\u5316\u6b65\u9aa4\uff0c\u4e4b\u540e\uff0c\u901a\u8fc7\u5269\u4f59\u6709\u673a\u7845\u70f7\u4e0e\u8d1f\u79bb\u5b50\u7684\u7ed3\u5408\uff0c\u8fdb\u800c\u5f15\u53d1\u540e\u7eed\u7684Michael\u52a0\u6210\u53cd\u5e94 (Scheme 4b)\u3002\u540c\u65f6\uff0c\u4f5c\u8005\u53d1\u73b0\uff0c<em>\u03b3<\/em><em>,<\/em><em>\u03b3<\/em>-\u4e8c\u82b3\u57fa\u9170\u80fa<strong>57<\/strong>\u4e0e<strong>58<\/strong>\u540c\u6837\u80fd\u591f\u901a\u8fc7\u4e0a\u8ff0\u7684\u4e09\u7ec4\u5206\u53cd\u5e94\u7b56\u7565\u8fdb\u884c\u6709\u6548\u7684\u5236\u5907\u3002\u4e4b\u540e\uff0c\u8be5\u5c0f\u7ec4\u89c2\u5bdf\u5230\uff0c\u91c7\u7528\u7532\u57fa\u70ef\u4e19\u57fa\u4e09\u7532\u57fa\u7845\u70f7\u5e95\u7269\u65f6\uff0c\u80fd\u591f\u901a\u8fc7\u78b1\u4fc3\u8fdb\u7684\u4e09\u6b65\u9009\u62e9\u6027\u7684\u53cd\u5e94\u8fc7\u7a0b (\u5373\u82b3\u57fa\u5316\u3001\u52a0\u6210\u4e0e\u70ef\u57fa\u5f02\u6784\u5316)\uff0c\u6700\u7ec8\u5f62\u6210\u56db\u53d6\u4ee3\u70ef\u57fa\u5316\u5408\u7269<strong>59<\/strong>\u3002<\/p>\n<p><a href=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/11.png\"><img loading=\"lazy\" decoding=\"async\" class=\"aligncenter wp-image-40355 size-full\" src=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/11.png\" alt=\"\" width=\"550\" height=\"709\" srcset=\"https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/11.png 550w, https:\/\/assets.www.gsbet888.com\/uploads\/2021\/10\/11-233x300.png 233w\" sizes=\"(max-width: 550px) 100vw, 550px\" \/><\/a><\/p>\n<h4><strong>\u603b\u7ed3<\/strong><\/h4>\n<p>\u7f8e\u56fdColorado\u5dde\u7acb\u5927\u5b66\u7684J. S. Bandar\u8bfe\u9898\u7ec4\u62a5\u9053\u4e00\u79cd\u901a\u8fc7Lewis\u78b1\u6027\u76d0\u8bd5\u5242\u4fc3\u8fdb\u7684\u82c4\u57fa\u4ee5\u53ca\u70ef\u4e19\u57fa\u4e09\u7532\u57fa\u7845\u70f7\u4e0e(\u6742)\u82b3\u57fa\u8148\u3001\u781c\u4ee5\u53ca\u6c2f\u4ee3\u7269\u4e4b\u95f4\u7684\u5076\u8054\u53cd\u5e94\u65b9\u6cd5\u5b66\u3002\u5e76\u4e14\uff0c\u901a\u8fc7\u8fd9\u4e00\u5168\u65b0\u7684\u5076\u8054\u7b56\u7565\uff0c\u80fd\u591f\u4ee5\u4f18\u826f\u7684\u533a\u57df\u9009\u62e9\u6027\u4e0e\u5355\u9009\u62e9\u6027\u00a0(monoselectivity)\uff0c\u83b7\u5f97\u4e00\u7cfb\u52171,1-\u4e8c\u82b3\u57fa\u70f7\u70c3\u4ee5\u53ca\u82b3\u57fa\u70ef\u884d\u751f\u7269\u3002\u540c\u65f6\uff0c\u4e0a\u8ff0\u7b56\u7565\u4e0e\u73b0\u6709\u7684\u5408\u6210\u8f6c\u5316\u65b9\u6cd5\u5b66\u5f62\u6210\u6709\u6548\u7684\u4e92\u8865\u3002\u6b64\u5916\uff0c\u8be5\u5c0f\u7ec4\u901a\u8fc7\u4e0a\u8ff0\u5076\u8054\u7b56\u7565\u5728\u836f\u7269\u7c7b\u4f3c\u7269\u5206\u5b50\u7684\u5408\u6210\u4ee5\u53ca\u5728\u591a\u7ec4\u5206\u53cd\u5e94\u4e2d\u7684\u5e94\u7528\uff0c\u8fdb\u4e00\u6b65\u9610\u660e\u8fd9\u4e00\u5168\u65b0\u7684\u5076\u8054\u53cd\u5e94\u65b9\u6cd5\u5b66\u5177\u6709\u826f\u597d\u7684\u5408\u6210\u5e94\u7528\u524d\u666f\u3002<\/p>\n<h4><strong><b>\u53c2\u8003\u6587\u732e<\/b><\/strong><\/h4>\n[1]\u00a0(a) M. Li, S. Berritt, L. Matuszewski, G. Deng, A. Pascual-Escudero, G. B. Panetti, M. Poznik, X. Yang, J. J. Chruma, P. J.\u00a0Walsh, <em><i>J. Am. Chem. Soc.<\/i><\/em><strong><em><b><i>\u00a0<\/i><\/b><\/em><\/strong><strong><b>2017<\/b><\/strong>,<em><i>\u00a0139<\/i><\/em>, 16327.