{"id":40120,"date":"2021-09-22T08:00:22","date_gmt":"2021-09-22T00:00:22","guid":{"rendered":"\/\/www.gsbet888.com\/?p=40120"},"modified":"2021-10-06T12:28:47","modified_gmt":"2021-10-06T04:28:47","slug":"org-lett-%ef%bc%9a%e9%80%9a%e8%bf%87%e8%8b%af%e7%94%b2%e9%85%b8%e7%9a%84%e4%b8%89%e6%b0%9f%e7%94%b2%e5%9f%ba%e5%8c%96%e7%ad%96%e7%95%a5%e5%ae%9e%e7%8e%b0%e8%8a%b3%e5%9f%ba%e4%b8%89%e6%b0%9f%e7%94%b2","status":"publish","type":"post","link":"\/\/www.gsbet888.com\/%e5%8c%96%e5%ad%a6%e6%9d%82%e8%ae%b0\/recentpaper\/2021\/09\/org-lett-%ef%bc%9a%e9%80%9a%e8%bf%87%e8%8b%af%e7%94%b2%e9%85%b8%e7%9a%84%e4%b8%89%e6%b0%9f%e7%94%b2%e5%9f%ba%e5%8c%96%e7%ad%96%e7%95%a5%e5%ae%9e%e7%8e%b0%e8%8a%b3%e5%9f%ba%e4%b8%89%e6%b0%9f%e7%94%b2.html","title":{"rendered":"Org. Lett.\uff1a\u901a\u8fc7\u82ef\u7532\u9178\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u7b56\u7565\u5b9e\u73b0\u82b3\u57fa\u4e09\u6c1f\u7532\u57fa\u916e\u7684\u5408\u6210"},"content":{"rendered":"

\u672c\u6587\u4f5c\u8005\uff1a\u6749\u6749<\/strong><\/p>\n

\u5bfc\u8bfb<\/h4>\n

\u8fd1\u65e5\uff0c\u6d77\u5357\u5927\u5b66\u7684\u9648\u94c1\u6865\u6559\u6388\u8bfe\u9898\u7ec4\u5728Org. Lett.<\/em>\u4e2d\u53d1\u8868\u8bba\u6587\uff0c\u62a5\u9053\u4e00\u79cd\u9ad8\u6548\u5e76\u901a\u7528\u7684\u82ef\u7532\u9178\u4e0eTMSCF3<\/sub>\u4e4b\u95f4\u7684\u76f4\u63a5\u4e09\u6c1f\u7532\u57fa\u5316\u53cd\u5e94\u65b9\u6cd5\u5b66\u3002\u540c\u65f6\uff0c\u4f5c\u8005\u901a\u8fc7\u5bf9\u5177\u6709\u7fa7\u9178\u7ed3\u6784\u5355\u5143\u7684\u751f\u7269\u6d3b\u6027\u5206\u5b50\u76f4\u63a5\u4fee\u9970\u7684\u7814\u7a76\uff0c\u8fdb\u4e00\u6b65\u9610\u660e\u8fd9\u4e00\u7b56\u7565\u7684\u5408\u6210\u5e94\u7528\u4ef7\u503c\u3002\u6b64\u5916\uff0c\u8fd9\u4e00\u5168\u65b0\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u7b56\u7565\u5177\u6709\u5b9e\u9a8c\u64cd\u4f5c\u7b80\u6d01\u3001\u53cd\u5e94\u6761\u4ef6\u6e29\u548c\u3001\u539f\u6599\u6613\u5f97\u4ee5\u53ca\u5e95\u7269\u5e94\u7528\u8303\u56f4\u5e7f\u6cdb\u7b49\u4f18\u52bf\u3002<\/p>\n

Trifluoromethylation of Benzoic Acids: An Access to Aryl Trifluoromethyl Ketones
\nX. Liu, L. Liu, T. Huang, J. Zhang, Z. Tang, C. Li, T. Chen, Org. Lett. 2021, 23, 4930. doi: 10.1021\/acs.orglett.1c01720<\/u><\/a>.<\/u><\/p><\/blockquote>\n

\"\"<\/a><\/p>\n

\u6b63\u6587<\/h4>\n

\u6c1f\u539f\u5b50\u7684\u5f15\u5165\u662f\u5316\u5b66\u79d1\u5b66\u3001\u6750\u6599\u79d1\u5b66\u4ee5\u53ca\u751f\u7269\u79d1\u5b66\u4e2d\u7528\u4e8e\u589e\u5f3a\u6216\u6539\u53d8\u529f\u80fd\u6027\u6709\u673a\u5206\u5b50\u7269\u7406\u4e0e\u5316\u5b66\u6027\u80fd\u7684\u91cd\u8981\u7b56\u7565\u4e4b\u4e00\u3002\u6839\u636e\u76f8\u5173\u7684\u6587\u732e\u62a5\u9053\uff0c\u7ea620%\u7684\u836f\u7269\u5206\u5b50\u4ee5\u53ca30%\u7684\u519c\u836f\u5206\u5b50\u4e2d\u5b58\u5728\u6c1f\u539f\u5b50\u7684\u53d6\u4ee3\u3002\u540c\u65f6\uff0c\u4e09\u6c1f\u7532\u57fa\u916e\u4f5c\u4e3a\u91cd\u8981\u7684\u6709\u673a\u6c1f\u5316\u5408\u7269\uff0c\u9664\u5177\u6709\u8f83\u597d\u7684\u4eb2\u8102\u6027\u4e0e\u4ee3\u8c22\u7a33\u5b9a\u6027\u4e4b\u5916\uff0c\u540c\u6837\u5177\u6709\u8f83\u5f3a\u7684\u5438\u7535\u5b50\u7279\u6027\uff0c\u5e76\u80fd\u591f\u5f62\u6210\u8f83\u4e3a\u7a33\u5b9a\u7684\u6c34\u5408\u7269\u3002\u800c\u4e14\uff0c\u4e09\u6c1f\u7532\u57fa\u916e\u7c7b\u5316\u5408\u7269\u8868\u73b0\u51fa\u7684\u4e0a\u8ff0\u7279\u6b8a\u6027\u80fd\uff0c\u76ee\u524d\u5df2\u7ecf\u5e7f\u6cdb\u5e94\u7528\u4e8e\u836f\u7269\u5206\u5b50\u7684\u8bbe\u8ba1\u4e0e\u7814\u53d1\u3002\u5e76\u4e14\uff0c\u7531\u4e8e\u5176\u7fb0\u57fa\u5b98\u80fd\u56e2\u8868\u73b0\u51fa\u7684\u591a\u91cd\u53cd\u5e94\u6d3b\u6027\uff0c\u4e09\u6c1f\u7532\u57fa\u916e\u7c7b\u5316\u5408\u7269\u540c\u6837\u80fd\u591f\u4f5c\u4e3a\u6784\u5efa\u5176\u5b83\u542b\u6c1f\u529f\u80fd\u6709\u673a\u5206\u5b50\u7684\u91cd\u8981\u780c\u5757\u3002\u901a\u5e38\uff0c\u901a\u8fc7\u82b3\u57fa\u91d1\u5c5e\u8bd5\u5242 (Li\u6216Mg)\u4e0e\u4e09\u6c1f\u4e59\u9170\u57fa\u884d\u751f\u7269\u4e4b\u95f4\u7684\u4eb2\u6838\u53d6\u4ee3\u53cd\u5e94\u7b56\u7565\uff0c\u80fd\u591f\u8f83\u597d\u5730\u5b8c\u6210\u4e00\u7cfb\u5217\u4e09\u6c1f\u7532\u57fa\u916e\u5206\u5b50\u7684\u5408\u6210[<\/sup>1<\/sup>]<\/sup>\u3002\u7136\u800c\uff0c\u7531\u4e8e\u5176\u8f83\u4e3a\u82db\u523b\u7684\u53cd\u5e94\u6761\u4ef6\uff0c\u8fdb\u800c\u4f7f\u4e0a\u8ff0\u7b56\u7565\u7684\u8fdb\u4e00\u6b65\u5e94\u7528\u53d7\u5230\u9650\u5236\u3002\u540c\u65f6\uff0c\u7814\u7a76\u8868\u660e\uff0c\u91c7\u7528\u5bcc\u7535\u5b50\u82b3\u57fa\u5e95\u7269\u53c2\u4e0e\u7684Friedel-Crafts\u9170\u5316\u53cd\u5e94\u65b9\u6cd5\u5b66[<\/sup>2<\/sup>]<\/sup>\uff0c\u5219\u5b58\u5728\u5e95\u7269\u5e94\u7528\u8303\u56f4\u8f83\u4e3a\u6709\u9650\u4ee5\u53ca\u7f3a\u4e4f\u826f\u597d\u7684\u533a\u57df\u9009\u62e9\u6027\u63a7\u5236\u7b49\u95ee\u9898\u3002\u56e0\u6b64\uff0c\u6709\u673a\u5408\u6210\u5316\u5b66\u5bb6\u81f4\u529b\u4e8e\u53d1\u5c55\u4e00\u7cfb\u5217\u66f4\u4e3a\u6709\u6548\u7684\u53cd\u5e94\u7b56\u7565\uff0c\u5b9e\u73b0\u4e09\u6c1f\u7532\u57fa\u916e\u5206\u5b50\u7684\u9ad8\u6548\u5236\u5907 (Scheme 1)\u00a0[<\/sup>3<\/sup>]<\/sup>\u3002\u76ee\u524d\uff0c\u5df2\u7ecf\u6210\u529f\u5f00\u53d1\u51fa\u91c7\u7528\u8fc7\u6e21\u91d1\u5c5e\u50ac\u5316\u7684\u82b3\u5364\u6216\u82b3\u9999\u62df\u5364\u4ee3\u7269\u53c2\u4e0e\u7684\u4e09\u6c1f\u4e59\u9170\u5316\u53cd\u5e94\u65b9\u6cd5\u5b66\uff0c\u5e76\u8fdb\u4e00\u6b65\u5e94\u7528\u4e8e\u4e09\u6c1f\u7532\u57fa\u916e\u7c7b\u5316\u5408\u7269\u7684\u5236\u5907[<\/sup>4<\/sup>]<\/sup>\u3002\u540c\u65f6\uff0c\u901a\u8fc7\u03b1<\/em>-\u4e09\u6c1f\u7532\u9187\u7684\u6c27\u5316\u53cd\u5e94\u65b9\u6cd5\u5b66\uff0c\u540c\u6837\u80fd\u591f\u5b9e\u73b0\u76f8\u5e94\u4e09\u6c1f\u7532\u57fa\u916e\u7c7b\u5316\u5408\u7269\u7684\u5408\u6210[<\/sup>5<\/sup>]<\/sup>\uff0c\u7136\u800c\uff0c\u5728\u8fd9\u4e00\u7b56\u7565\u4e2d\uff0c\u9700\u8981\u9009\u62e9\u8f83\u4e0d\u7a33\u5b9a\u7684\u919b\u4f5c\u4e3a\u8d77\u59cb\u539f\u6599\uff0c\u8fdb\u884c\u76f8\u5e94\u9187\u5e95\u7269\u7684\u9884\u5148\u5408\u6210\u3002\u5e76\u4e14\uff0c\u53cd\u5e94\u8fc7\u7a0b\u4e2d\u901a\u5e38\u9700\u8981\u9009\u62e9\u8d85\u5316\u5b66\u8ba1\u91cf (overstoichiometric)\u7684\u7279\u6b8a\u6c27\u5316\u5242\u3002\u4e3a\u6709\u6548\u89e3\u51b3\u4e0a\u8ff0\u7b56\u7565\u4e2d\u5b58\u5728\u7684\u8bf8\u591a\u5c40\u9650\uff0c\u8fd9\u91cc\uff0c\u672c\u6587\u5c06\u62a5\u9053\u4e00\u79cd\u82ef\u7532\u9178\u4e0eTMSCF3<\/sub>\u4e4b\u95f4\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u53cd\u5e94\u65b9\u6cd5\u5b66\uff0c\u8fdb\u800c\u4ee5\u826f\u597d\u81f3\u4f18\u826f\u7684\u53cd\u5e94\u6536\u7387\uff0c\u83b7\u5f97\u4e00\u7cfb\u5217\u76f8\u5e94\u7684\u82b3\u57fa\u4e09\u6c1f\u7532\u57fa\u916e\u7c7b\u5206\u5b50 (Scheme 1)\u3002\u5e76\u4e14\uff0c\u8fd9\u4e00\u5168\u65b0\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u7b56\u7565\u5177\u6709\u5b9e\u9a8c\u64cd\u4f5c\u7b80\u6d01\u3001\u53cd\u5e94\u6761\u4ef6\u6e29\u548c\u3001\u539f\u6599\u6613\u5f97\u4ee5\u53ca\u5e95\u7269\u5e94\u7528\u8303\u56f4\u5e7f\u6cdb\u7b49\u4f18\u52bf\u3002<\/p>\n