\u00a0doi:\u00a0<a href=\"https:\/\/doi.org\/10.1021\/jacs.7b09394\"><u>10.1021\/jacs.7b09394<\/u><\/a><u>.<\/u><\/p>\n<p>(b) X. Ji, T. Huang, W. Wu, F. Liang, S. Cao, <em><i>Org. Lett.<\/i><\/em>\u00a0<strong><b>2015<\/b><\/strong>, <em><i>17<\/i><\/em>, 5096.\u00a0doi:\u00a0<a href=\"https:\/\/doi.org\/10.1021\/jacs.7b09394\"><u>10.1021\/jacs.7b09394<\/u><\/a><u>.<\/u><\/p>\n[2]\u00a0M. Takeda, K. Nagao, H.\u00a0Ohmiya, <em><i>Angew. Chem. Int. Ed.<\/i><\/em>\u00a0<strong><b>2020<\/b><\/strong>, <em><i>59<\/i><\/em>, 22460. doi:\u00a0<a href=\"https:\/\/doi.org\/10.1002\/anie.202010251\"><u>10.1002\/anie.202010251<\/u><\/a><u>.<\/u><\/p>\n[3]\u00a0(a) S. Utsumi, T. Katagiri, K. Uneyama, <em>Tetrahedron<\/em>\u00a0<strong>2012<\/strong>, <em>68<\/em>, 1085. doi:\u00a0<a href=\"https:\/\/doi.org\/10.1016\/j.tet.2011.11.082\"><u>10.1016\/j.tet.2011.11.082<\/u><\/a><u>.<\/u><\/p>\n<p>(b) P. K. Kundu, S. K.\u00a0Ghosh, <em>Tetrahedron <\/em><strong>2010<\/strong>, <em>66<\/em>, 8562.\u00a0doi:\u00a0<a href=\"https:\/\/doi.org\/10.1016\/j.tet.2010.09.001\"><u>10.1016\/j.tet.2010.09.001<\/u><\/a><u>.<\/u><\/p>\n[4]\u00a0(a) Y. Wu, S. Bouvet, S. Izquierdo, A.\u00a0Shafir, <em><i>Angew. Chem. Int. Ed.<\/i><\/em>\u00a0<strong><b>2019<\/b><\/strong>, <em><i>58<\/i><\/em>, 2617. doi:\u00a0<a href=\"https:\/\/doi.org\/10.1002\/anie.201809657\"><u>10.1002\/anie.201809657<\/u><\/a><u>.<\/u><\/p>\n<p>(b) J. Dong, X. Wang, Z. Wang, H. Song, Y. Liu, Q. Wang, <em><i>Org. Chem. Front.<\/i><\/em>\u00a0<strong><b>2019<\/b><\/strong>, <em><i>6<\/i><\/em>,\u00a02902. doi:\u00a0<a href=\"https:\/\/doi.org\/10.1039\/C9QO00690G\"><u>10.1039\/C9QO00690G<\/u><\/a><u>.<\/u><\/p>\n<p>(c) M. Puthanveedu, V. Polychronidou, A.\u00a0P. Antonchick, <em><i>Org. Lett.<\/i><\/em>\u00a0<strong><b>2019<\/b><\/strong>, <em><i>21<\/i><\/em>, 3407.\u00a0doi:\u00a0<a href=\"https:\/\/doi.org\/10.1021\/acs.orglett.9b01141\"><u>10.1021\/acs.orglett.9b01141<\/u><\/a><u>.<\/u><\/p>\n[5]\u00a0(a) K. Itami, M. Mineno, T. Kamei, J. Yoshida, <em>Org. Lett.<\/em>\u00a0<strong>2002<\/strong>,<em>\u00a04<\/em>,\u00a03635. doi:\u00a0<a href=\"https:\/\/doi.org\/10.1021\/ol026573t\"><u>10.1021\/ol026573t<\/u><\/a><u>.<\/u><\/p>\n<p>(b) V. Corc\u00e9, L.-M. Chamoreau, E. Derat, J.-\u00a0P. Goddard, C. Ollivier, L. Fensterbank, <em>Angew. Chem. Int. Ed.<\/em>\u00a0<strong>2015<\/strong>, <em>54<\/em>,\u00a011414.\u00a0doi:\u00a0<a href=\"https:\/\/doi.org\/10.1002\/anie.201504963\"><u>10.1002\/anie.201504963<\/u><\/a><u>.<\/u><\/p>\n[6]\u00a0C. Luo, J. S. Bandar, <em>J. Am. Chem. Soc.<\/em>\u00a0<strong>2019<\/strong>, <em>141<\/em>, 14120.\u00a0doi:\u00a0<a href=\"https:\/\/doi.org\/10.1021\/jacs.9b07766\"><u>10.1021\/jacs.9b07766<\/u><\/a><u>.<\/u><\/p>\n[7]\u00a0Y. Liu, H. Li, S.<em><i>\u00a0<\/i><\/em>Chiba, <em><i>Org. Lett.<\/i><\/em>\u00a0<strong><b>2021<\/b><\/strong>,<em><i>\u00a023<\/i><\/em>, 427.\u00a0doi:\u00a0<a href=\"https:\/\/doi.org\/10.1021\/acs.orglett.0c03935\"><u>10.1021\/acs.orglett.0c03935<\/u><\/a><u>.<\/u><\/p>\n[8]\u00a0Y. Deng, Q. Liu, A. B. Smith, III. <em><i>J. Am. Chem. Soc. <\/i><\/em><strong><b>2017<\/b><\/strong>, <em><i>139<\/i><\/em>,\u00a09487.