\"\"<\/a><\/p>\n

\u9996\u5148\uff0c\u4f5c\u8005\u91c7\u75284-\u82ef\u57fa\u82ef\u7532\u91781a<\/strong>\u4e0eTMSCF3<\/sub>\u4f5c\u4e3a\u6a21\u578b\u5e95\u7269\uff0c\u8fdb\u884c\u76f8\u5173\u53cd\u5e94\u6761\u4ef6\u7684\u4f18\u5316\u7b5b\u9009 (Table 1)\u3002\u8fdb\u800c\u786e\u5b9a\u6700\u4f73\u7684\u53cd\u5e94\u6761\u4ef6\u4e3a\uff1a\u91c7\u7528DMAP\u4f5c\u4e3a\u78b1\uff0c\u82ef\u7532\u919a\u4f5c\u4e3a\u53cd\u5e94\u6eb6\u5242\uff0c\u540c\u65f6\u52a0\u5165TFAA\u4e0eCsF\uff0c\u5728\u53cd\u5e94\u6e29\u5ea6\u4e3a120\u2103\u7684\u6761\u4ef6\u4e0b\u8fdb\u884c\u53cd\u5e94\uff0c\u6700\u7ec8\u83b7\u5f9790%\u6536\u7387\u7684\u76ee\u6807\u4ea7\u72693a<\/strong>\u3002<\/p>\n

\"\"<\/a><\/p>\n

 <\/p>\n

\"\"<\/a><\/p>\n

\u5728\u83b7\u5f97\u4e0a\u8ff0\u7684\u6700\u4f73\u53cd\u5e94\u6761\u4ef6\u4e4b\u540e\uff0c\u4f5c\u8005\u5f00\u59cb\u5bf9\u7fa7\u9178\u5e95\u7269\u7684\u5e94\u7528\u8303\u56f4\u8fdb\u884c\u8003\u5bdf (Table 2)\u3002\u7814\u7a76\u8868\u660e\uff0c\u82ef\u73af\u4e2d\u5177\u6709\u4e0d\u540c\u5438\u7535\u5b50\u4e0e\u4f9b\u7535\u5b50\u57fa\u56e2\u53d6\u4ee3\u7684\u82ef\u7532\u9178\u5e95\u7269\uff0c\u5747\u80fd\u591f\u987a\u5229\u5730\u53c2\u4e0e\u4e0a\u8ff0\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u8fc7\u7a0b\uff0c\u5e76\u83b7\u5f97\u76f8\u5e94\u7684\u76ee\u6807\u4ea7\u72693a<\/strong>–3q<\/strong>\u3002\u540c\u65f6\uff0c\u4f5c\u8005\u53d1\u73b0\uff0c\u4e0a\u8ff0\u5bf9\u6807\u51c6\u53cd\u5e94\u6761\u4ef6\u5bf9\u4e8e\u8418\u7532\u9178\u4e0e\u591a\u73af\u82b3\u9999\u7fa7\u9178\u4ee5\u53ca\u6742\u73af\u82b3\u9999\u7fa7\u9178\u5e95\u7269\uff0c\u540c\u6837\u80fd\u591f\u6709\u6548\u5730\u517c\u5bb9\uff0c\u5e76\u83b7\u5f97\u76f8\u5e94\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u4ea7\u72693r<\/strong>–3z<\/strong>\u3002\u6b64\u5916\uff0c\u4f5c\u8005\u8fdb\u4e00\u6b65\u53d1\u73b0\uff0c\u4e0a\u8ff0\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u7b56\u7565\u540c\u6837\u80fd\u591f\u5e94\u7528\u4e8e\u5404\u7c7b\u8102\u80aa\u65cf\u7fa7\u9178\u5e95\u7269\uff0c\u5e76\u83b7\u5f97\u76f8\u5e94\u7684\u4e09\u6c1f\u7532\u57fa\u916e\u4ea7\u72693aa<\/strong>\u4e0e3ab<\/strong>\uff0c\u7136\u800c\uff0c\u5374\u8868\u73b0\u51fa\u53cd\u5e94\u6536\u7387\u7684\u663e\u8457\u964d\u4f4e\uff0c\u53ef\u80fd\u6e90\u81ea\u4e8e\u7fb0\u57fa\u78b3\u7684\u7535\u5b50\u5bc6\u5ea6\u76f8\u5bf9\u8f83\u9ad8\uff0c\u56e0\u800c\uff0c\u4e0d\u5229\u4e8e\u540e\u7eed\u4eb2\u6838\u52a0\u6210\u6b65\u9aa4\u7684\u8fdb\u884c\u3002<\/p>\n

\"\"<\/a><\/p>\n

\u4e3a\u8fdb\u4e00\u6b65\u9610\u660e\u8fd9\u4e00\u7b56\u7565\u7684\u5408\u6210\u5b9e\u7528\u6027\uff0c\u4f5c\u8005\u53d1\u73b0\uff0c\u91c7\u7528\u4e0a\u8ff0\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u6761\u4ef6\uff0c\u80fd\u591f\u6210\u529f\u5730\u5bf9\u4e00\u7cfb\u5217\u5177\u6709\u751f\u7269\u6d3b\u6027\u7684\u7fa7\u9178\u5206\u5b50\u8fdb\u884c\u76f4\u63a5\u4fee\u9970\uff0c\u5e76\u83b7\u5f97\u76f8\u5e94\u7684\u4e09\u6c1f\u7532\u57fa\u916e\u4ea7\u7269 (Scheme 2)\u3002\u4f8b\u5982\uff0c\u7528\u4e8e\u76ae\u80a4\u75c5\u6cbb\u7597\u7684\u4e34\u5e8a\u836f\u7269adapalin\uff0c\u5728\u4e0a\u8ff0\u7684\u6807\u51c6\u53cd\u5e94\u6761\u4ef6\u4e0b\uff0c\u80fd\u591f\u8f83\u4e3a\u5bb9\u6613\u5730\u8fdb\u884c\u76f8\u5e94\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u8fc7\u7a0b\uff0c\u5e76\u4ee580%\u7684\u6536\u7387\u83b7\u5f97\u76f8\u5e94\u76ee\u6807\u4ea7\u72693ac<\/strong>\u3002\u800c\u4f5c\u4e3a\u6297\u75db\u98ce\u836f\u7269 (antigout drug)\u4ee5\u53ca\u6297\u751f\u7d20\u4f50\u5242 (antibiotic adjuvant)\u7684probenecid\u5206\u5b50\uff0c\u5728\u8fd9\u4e00\u5168\u65b0\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u53cd\u5e94\u6761\u4ef6\u4e0b\uff0c\u80fd\u591f\u4ee590%\u7684\u6536\u7387\u83b7\u5f97\u76f8\u5e94\u7684\u4e09\u6c1f\u7532\u57fa\u916e\u4ea7\u72693ad<\/strong>\u3002\u4e4b\u540e\uff0c\u4f5c\u8005\u53d1\u73b0\uff0c\u5c06\u7528\u4e8e\u51a0\u5fc3\u75c5\u4e34\u5e8a\u6cbb\u7597\u7684\u836f\u7269\u5206\u5b503-\u7532\u57fa\u9ec4\u916e-8-\u7fa7\u9178\u5e94\u7528\u4e8e\u4e0a\u8ff0\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u53cd\u5e94\u65f6\uff0c\u80fd\u591f\u4ee580%\u7684\u6536\u7387\uff0c\u83b7\u5f97\u76f8\u5e94\u7684\u76ee\u6807\u4ea7\u72693ae<\/strong>\u3002\u540c\u65f6\uff0c\u4f5c\u8005\u8fdb\u4e00\u6b65\u53d1\u73b0\uff0c\u6297\u9ad8\u8840\u538b\u836f\u7269telmisartan\u5728\u4e0a\u8ff0\u7684\u6807\u51c6\u53cd\u5e94\u6761\u4ef6\u4e0b\uff0c\u540c\u6837\u80fd\u591f\u4ee554%\u7684\u53cd\u5e94\u6536\u7387\uff0c\u83b7\u5f97\u76f8\u5e94\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u4ea7\u72693af<\/strong>\u3002<\/p>\n

\"\"<\/a><\/p>\n

\u63a5\u4e0b\u6765\uff0c\u4f5c\u8005\u8fdb\u884c\u4e00\u7cfb\u5217\u514b\u7ea7\u89c4\u6a21\u5b9e\u9a8c\u7684\u7814\u7a76 (Scheme 3)\u3002\u8be5\u5c0f\u7ec4\u53d1\u73b0\uff0c\u91c7\u7528probenecid\u00a01ad<\/strong>\u4f5c\u4e3a\u6a21\u578b\u5e95\u7269\uff0c\u5728\u4e0a\u8ff0\u7684\u6807\u51c6\u53cd\u5e94\u6761\u4ef6\u4e0b\uff0c\u5206\u522b\u8fdb\u884c1mmol\u30012mmol\u4ee5\u53ca5 mmol\u89c4\u6a21\u7684\u53cd\u5e94\u5b9e\u9a8c\u3002\u7814\u7a76\u53d1\u73b0\uff0c\u901a\u8fc7\u4e00\u7cfb\u5217\u76f8\u5173\u7684\u5b9e\u9a8c\u540e\u5904\u7406\u64cd\u4f5c\u4e4b\u540e\uff0c\u9009\u62e9\u7845\u80f6\u67f1\u8272\u8c31\u8fdb\u884c\u5206\u79bb\uff0c\u5747\u80fd\u591f\u83b7\u5f97\u8f83\u9ad8\u6536\u7387\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u4ea7\u72693ad<\/strong>\uff0c\u8fdb\u800c\u8868\u660e\uff0c\u8fd9\u4e00\u5168\u65b0\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u53cd\u5e94\u65b9\u6cd5\u5b66\u5177\u6709\u826f\u597d\u7684\u5408\u6210\u5e94\u7528\u4ef7\u503c\u3002<\/p>\n