\u00a0doi:\u00a0<a href=\"https:\/\/doi.org\/10.1021\/jacs.7b05165\"><u>10.1021\/jacs.7b05165<\/u><\/a><u>.<\/u><\/p>\n","protected":false},"excerpt":{"rendered":"\u672c\u6587\u4f5c\u8005\uff1a\u6749\u6749 \u5bfc\u8bfb \u8fd1\u65e5\uff0c\u7f8e\u56fdColorado\u5dde\u7acb\u5927\u5b66 (Colorado State\u00a0University)\u7684J.\u00a0S. Bandar\u8bfe\u9898\u7ec4\u62a5\u9053\u4e00\u79cd\u901a\u8fc7Lewis\u78b1\u6027\u76d0\u8bd5\u5242\u4fc3\u8fdb\u7684\u82c4\u57fa\u4e09\u7532\u57fa\u7845\u70f7\u4e0e(\u6742)\u82b3\u57fa\u8148\u3001\u781c\u4ee5\u53ca\u6c2f\u4ee3\u4e4b\u95f4\u7684\u4ea4\u53c9\u5076\u8054\u53cd\u5e94\u65b9\u6cd5\u5b66\uff0c\u8fdb\u800c\u83b7\u5f97\u4e00\u7cfb\u52171,1-\u4e8c\u82b3\u57fa\u70f7\u70c3\u884d\u751f\u7269\u3002\u503c\u5f97\u6ce8\u610f\u7684\u662f\uff0c\u8fd9\u4e00\u5168\u65b0\u7684\u5076\u8054\u7b56\u7565\u4e2d\uff0c\u9009\u62e9\u7a33\u5b9a\u3001\u5ec9\u4ef7\u5e76\u6613\u4e8e\u5236\u5907\u7684\u6709\u673a\u7845\u70f7\u4f5c\u4e3a\u5076\u8054\u53c2\u4e0e\u7269\uff0c\u540c\u65f6\uff0c\u80fd\u591f\u5728\u9178\u6027\u5b98\u80fd\u56e2\u7684\u5b58\u5728\u4e0b\uff0c\u5b9e\u73b0\u9009\u62e9\u6027\u7684\u82b3\u57fa\u5316\u53cd\u5e94\u3002\u6b64\u5916\uff0c\u8be5\u5c0f\u7ec4\u901a\u8fc7\u5bf9\u8fd9\u4e00\u65b0\u578b\u7684\u5076\u8054\u7b56\u7565\u5728\u836f\u7269\u7c7b\u4f3c\u7269\u5206\u5b50\u7684\u5408\u6210\u4ee5\u53ca\u591a\u7ec4\u5206\u53cd\u5e94\u4e2d\u7684\u5e94\u7528\uff0c\u8fdb\u4e00\u6b65\u9610\u660e\u8fd9\u4e00\u5168\u65b0\u7684\u5076\u8054\u53cd\u5e94\u65b9\u6cd5\u5b66\u5177\u6709\u826f\u597d\u7684\u5408\u6210\u5e94\u7528\u4ef7\u503c\u3002 Lewis Basic Salt-Promoted Organosilane Coupling Reactions with Aromatic Electrophiles T. W. Reidl, J. S. Bandar, J. Am. Chem. Soc. \u00a02021, 143, 11939. doi: 10.1021\/jacs.1c05764. \u6b63\u6587 1,1-\u4e8c\u82b3\u57fa\u70f7\u70c3\u662f\u4e00\u7c7b\u5177\u6709\u8f83\u9ad8\u5e94\u7528\u4ef7\u503c\u7684\u6709\u673a\u5206\u5b50\uff0c\u901a\u5e38\u91c7\u7528\u5b98\u80fd\u56e2\u5316\u7684\u82c4\u57fa\u8bd5\u5242\u4e0e\u82b3\u9999\u4eb2\u7535\u5e95\u7269\u4e4b\u95f4\u7684\u5076\u8054\u53cd\u5e94\u7b56\u7565\uff0c\u5b8c\u6210\u4e0a\u8ff0\u5206\u5b50\u7684\u5236\u5907\u3002\u5176\u4e2d\uff0c\u8fc7\u6e21\u91d1\u5c5e\u50ac\u5316\u7684\u82b3\u5364\u6216\u82b3\u57fa\u62df\u5364\u4ee3\u7269\u4e0e\u82c4\u57fa\u9541\u3001\u950c\u4ee5\u53ca\u787c\u5316\u5408\u7269\u4e4b\u95f4\u7684\u5076\u8054\u53cd\u5e94\u65b9\u6cd5\u5b66\u5e94\u7528\u6700\u4e3a\u5e7f\u6cdb\u3002\u7136\u800c\uff0c\u4e0a\u8ff0\u7b56\u7565\u4e2d\uff0c\u901a\u5e38\u9700\u8981\u539f\u4f4d\u5236\u5907\u51fa\u5177\u6709\u8f83\u9ad8\u53cd\u5e94\u6d3b\u6027\u7684\u82c4\u57fa\u8bd5\u5242\uff0c\u56e0\u6b64\uff0c\u5b9e\u9a8c\u64cd\u4f5c\u8f83\u4e3a\u7e41\u7410\u3002\u7531\u6b64\uff0c\u6709\u673a\u5408\u6210\u5316\u5b66\u5bb6\u5f00\u59cb\u81f4\u529b\u4e8e\u8bbe\u8ba1\u5168\u65b0\u7684\u5076\u8054\u53cd\u5e94\u7b56\u7565\uff0c\u8fdb\u800c\u5b9e\u73b01,1-\u4e8c\u82b3\u57fa\u70f7\u70c3\u5206\u5b50\u7684\u9ad8\u6548\u6784\u5efa\u3002 \u82c4\u57fa\u53bb\u8d28\u5b50\u5316\u53cd\u5e94\u65b9\u6cd5\u5b66[1]\u4f5c\u4e3a\u4e00\u79cd\u6781\u5177\u5438\u5f15\u529b\u7684\u53cd\u5e94\u7b56\u7565\uff0c\u80fd\u591f\u901a\u8fc7\u78b3\u8d1f\u79bb\u5b50\u4e2d\u95f4\u4f53\u7684\u5f62\u6210\uff0c\u8fdb\u800c\u4e0e\u82b3\u57fa\u4eb2\u7535\u5e95\u7269\u5728\u91d1\u5c5e\u50ac\u5316\u5242\u5b58\u5728\u6216\u65e0\u50ac\u5316\u5242\u5b58\u5728\u7684\u6761\u4ef6\u4e0b\uff0c\u5b8c\u6210\u76f8\u5e94\u7684\u5076\u8054\u53cd\u5e94\u8fc7\u7a0b (Figure 1, left)\u3002\u7136\u800c\uff0c\u8fd9\u4e00\u7b56\u7565\u4e2d\uff0c\u5374\u4f34\u968f\u591a\u82b3\u57fa\u5316\u526f\u4ea7\u7269\u7684\u4ea7\u751f\uff0c\u5e76\u4e14\uff0c\u9700\u8981\u9009\u62e9\u5177\u6709\u4e00\u5b9a\u9178\u6027\u7684\u524d\u4eb2\u6838\u5e95\u7269\uff0c\u4f8b\u5982\u4e8c\u82b3\u57fa\u7532\u70f7\u3002\u540c\u65f6\uff0c\u4e0a\u8ff0\u53bb\u8d28\u5b50\u6d3b\u5316\u8fc7\u7a0b\u7684\u5e95\u7269\u5e94\u7528\u8303\u56f4\u540c\u6837\u8f83\u4e3a\u6709\u9650\u3002 \u4e3a\u89e3\u51b3\u4e0a\u8ff0\u95ee\u9898\uff0c\u672c\u8bfe\u9898\u7ec4\u5f00\u59cb\u81f4\u529b\u4e8e\u8bbe\u8ba1\u4e00\u79cd\u91c7\u7528\u78b1\u4fc3\u8fdb\u7684\u5168\u65b0\u7684\u82c4\u4f4d\u82b3\u57fa\u5316\u7b56\u7565\uff0c\u53cd\u5e94\u8fc7\u7a0b\u4e2d\u6d89\u53caLewis\u78b1\u5bf9\u4e8e\u5177\u6709\u4e00\u5b9aLewis\u9178\u6027\u7684\u82c4\u57fa\u5316\u5408\u7269\u7684\u6d3b\u5316\uff0c\u8fdb\u800c\u5b9e\u73b0\u82b3\u57faCsp2-Csp3\u952e\u4e4b\u95f4\u7684\u5076\u8054\u8fc7\u7a0b[2]\u3002\u5176\u4e2d\uff0c\u7531\u4e8e\u82c4\u57fa\u4e09\u7532\u57fa\u7845\u70f7\u5177\u6709\u826f\u597d\u7684\u7a7a\u6c14\u7a33\u5b9a\u6027\u3001\u65e0\u5438\u6e7f\u6027\u4ee5\u53ca\u5ec9\u4ef7\u6613\u5f97\u7b49\u4f18\u52bf\uff0c\u7531\u6b64\u6210\u4e3a\u8f83\u4e3a\u7406\u60f3\u7684\u5076\u8054\u5e95\u7269\u3002\u4ee5\u6b64\u540c\u65f6\uff0c\u6d89\u53ca\u590d\u6742\u82c4\u57fa\u4e09\u7532\u57fa\u7845\u70f7\u5408\u6210[3]\u7684\u76f8\u5173\u53cd\u5e94\u7b56\u7565\u5df2\u6709\u6587\u732e\u62a5\u9053\u3002\u800c\u4e14\uff0c\u8fc4\u4eca\u4e3a\u6b62\uff0c\u7531\u4e8e\u82c4\u57fa\u4e09\u7532\u57fa\u7845\u70f7\u5206\u5b50\u6240\u5177\u6709\u7684\u9ad8\u5ea6\u7a33\u5b9a\u6027\uff0c\u81f4\u4f7f\u5176\u5728\u91d1\u5c5e\u50ac\u5316\u7684\u4ea4\u53c9\u5076\u8054\u53cd\u5e94\u8fc7\u7a0b\u4e2d\uff0c\u65e0\u6cd5\u8868\u73b0\u51fa\u826f\u597d\u7684\u53cd\u5e94\u6d3b\u6027\uff0c\u8fdb\u800c\u4f7f\u5176\u5728\u82b3\u57fa\u5316\u53cd\u5e94\u65b9\u6cd5\u5b66\u4e2d\u7684\u5e94\u7528\u53d7\u5230\u8f83\u5927\u9650\u5236[4]\u3002\u4e3a\u8fdb\u4e00\u6b65\u89e3\u51b3\u4e0a\u8ff0\u53cd\u5e94\u8fc7\u7a0b\u4e2d\u5b58\u5728\u7684\u5c40\u9650\uff0c\u540c\u6837\u6709\u6587\u732e\u62a5\u9053\u91c7\u7528\u94af\u50ac\u5316\u4ee5\u53ca\u91d1\u5c5e\u5149\u6c27\u5316\u8fd8\u539f\u50ac\u5316[5]\u7684\u76f8\u5173\u5076\u8054\u53cd\u5e94\u7b56\u7565 (Figure 1, right)\u3002 \u8fd9\u91cc\uff0cJ. S. Bandar\u8bfe\u9898\u7ec4\u62a5\u9053\u4e00\u79cd\u5168\u65b0\u7684\uff0c\u901a\u8fc7Lewis\u78b1\u6027\u76d0\u8bd5\u5242\u4fc3\u8fdb\u7684\u82c4\u57fa\u4e09\u7532\u57fa\u7845\u70f7\u4e0e\u5404\u7c7b\u82b3\u9999\u4eb2\u7535\u5e95\u7269\u4e4b\u95f4\u7684\u76f4\u63a5\u5076\u8054\u53cd\u5e94\u65b9\u6cd5\u5b66\uff0c\u8fdb\u800c\u83b7\u5f97\u4e00\u7cfb\u5217\u76f8\u5e94\u76841,1-\u4e8c\u82b3\u57fa\u70f7\u70c3\u884d\u751f\u7269 (Figure 1, bottom)\u3002\u503c\u5f97\u6ce8\u610f\u7684\u662f\uff0c\u5728\u8fd9\u4e00\u5168\u65b0\u7684\u5076\u8054\u7b56\u7565\u4e2d\uff0c\u82c4\u4f4d\u7684\u82b3\u57fa\u5316\u80fd\u591f\u4e0e\u6f5c\u5728\u7684\u8d1f\u79bb\u5b50\u526f\u53cd\u5e94\u8fdb\u884c\u6709\u6548\u7684\u7ade\u4e89\uff0c\u8fdb\u800c\u4f7f\u8fd9\u4e00\u65b0\u578b\u7684\u5076\u8054\u53cd\u5e94\u8fc7\u7a0b\uff0c\u80fd\u591f\u4e0e\u5e95\u7269\u4e2d\u5b58\u5728\u7684\u9178\u6027\u4e0e\u4eb2\u7535\u5b98\u80fd\u56e2\u826f\u597d\u5730\u8fdb\u884c\u517c\u5bb9\u3002\u5e76\u4e14\uff0c\u540c\u6837\u80fd\u591f\u826f\u597d\u5730\u5e94\u7528\u4e8e\u5176\u5b83\u7845\u70f7\u5e95\u7269\u4ee5\u53ca\u5176\u5b83\u76f8\u5173\u7684\u53cd\u5e94\u5e8f\u5217\uff0c\u4f8b\u5982\u91c7\u7528\u70ef\u4e19\u57fa\u7845\u70f7\u53c2\u4e0e\u7684\u4e32\u8054\u82b3\u57fa\u5316\/\u5f02\u6784\u5316\u53cd\u5e94\u65b9\u6cd5\u5b66\uff0c\u80fd\u591f\u8f83\u597d\u5730\u5b8c\u6210\u5404\u7c7b\u82b3\u57fa\u70ef\u5206\u5b50\u7684\u6784\u5efa\u3002\u56e0\u6b64\uff0c\u91c7\u7528Lewis\u78b1\u4fc3\u8fdb\u7684\u82b3\u57fa\u5316\u53cd\u5e94\u65b9\u6cd5\u5b66\uff0c\u5177\u6709\u826f\u597d\u7684\u5408\u6210\u5b9e\u7528\u6027\u4ee5\u53ca\u8f83\u4e3a\u5e7f\u6cdb\u7684\u5e95\u7269\u9002\u7528\u8303\u56f4\u3002 \u540c\u65f6\uff0c\u57282019\u5e74\uff0cJ.\u00a0S. Bandar\u56e2\u961f\u62a5\u9053\u4e00\u79cd\u901a\u8fc7\u6c1f\u79bb\u5b50\u6d3b\u5316\u7684\u70ef\u4e19\u57fa\u4e09\u7532\u57fa\u7845\u70f7\u4e0e\u4e09\u6c1f\u7532\u57fa\u82b3\u70c3\u4e4b\u95f4\u7684\u5355\u9009\u62e9\u6027\u53bb\u6c1f\u70ef\u4e19\u57fa\u5316\u53cd\u5e94\u65b9\u6cd5\u5b66 (monoselective defluoroallylation)[6]\u3002\u5176\u4e2d\uff0c\u53cd\u5e94\u8fc7\u7a0b\u6d89\u53ca\u8d1f\u79bb\u5b50\u70ef\u4e19\u57fa\u4e2d\u95f4\u4f53\u7684\u5f62\u6210\uff0c\u5e76\u8fdb\u4e00\u6b65\u4e0e\u4e09\u6c1f\u7532\u57fa\u82b3\u70c3\u7ecf\u5386\u5355\u7535\u5b50\u8f6c\u79fb\u8fc7\u7a0b\uff0c\u8fdb\u800c\u4f7fC-F\u952e\u65ad\u88c2\uff0c\u5e76\u901a\u8fc7\u5f62\u6210\u7684\u4e8c\u6c1f\u82c4\u57fa\u81ea\u7531\u57fa\uff0c\u8fdb\u884c\u540e\u7eed\u7684\u70ef\u4e19\u57fa\u5316\u8fc7\u7a0b (Scheme 1a)\u3002\u8fd9\u4e00\u7b56\u7565\u7c7b\u4f3c\u4e8e\u91c7\u7528\u70ef\u4e19\u57fa\u4e09\u7532\u57fa\u7845\u70f7\u8fdb\u884c\u76841,4-\u4e8c\u6c30\u57fa\u82b3\u70c3\u7684\u5149\u8bf1\u5bfc\u7535\u5b50\u8f6c\u79fb (PET)\u70ef\u4e19\u57fa\u5316\u8fc7\u7a0b\uff0c\u5373\u53cd\u5e94\u673a\u7406\u4e2d\uff0cSET\u8fc7\u7a0b\u5148\u4e8eC-C\u952e\u7684\u5f62\u6210\u8fc7\u7a0b\u00a0[7]\u3002\u540c\u65f6\uff0c\u5728PET\u8fc7\u7a0b\u7684\u7814\u7a76\u4e2d\uff0c\u8be5\u5c0f\u7ec4\u540c\u6837\u5bf9\u82c4\u57fa\u4e09\u7532\u57fa\u7845\u70f7\u7684\u5e94\u7528\u8fdb\u884c\u7814\u7a76\u3002\u7136\u800c\uff0c\u4e0a\u8ff0\u7684PET\u70ef\u4e19\u57fa\u5316\u8fc7\u7a0b\u5177\u6709\u8f83\u4f4e\u7a0b\u5ea6\u7684\u533a\u57df\u9009\u62e9\u6027\u4ee5\u53ca\u526f\u4ea7\u7269\u5f62\u6210\u7684\u95ee\u9898\uff0c\u540c\u65f6\uff0c\u53cd\u5e94\u8fc7\u7a0b\u4e2d\u9700\u8981\u8fdb\u4e00\u6b65\u91c7\u7528\u7d2b\u5916\u5149\u8f90\u5c04 (Scheme 