\"\"<\/a><\/p>\n

\u6700\u540e\uff0c\u6839\u636e\u524d\u671f\u7684\u6587\u732e\u62a5\u9053[6]-[9]<\/sup>\uff0c\u4f5c\u8005\u63d0\u51fa\u4e00\u79cd\u5408\u7406\u7684\u53cd\u5e94\u673a\u7406 (Scheme 4)\u3002\u9996\u5148\uff0c\u7fa7\u91781<\/strong>\u901a\u8fc7TFAA\u7684\u539f\u4f4d\u6d3b\u5316\uff0c\u5f62\u6210\u6df7\u5408\u9178\u9150A<\/strong>\u3002\u4e4b\u540e\uff0c\u5728CsF\u4e0e\u00a0DMAP\u7684\u8f85\u52a9\u4e0b\uff0c\u6df7\u5408\u9178\u9150A<\/strong>\u00a0\u4e0eTMSCF3<\/sub>\u7ecf\u5386\u4eb2\u6838\u52a0\u6210-\u6d88\u9664\u8fc7\u7a0b\uff0c\u5f62\u6210\u76f8\u5e94\u7684\u4e09\u6c1f\u7532\u57fa\u916e\u4ea7\u72693<\/b><\/strong>\u3002<\/p>\n

\"\"<\/a><\/p>\n

\u603b\u7ed3<\/h4>\n

\u6d77\u5357\u5927\u5b66\u9648\u94c1\u6865\u6559\u6388\u8bfe\u9898\u7ec4\u62a5\u9053\u4e00\u79cd\u73af\u5883\u53cb\u597d\u7684\uff0c\u5e76\u901a\u8fc7\u5ec9\u4ef7\u6613\u5f97\u7684\u7fa7\u9178\u4f5c\u4e3a\u8d77\u59cb\u539f\u6599\u8fdb\u884c\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u53cd\u5e94\u65b9\u6cd5\u5b66\uff0c\u5e76\u6210\u529f\u5b8c\u6210\u4e00\u7cfb\u5217\u4e09\u6c1f\u7532\u57fa\u916e\u5206\u5b50\u7684\u6784\u5efa\u3002\u8fd9\u4e00\u5168\u65b0\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u7b56\u7565\u5177\u6709\u5b9e\u9a8c\u64cd\u4f5c\u7b80\u6d01\u3001\u53cd\u5e94\u6761\u4ef6\u6e29\u548c\u3001\u539f\u6599\u6613\u5f97\u3001\u5e95\u7269\u5e94\u7528\u8303\u56f4\u5e7f\u6cdb\u4ee5\u53ca\u4f18\u826f\u7684\u5b98\u80fd\u56e2\u517c\u5bb9\u6027\u7b49\u4f18\u52bf\u3002\u6b64\u5916\uff0c\u8be5\u5c0f\u7ec4\u901a\u8fc7\u5bf9\u4e00\u7cfb\u5217\u5177\u6709\u826f\u597d\u751f\u7269\u6d3b\u6027\u7684\u7fa7\u9178\u5206\u5b50\u7684\u76f4\u63a5\u4fee\u9970\u4ee5\u53ca\u540e\u7eed\u514b\u7ea7\u89c4\u6a21\u5b9e\u9a8c\u7684\u7814\u7a76\uff0c\u8fdb\u4e00\u6b65\u9610\u660e\u8fd9\u4e00\u5168\u65b0\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u7b56\u7565\u5177\u6709\u826f\u597d\u7684\u5408\u6210\u5e94\u7528\u524d\u666f\u3002<\/p>\n

\u53c2\u8003\u6587\u732e<\/b><\/strong><\/h4>\n[1]\u00a0(a) R. J. Andrew, J. M. Mellor, Tetrahedron<\/i><\/em>\u00a02000<\/b><\/strong>, 56<\/i><\/em>,\u00a07261. doi:\u00a010.1016\/S0040-4020(00)00597-4<\/u><\/a>.<\/u><\/p>\n

(b) L. Zhu, Z. Miao, C. Sheng, J. Yao, C. Zhuang, W. Zhang, J. Fluorine Chem. <\/i><\/em>2010<\/b><\/strong>, 131<\/i><\/em>, 800. doi:\u00a010.1016\/j.jfluchem.2010.04.002<\/u><\/a>.<\/u><\/p>\n

(c) B. Heinz, D. Djukanovic, M. A. Ganiek, B. Martin, B. Schenkel, P. Knochel, Org. Lett.<\/i><\/em>\u00a02020<\/b><\/strong>, 22<\/i><\/em>, 493.\u00a0doi:\u00a010.1021\/acs.orglett.9b04254<\/u><\/a>.<\/u><\/p>\n[2]\u00a0(a) A. Andicsov\u00e1-Eckstein, E. Kozma, Z. Puterov\u00e1-Tok\u00e1rov\u00e1, D. V\u00e9gh, J. Fluorine Chem. <\/i><\/em>2015<\/b><\/strong>, 180<\/i><\/em>, 272.\u00a0doi:\u00a010.1016\/j.jfluchem.2015.10.011<\/u><\/a>.<\/u><\/p>\n

(b) R. A. Wolf, Org. Process Res. Dev.<\/i><\/em>\u00a02008<\/b><\/strong>,\u00a012<\/i><\/em>, 23.\u00a0doi:\u00a010.1021\/op700199p<\/u><\/a>.<\/u><\/p>\n

(c) S. Yao, Z. Ren, Y. Wang, Z. Guan, J. Org. Chem.<\/i><\/em>\u00a02016<\/b><\/strong>, 81<\/i><\/em>, 4226.\u00a0doi:\u00a010.1021\/acs.joc.6b00580<\/u><\/a>.<\/u><\/p>\n

(d) W. Wang, W. Xiong, J. Wang, Q. Wang, W.\u00a0<\/i><\/em>Yang, J. Org.<\/i><\/em>\u00a0<\/i><\/em>Chem.<\/i><\/em>\u00a02020<\/b><\/strong>, 85<\/i><\/em>, 4398. doi:\u00a010.1021\/acs.joc.0c00116<\/u><\/a>.<\/u><\/p>\n

(e) Y. Hua, J. Chen, H. Yang,\u00a0M. Wang, J. Org. Chem. <\/i><\/em>2018<\/b><\/strong>, 83<\/i><\/em>, 1160. doi:\u00a010.1021\/acs.joc.7b02599<\/u><\/a>.<\/u><\/p>\n

(f) F. Rahmani, A. Darehkordi, Synthesis<\/i><\/em>\u00a02018<\/b><\/strong>, 50<\/i><\/em>, 2124. doi:\u00a010.1055\/s-0037-1609433<\/u>.<\/u><\/a><\/p>\n[3]\u00a0(a) C. B. Kelly, M. A. Mercadante, N. E.\u00a0<\/i><\/em>Leadbeater,\u00a0<\/i><\/em>Chem. Commun.<\/i><\/em>\u00a02013<\/b><\/strong>,\u00a049<\/i><\/em>, 11133. doi:\u00a010.1039\/C3CC46266H<\/u><\/a>.<\/u><\/p>\n

(b) W. Wu, Z.\u00a0<\/i><\/em>Weng, Synthesis <\/i><\/em>2018<\/b><\/strong>, 50<\/i><\/em>, 1958. doi:\u00a010.1055\/s-0036-1591971<\/u>.<\/u><\/a><\/p>\n

(c) K. Funabiki, A. Hayakawa, T. Inuzuka, Org. Biomol. Chem.<\/i><\/em>\u00a02018<\/b><\/strong>, 16<\/i><\/em>, 913. doi:\u00a010.1039\/C7OB02862H<\/u><\/a>.<\/u><\/p>\n

(d) H. Cheng,\u00a0Y. Pei, F. Leng, J. Li, A. Liang, D. Zou, Y. Wu, Y.\u00a0Wu, Tetrahedron Lett. <\/i><\/em>2013<\/b><\/strong>, 54<\/i><\/em>, 4483. doi:\u00a010.1016\/j.tetlet.2013.06.045<\/u><\/a>.<\/u><\/p>\n[4]\u00a0(a) M. B. Johansen, O. R. Gedde, T. S. Mayer, T.\u00a0Skrydstrup, Org. Lett.<\/i><\/em>\u00a0<\/i><\/b><\/em><\/strong>2020<\/b><\/strong>,\u00a022<\/i><\/em>, 4068. doi:\u00a010.1021\/acs.orglett.0c01117<\/u><\/a>.<\/u><\/p>\n

(b) K. Funabiki, A. Hayakawa, T.\u00a0Inuzuka, Org. Biomol. Chem. <\/i><\/em>2018<\/b><\/strong>, 16<\/i><\/em>, 913.\u00a0doi:\u00a010.1039\/C7OB02862H<\/u><\/a>.<\/u><\/p>\n

(c) F. Zhu, G. Yang, S. Zhou, X.\u00a0Wu, RSC Adv.<\/i><\/em>\u00a02016<\/b><\/strong>, 6<\/i><\/em>, 57070.\u00a0doi:\u00a010.1039\/C6RA12287F<\/u><\/a>.<\/u><\/p>\n

(d) K. Domino, M. B. Johansen, K. Daasbjerg, T.\u00a0Skrydstrup, Organometallics<\/i><\/em>\u00a02020<\/b><\/strong>, 39<\/i><\/em>, 688. doi:\u00a010.1021\/acs.organomet.9b00849<\/u><\/a>.<\/u><\/p>\n

(e) X. Yi, Y. Cao, X. Wang, H. Xu, S. Ban, H. Dai, Tetrahedron Let<\/i><\/em>t. 2020<\/b><\/strong>,\u00a061<\/i><\/em>, 151780.\u00a0doi:\u00a010.1016\/j.tetlet.2020.151780<\/u><\/a>.<\/u><\/p>\n

(f) W. Wu, Q. Tian, T. Chen, Z. Weng, Chem. – Eur. J.<\/i><\/em>\u00a0<\/i><\/em>2016<\/b><\/strong>, 22<\/i><\/em>, 16455. doi:\u00a010.1002\/chem.201604300<\/u><\/a>.<\/u><\/p>\n[5]\u00a0(a) Y. Kadoh, M. Tashiro, K. Oisaki, M. Kanai, Adv. Synth. Catal.<\/i><\/em>\u00a0<\/i><\/b><\/em><\/strong>2015<\/b><\/strong>,\u00a0357<\/i><\/em>, 2193. doi:\u00a010.1002\/adsc.201500131<\/u><\/a>.<\/u><\/p>\n

(b) S. A. Miller, K. A. Bisset, N. E. Leadbeater, N.\u00a0<\/i><\/em>Eddy, Eur. J. Org. Chem. <\/i><\/em>2019<\/b><\/strong>, 1413. doi:\u00a010.1002\/ejoc.201801718<\/u><\/a>.<\/u><\/p>\n

(c) C. B. Kelly, M. A. Mercadante, T. A. Hamlin, M. H. Fletcher, N. E. Leadbeater,Org. Chem.<\/i><\/em><\/i><\/b>2012<\/b><\/strong>,<\/i>77<\/i><\/em>, 8131. doi:\u00a010.1021\/jo301477s<\/u><\/a>.<\/u><\/p>\n