1b)\u00a0[8]\u3002\u57fa\u4e8e\u4e0a\u8ff0\u7684\u7814\u7a76\u62a5\u9053\uff0c\u4f5c\u8005\u5047\u8bbe\uff0c\u6709\u673a\u4e09\u7532\u57fa\u7845\u70f7\u901a\u8fc7Lewis\u78b1\u7684\u6d3b\u5316\uff0c\u80fd\u591f\u826f\u597d\u5730\u4fc3\u8fdb\u5176\u4e0e\u5176\u5b83\u82b3\u9999\u4eb2\u7535\u5e95\u7269\u4e4b\u95f4\u7684\u76f4\u63a5\u5076\u8054\u8fc7\u7a0b\u3002 \u4e3a\u8fdb\u4e00\u6b65\u9a8c\u8bc1\u8fd9\u4e00\u5047\u8bbe\uff0c\u4f5c\u8005\u9009\u62e94-\u6c30\u57fa\u5421\u5576 (1)\u4e0e\u82c4\u57fa\u4e09\u7532\u57fa\u7845\u70f7 (2) \u4f5c\u4e3a\u6a21\u578b\u5e95\u7269\uff0c\u5bf9\u76f8\u5e94\u7684Lewis\u78b1\u8fdb\u884c\u7b5b\u9009\u3002\u6700\u7ec8\uff0c\u8be5\u5c0f\u7ec4\u786e\u5b9a\u51fa\u6700\u4f73\u7684\u53cd\u5e94\u6761\u4ef6\u4e3a\uff1a\u91c7\u75281\u00a0eq.\u7684\u6c1f\u5316\u94ef\u4e3a\u78b1\uff0c\u540c\u65f6\u52a0\u51651.1\u00a0eq.18-crown-6\uff0c\u5728DMSO\u4f5c\u4e3a\u53cd\u5e94\u6eb6\u5242\u4ee5\u53ca\u5ba4\u6e29\u7684\u53cd\u5e94\u6761\u4ef6\u4e0b\uff0c\u53cd\u5e94\u65f6\u95f4\u4e3a3 h\uff0c\u8fdb\u800c\u83b7\u5f9795%\u6536\u7387\u7684\u5076\u8054\u4ea7\u72693\u00a0(Scheme 1c)\u3002 \u5728\u4e0a\u8ff0\u7684\u6700\u4f73\u53cd\u5e94\u6761\u4ef6\u4e0b\uff0c\u4f5c\u8005\u9996\u5148\u5bf9\u4e0a\u8ff0\u5076\u8054\u8fc7\u7a0b\u7684\u5e95\u7269\u5e94\u7528\u8303\u56f4\u8fdb\u884c\u8003\u5bdf (Table 1)\u3002\u7814\u7a76\u8868\u660e\uff0c\u7f3a\u7535\u5b50\u7684\u6c30\u57fa\u5421\u5576\u4e0e\u6c30\u57fa\u82ef\u5e95\u7269\u80fd\u591f\u4e0e\u4e00\u7cfb\u5217\u4e00\u7ea7\u3001\u4e8c\u7ea7\u4ee5\u53ca\u4e09\u7ea7\u82c4\u57fa\u7845\u70f7\u5728\u4e0a\u8ff0\u7684\u6807\u51c6\u53cd\u5e94\u6761\u4ef6\u4e0b\uff0c\u8fdb\u884c\u76f8\u5e94\u7684\u5076\u8054\u8fc7\u7a0b\uff0c\u5e76\u83b7\u5f97\u6700\u7ec8\u7684\u76ee\u6807\u4ea7\u72694&#8211;24\uff0c\u6536\u7387\u4e3a50-94%\u3002\u540c\u65f6\uff0c\u53cd\u5e94\u8fc7\u7a0b\u4e2d\u8868\u73b0\u51fa\u4f18\u826f\u7684\u5b98\u80fd\u56e2\u517c\u5bb9\u6027\u3002\u4e4b\u540e\uff0c\u8be5\u5c0f\u7ec4\u89c2\u5bdf\u5230\uff0c\u5177\u6709\u03b1-\u6742\u539f\u5b50\u7684\u82c4\u57fa\u7845\u70f7\u5e95\u7269 (25&#8211;27)\u4ee5\u53ca\u836f\u7269\u5206\u5b50paroxetine\u00a0(28)\u4e0ebepotastine\u00a0(29)\uff0c\u5747\u80fd\u591f\u4e0e\u4e0a\u8ff0\u7684\u6807\u51c6\u53cd\u5e94\u6761\u4ef6\u826f\u597d\u5730\u8fdb\u884c\u517c\u5bb9\u3002 \u4e4b\u540e\uff0c\u4f5c\u8005\u5bf9\u5404\u7c7b\u82b3\u57fa\u4eb2\u7535\u5e95\u7269\u7684\u5e94\u7528\u8303\u56f4\u8fdb\u884c\u8003\u5bdf (Scheme 2)\u3002\u7814\u7a76\u8868\u660e\uff0c2-\u6c2f-1,3-\u5511\u7c7b\u4e3a\u4e0a\u8ff0\u5076\u8054\u8fc7\u7a0b\u7684\u6709\u6548\u5e95\u7269 (30&#8211;32)\u3002\u5e76\u4e14\uff0c\u5177\u6709\u6269\u5f20\u03c0-\u4f53\u7cfb\u7684\u6c2f\u4ee3\u7269\uff0c\u4f8b\u59821,3-\u4e8c\u6c2f\u5f02\u55b9\u5549 (33)\u30019-\u6c2f\u5416\u5576(34)\u4ee5\u53ca\u6297\u80bf\u7624\u836f\u7269\u5206\u5b50imiquimod\u7684\u6c2f\u55b9\u5549\u884d\u751f\u7269 (35)\u540c\u6837\u80fd\u591f\u4e0e\u4e0a\u8ff0\u7684\u6700\u4f73\u53cd\u5e94\u6761\u4ef6\u826f\u597d\u5730\u517c\u5bb9\u3002\u540c\u65f6\uff0c\u4f5c\u8005\u53d1\u73b0\uff0c\u5c3d\u7ba14-\u5364\u5421\u5576\u5728\u4e0a\u8ff0\u7684\u6807\u51c6\u53cd\u5e94\u6761\u4ef6\u4e0b\uff0c\u65e0\u6cd5\u6709\u6548\u5730\u8fdb\u884c\u76f8\u5e94\u7684\u5076\u8054\u8fc7\u7a0b\uff0c\u7136\u800c\uff0c\u4e0a\u8ff0\u7684\u6807\u51c6\u53cd\u5e94\u4f53\u7cfb\u5bf9\u4e8e4-\u78fa\u9170\u57fa\u5421\u5576 (36)\u5e95\u7269\uff0c\u5219\u80fd\u591f\u83b7\u5f97\u5177\u6709\u826f\u597d\u6536\u7387\u7684\u5076\u8054\u4ea7\u7269 (Scheme 2b)\u3002\u6b64\u5916\uff0c\u4f5c\u8005\u89c2\u5bdf\u5230\uff0c\u5c064-\u6c2f\u5421\u557637\u8f6c\u5316\u4e3a\u78fa\u9170\u5316\u4ea7\u726938\u00a0(Scheme 2c)\u4e4b\u540e\uff0c\u518d\u4e0e\u82c4\u57fa\u7845\u70f7\u8fdb\u884c\u4e0a\u8ff0\u7684\u5076\u8054\u8fc7\u7a0b\uff0c\u6700\u7ec8\u80fd\u591f\u987a\u5229\u83b7\u5f97\u76f8\u5e94\u7684\u4e8c\u82b3\u57fa\u70f7\u70c3\u4ea7\u726939\u3002 &nbsp; \u63a5\u4e0b\u6765\uff0c\u4f5c\u8005\u8fdb\u4e00\u6b65\u5bf9\u6709\u673a\u7845\u5316\u5408\u726940\u4e0e\u5404\u7c7b\u82b3\u57fa\u4e0e\u6742\u82b3\u57fa\u4eb2\u7535\u5e95\u7269\u4e4b\u95f4\u7684\u5076\u8054\u8fc7\u7a0b\u8fdb\u884c\u8fdb\u4e00\u6b65\u7814\u7a76 (Figure 2)\u3002\u8be5\u5c0f\u7ec4\u89c2\u5bdf\u5230\uff0c\u901a\u8fc7\u5316\u5408\u726940\u53c2\u4e0e\u7684\u5076\u8054\u8fc7\u7a0b\uff0c\u6700\u7ec8\u80fd\u591f\u83b7\u5f97\u4e00\u7cfb\u5217\u76f8\u5e94\u7684chlorpheniramine\u7c7b\u4f3c\u7269\uff0c\u4f8b\u598241&#8211;48\uff0c\u6536\u7387\u4e3a45-95%\u3002 \u6b64\u5916\uff0c\u4f5c\u8005\u8fd8\u540c\u6837\u5bf9\u4e0a\u8ff0\u5076\u8054\u8fc7\u7a0b\u7684\u9009\u62e9\u6027\u8fdb\u884c\u6df1\u5165\u7814\u7a76 (Scheme 3)\u3002\u9996\u5148\uff0c\u4f5c\u8005\u53d1\u73b0\uff0c\u82b3\u57fa\u4eb2\u7535\u5e95\u72692\u5728\u4e0a\u8ff0\u7684\u6807\u51c6\u53cd\u5e94\u6761\u4ef6\u4e0b\uff0c\u80fd\u591f\u83b7\u5f9780%\u6536\u7387\u7684\u7532\u82ef\u4ea7\u7269 (Scheme 3a)\u3002\u8fdb\u800c\u8868\u660e\u82c4\u57fa\u7684\u8d28\u5b50\u5316\u8fc7\u7a0b\u4e0e\u82b3\u57fa\u5316\u8fc7\u7a0b\u4e4b\u95f4\u5b58\u5728\u7ade\u4e89\u3002\u7136\u800c\uff0c\u8f83\u4e3a\u6709\u8da3\u7684\u662f\uff0c\u5728\u9178\u6027\u663e\u8457\u9ad8\u4e8e\u7532\u82ef\u7684\u53cd\u5e94\u6eb6\u5242\u4e2d\uff0c4-\u6c30\u57fa\u5421\u5576\u7684\u82c4\u57fa\u5316\u8fc7\u7a0b\u540c\u6837\u80fd\u591f\u8f83\u597d\u5730\u8fdb\u884c (Scheme 3b)\u3002\u6b64\u5916\uff0c\u4f5c\u8005\u5728\u9009\u62e9\u82c4\u57fa\u7845\u70f7\u7684\u4e24\u79cd\u533a\u57df\u5f02\u6784\u4f53 (50\u4e0e52)\u00a0\u53c2\u4e0e\u7684\u5076\u8054\u8fc7\u7a0b\u4e2d\u53d1\u73b0\uff0c\u4e0a\u8ff0\u82c4\u57fa\u7845\u70f7\u7684\u82b3\u57fa\u5316\u8fc7\u7a0b\u80fd\u591f\u533a\u57df\u4e13\u4e00\u6027\u5730\u5728\u5177\u6709TMS\u57fa\u56e2\u7684\u4f4d\u7f6e\u8fdb\u884c (Scheme 3c)\u3002\u8fdb\u800c\u8868\u660e\uff0c\u82b3\u57fa\u5316\u8fc7\u7a0b\u5728\u8d28\u5b50\u8f6c\u79fb\u4e4b\u524d\u8fdb\u884c\u3002\u540c\u65f6\uff0c\u7814\u7a76\u53d1\u73b0\uff0c\u5177\u6709\u4e00\u5b9a\u9178\u6027\u7684\u4e8c\u82b3\u57fa\u70f7\u70c3\u4ea7\u7269\u7684\u53bb\u8d28\u5b50\u5316\u8fc7\u7a0b\u53d7\u5230\u6781\u5927\u7a0b\u5ea6\u7684\u6291\u5236\uff0c\u8fdb\u800c\u80fd\u591f\u8fdb\u4e00\u6b65\u6291\u5236\u591a\u82b3\u57fa\u5316\u526f\u53cd\u5e94\u8fc7\u7a0b\u7684\u8fdb\u884c\u3002\u4e0a\u8ff0\u4e8b\u5b9e\u540c\u6837\u8868\u660e\uff0cLewis\u78b1\u4fc3\u8fdb\u7684\u82b3\u57fa\u5316\u53cd\u5e94\u65b9\u6cd5\u5b66\u5177\u6709\u