(d) Y. Tanaka, T. Ishihara, T.\u00a0<\/i><\/em>Konno, J. Fluorine Chem. <\/i><\/em>2012<\/b><\/strong>, 137<\/i><\/em>, 99. doi:\u00a010.1016\/j.jfluchem.2012.03.002<\/u><\/a>.<\/u><\/p>\n

(e) M. Kirihara, K.Suzuki, K. Nakakura, K. Saito, R. Nakamura, K. Tujimoto, Y. Sakamoto, Y. Kikkawa, H. Shimazu, Y.\u00a0Kimura, J. Fluorine Chem.<\/i><\/em>\u00a0<\/i><\/b><\/em><\/strong>2021<\/b><\/strong>, 243<\/i><\/em>, 109719. doi:\u00a010.1016\/j.jfluchem.2020.109719<\/u><\/a>.<\/u><\/p>\n[6]\u00a0(a) J. Boivin, L. E. Kaim, S. Z.\u00a0Zard, Tetrahedron <\/i><\/em>1995<\/b><\/strong>, 51<\/i><\/em>, 2573. doi:\u00a010.1016\/0040-4020(95)00006-T<\/u><\/a>.<\/u><\/p>\n

(b) Y. Chang, C.\u00a0Cai, J. Fluorine Chem.<\/i><\/em>\u00a02005<\/b><\/strong>, 126<\/i><\/em>, 937. doi:\u00a010.1016\/j.jfluchem.2005.04.012<\/u><\/a>.<\/u><\/p>\n

(c) M.\u00a0M. Kremlev, A. I. Mushta, W. Tyrra, D. Naumann, H. T. M. Fischer, Y. L. Yagupolskii, J. Fluorine Chem. <\/i><\/em>2007<\/b><\/strong>, 128<\/i><\/em>, 1385.\u00a0doi:\u00a010.1016\/j.jfluchem.2007.06.009<\/u><\/a>.<\/u><\/p>\n[7]\u00a0(a) Z. Han, S. Chen, Y. Tu, X. Lian, G.\u00a0<\/i><\/em>Li, Eur. J. Org. Chem.<\/i><\/em>\u00a02019<\/b><\/strong>, 4658. doi:\u00a010.1002\/ejoc.201900250<\/u><\/a>.<\/u><\/p>\n

(b) N. Allend\u00f6rfer, M. Es-Sayed, M. Nieger, S.\u00a0<\/i><\/em>Br\u00e4se,\u00a0<\/i><\/em>Tetrahedron Lett.<\/i><\/em>\u00a0<\/i><\/b><\/em><\/strong>2012<\/b><\/strong>,\u00a053<\/i><\/em>,388 doi:10.1016\/j.tetlet.2011.11.014<\/u><\/a>.<\/u><\/p>\n

(c) R. P. Singh, G. Cao, R. L. Kirchmeier, J. M. Shreeve, J. Org. Chem. <\/i><\/em>1999<\/b><\/strong>,\u00a064<\/i><\/em>, 2873. doi:\u00a010.1021\/jo982494c<\/u><\/a>.<\/u><\/p>\n

(d) J. B. Geri, M. M. W.\u00a0Wolfe, N. K.\u00a0<\/i><\/em>Szymczak, Angew. Chem. Int. Ed.<\/i><\/em>\u00a0<\/i><\/em>2018<\/b><\/strong>, 57<\/i><\/em>, 1381.\u00a0doi:\u00a010.1002\/anie.201711316<\/u><\/a>.<\/u><\/p>\n[8]\u00a0D. M. Rudzinski, C. B. Kelly, N. E. Leadbeater, Chem.<\/i><\/em>\u00a0<\/i><\/em>Commun.<\/i><\/em>\u00a0<\/i><\/b><\/em><\/strong>2012<\/b><\/strong>, 48<\/i><\/em>, 9610.\u00a0doi:\u00a010.1039\/C2CC35037H<\/u><\/a>.<\/u><\/p>\n[9]\u00a0(a) C. Liu, Z. Qin, C. Ji, X. Hong,\u00a0M. Szostak, Chem. Sci.<\/i><\/em>\u00a02019<\/b><\/strong>, 10<\/i><\/em>, 5736.\u00a0doi:\u00a010.1039\/C9SC00892F<\/u><\/a>.<\/u><\/p>\n

(b) Z. Li, L. Liu, K. Xu, T. Huang, X. Li, B. Song, T. Chen, Org. Lett.<\/i><\/em>\u00a0<\/i><\/b><\/em><\/strong>2020<\/b><\/strong>, 22<\/i><\/em>, 5517.\u00a0doi:\u00a010.1021\/acs.orglett.0c01869<\/u><\/a>.<\/u><\/p>\n

(c) C. Liu, C. Ji, T. Zhou,\u00a0X. Hong, M. Szostak, Angew. Chem. Int. Ed.<\/i><\/em>\u00a0<\/i><\/b><\/em><\/strong>2021<\/b><\/strong>, 60<\/i><\/em>, 10690.\u00a0doi:\u00a010.1002\/anie.202100949<\/u><\/a>.<\/u><\/p>\n

(d) X. Qiu, P. Wang,\u00a0D. Wang, M. Wang, Y. Yuan, Z.\u00a0<\/i><\/em>Shi, Angew. Chem.<\/i><\/em>\u00a0<\/i><\/em>Int. Ed.<\/i><\/em>\u00a02019<\/b><\/strong>, 58<\/i><\/em>, 1504.\u00a0doi:\u00a010.1002\/anie.201813182<\/u><\/a>.<\/u><\/p>\n