663e\u8457\u7684\u4f18\u52bf\uff0c\u800c\u5728Br\u00f8nsted\u78b1\u53c2\u4e0e\u7684\u82b3\u57fa\u5316\u8fc7\u7a0b\u4e2d\uff0c\u5219\u65e0\u6cd5\u5f62\u6210\u76f8\u5e94\u7684\u82c4\u57fa\u78b3\u8d1f\u79bb\u5b50\u3002\u540c\u65f6\uff0c\u53ef\u80fd\u51fa\u73b0\u591a\u91cd\u82b3\u57fa\u5316\u7684\u526f\u53cd\u5e94\u3002\u5e76\u4e14\uff0c\u5728\u5177\u6709\u591a\u91cd\u82c4\u57fa\u4f4d\u7f6e\u53d6\u4ee3\u7684\u76f8\u5173\u5e95\u7269\u4e2d\uff0c\u65e0\u6cd5\u83b7\u5f97\u8f83\u4e3a\u4f18\u826f\u7684\u9009\u62e9\u6027 (\u8be6\u89c1Supporting Information)\u3002 \u4e3a\u89e3\u91ca\u4e0a\u8ff0\u82b3\u57fa\u5316\u8fc7\u7a0b\u4e2d\u7684\u9ad8\u5ea6\u9009\u62e9\u6027\uff0c\u4f5c\u8005\u5047\u8bbe\u82c4\u57fa\u8d1f\u79bb\u5b50\u4e2d\u95f4\u4f53\u901a\u8fc7\u6781\u6027\u6216SET\u673a\u7406\uff0c\u8fdb\u884c\u5feb\u901f\u7684\u82b3\u9999\u53d6\u4ee3\u8fc7\u7a0b (Figure 3)\u3002\u5176\u4e2d\uff0cSET\u673a\u7406\u8fc7\u7a0b\u901a\u8fc7\u78b1\u6027\u6761\u4ef6\u4fc3\u8fdb\uff0c\u5e76\u7c7b\u4f3c\u4e8e\u6709\u673a\u7845\u70f7\u4e0e1,4-\u4e8c\u6c30\u57fa\u82b3\u70c3\u4e4b\u95f4PET\u53cd\u5e94\u3002\u5e76\u4e14\uff0c\u6781\u6027\u673a\u7406\u540c\u6837\u5177\u6709\u5408\u7406\u6027\uff0c\u56e0\u4e3a\u6c30\u57fa\u82b3\u70c3\u4e0e\u78fa\u9170\u57fa\u82b3\u70c3\u5206\u5b50\u80fd\u591f\u53c2\u4e0e\u901a\u8fc7\u5178\u578b\u7684\u52a0\u6210-\u6d88\u9664\u8fc7\u7a0b\u8fdb\u884c\u7684\u53d6\u4ee3\u53cd\u5e94\u3002\u800c\u5728\u8d1f\u79bb\u5b50\u8bd5\u5242\u5bf9\u4e8e\u7c7b\u4f3c\u4eb2\u7535\u5e95\u7269\u7684\u52a0\u6210\u8fc7\u7a0b\u4e2d\uff0c\u51c6\u786e\u533a\u5206\u4e0a\u8ff0\u4e24\u79cd\u4e0d\u540c\u7684\u673a\u7406\u8def\u5f84\uff0c\u5219\u5177\u6709\u8f83\u5927\u7684\u6311\u6218\u6027\u3002\u5e76\u4e14\uff0c\u4e0a\u8ff0\u7684\u5076\u8054\u53cd\u5e94\u8fc7\u7a0b\u4e2d\u7684\u76f8\u5173\u5b9e\u9a8c\u7ed3\u8bba\uff0c\u5747\u80fd\u591f\u901a\u8fc7\u6781\u6027\u4e0eSET\u4e24\u79cd\u4e0d\u540c\u7684\u673a\u7406\u8def\u5f84\u8fdb\u884c\u5408\u7406\u7684\u89e3\u91ca\u3002\u540c\u65f6\uff0c\u4f5c\u8005\u53d1\u73b0\u4e0a\u8ff0\u7684\u5076\u8054\u53cd\u5e94\u65b9\u5f0f\u53ef\u80fd\u5177\u6709\u76f8\u5173\u7684\u5e95\u7269\u4f9d\u8d56\u6027\uff0c\u5c3d\u7ba1\u76f8\u5e94\u7684\u82b3\u57fa\u5316\u8fc7\u7a0b\u80fd\u591f\u4e0e\u5176\u5b83\u901a\u8fc7\u6f5c\u5728\u8d1f\u79bb\u5b50\u4e2d\u95f4\u4f53\u5f15\u53d1\u7684\u526f\u53cd\u5e94\u8fc7\u7a0b\u6709\u6548\u5730\u8fdb\u884c\u7ade\u4e89\u3002 \u901a\u8fc7\u4e0a\u8ff0\u7814\u7a76\uff0c\u4f5c\u8005\u8bbe\u60f3\uff0c\u6709\u673a\u7845\u70f7\u7684\u82b3\u57fa\u5316\u8fc7\u7a0b\u540c\u6837\u80fd\u591f\u4e0e\u78b1\u4fc3\u8fdb\u7684\u5176\u5b83\u5408\u6210\u8f6c\u5316\u8fc7\u7a0b\u8fdb\u884c\u6709\u6548\u5730\u7ed3\u5408 (Scheme 4)\u3002\u9996\u5148\uff0c\u4f5c\u8005\u53d1\u73b0\uff0c\u901a\u8fc7\u70ef\u4e19\u57fa\u4e09\u7532\u57fa\u7845\u70f7\u5f62\u6210\u7684\u70ef\u4e19\u57fa\u82b3\u70c3\u4e2d\u95f4\u4f53\uff0c\u80fd\u591f\u8fdb\u4e00\u6b65\u7ecf\u5386\u540e\u7eed\u7684\u7acb\u4f53\u9009\u62e9\u6027\u5f02\u6784\u5316\u8fc7\u7a0b\uff0c\u5e76\u83b7\u5f97\u76f8\u5e94\u7684\u70ef\u4ea7\u726954\u300155\u4e0e56\u00a0(Scheme 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