(e) C. Liu, C. Ji, X. Hong, M. Szostak, Angew. Chem. Int. Ed.<\/i><\/em>\u00a02018<\/b><\/strong>, 57<\/i><\/em>, 16721.\u00a0doi:\u00a010.1002\/anie.201810145<\/u><\/a>.<\/u><\/p>\n

 <\/p>\n

\u672c\u6587\u7248\u6743\u5c5e\u4e8e\u00a0Chem-Station\u5316\u5b66\u7a7a\u95f4<\/a>\uff0c \u6b22\u8fce\u70b9\u51fb\u6309\u94ae\u5206\u4eab\uff0c\u672a\u7ecf\u8bb8\u53ef\uff0c\u8c22\u7edd\u8f6c\u8f7d\uff01<\/strong><\/p>\n","protected":false},"excerpt":{"rendered":"\u672c\u6587\u4f5c\u8005\uff1a\u6749\u6749 \u5bfc\u8bfb \u8fd1\u65e5\uff0c\u6d77\u5357\u5927\u5b66\u7684\u9648\u94c1\u6865\u6559\u6388\u8bfe\u9898\u7ec4\u5728Org. Lett.\u4e2d\u53d1\u8868\u8bba\u6587\uff0c\u62a5\u9053\u4e00\u79cd\u9ad8\u6548\u5e76\u901a\u7528\u7684\u82ef\u7532\u9178\u4e0eTMSCF3\u4e4b\u95f4\u7684\u76f4\u63a5\u4e09\u6c1f\u7532\u57fa\u5316\u53cd\u5e94\u65b9\u6cd5\u5b66\u3002\u540c\u65f6\uff0c\u4f5c\u8005\u901a\u8fc7\u5bf9\u5177\u6709\u7fa7\u9178\u7ed3\u6784\u5355\u5143\u7684\u751f\u7269\u6d3b\u6027\u5206\u5b50\u76f4\u63a5\u4fee\u9970\u7684\u7814\u7a76\uff0c\u8fdb\u4e00\u6b65\u9610\u660e\u8fd9\u4e00\u7b56\u7565\u7684\u5408\u6210\u5e94\u7528\u4ef7\u503c\u3002\u6b64\u5916\uff0c\u8fd9\u4e00\u5168\u65b0\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u7b56\u7565\u5177\u6709\u5b9e\u9a8c\u64cd\u4f5c\u7b80\u6d01\u3001\u53cd\u5e94\u6761\u4ef6\u6e29\u548c\u3001\u539f\u6599\u6613\u5f97\u4ee5\u53ca\u5e95\u7269\u5e94\u7528\u8303\u56f4\u5e7f\u6cdb\u7b49\u4f18\u52bf\u3002 Trifluoromethylation of Benzoic Acids: An Access to Aryl Trifluoromethyl Ketones X. Liu, L. Liu, T. Huang, J. Zhang, Z. Tang, C. Li, T. Chen, Org. Lett. 2021, 23, 4930. doi: 10.1021\/acs.orglett.1c01720. \u6b63\u6587 \u6c1f\u539f\u5b50\u7684\u5f15\u5165\u662f\u5316\u5b66\u79d1\u5b66\u3001\u6750\u6599\u79d1\u5b66\u4ee5\u53ca\u751f\u7269\u79d1\u5b66\u4e2d\u7528\u4e8e\u589e\u5f3a\u6216\u6539\u53d8\u529f\u80fd\u6027\u6709\u673a\u5206\u5b50\u7269\u7406\u4e0e\u5316\u5b66\u6027\u80fd\u7684\u91cd\u8981\u7b56\u7565\u4e4b\u4e00\u3002\u6839\u636e\u76f8\u5173\u7684\u6587\u732e\u62a5\u9053\uff0c\u7ea620%\u7684\u836f\u7269\u5206\u5b50\u4ee5\u53ca30%\u7684\u519c\u836f\u5206\u5b50\u4e2d\u5b58\u5728\u6c1f\u539f\u5b50\u7684\u53d6\u4ee3\u3002\u540c\u65f6\uff0c\u4e09\u6c1f\u7532\u57fa\u916e\u4f5c\u4e3a\u91cd\u8981\u7684\u6709\u673a\u6c1f\u5316\u5408\u7269\uff0c\u9664\u5177\u6709\u8f83\u597d\u7684\u4eb2\u8102\u6027\u4e0e\u4ee3\u8c22\u7a33\u5b9a\u6027\u4e4b\u5916\uff0c\u540c\u6837\u5177\u6709\u8f83\u5f3a\u7684\u5438\u7535\u5b50\u7279\u6027\uff0c\u5e76\u80fd\u591f\u5f62\u6210\u8f83\u4e3a\u7a33\u5b9a\u7684\u6c34\u5408\u7269\u3002\u800c\u4e14\uff0c\u4e09\u6c1f\u7532\u57fa\u916e\u7c7b\u5316\u5408\u7269\u8868\u73b0\u51fa\u7684\u4e0a\u8ff0\u7279\u6b8a\u6027\u80fd\uff0c\u76ee\u524d\u5df2\u7ecf\u5e7f\u6cdb\u5e94\u7528\u4e8e\u836f\u7269\u5206\u5b50\u7684\u8bbe\u8ba1\u4e0e\u7814\u53d1\u3002\u5e76\u4e14\uff0c\u7531\u4e8e\u5176\u7fb0\u57fa\u5b98\u80fd\u56e2\u8868\u73b0\u51fa\u7684\u591a\u91cd\u53cd\u5e94\u6d3b\u6027\uff0c\u4e09\u6c1f\u7532\u57fa\u916e\u7c7b\u5316\u5408\u7269\u540c\u6837\u80fd\u591f\u4f5c\u4e3a\u6784\u5efa\u5176\u5b83\u542b\u6c1f\u529f\u80fd\u6709\u673a\u5206\u5b50\u7684\u91cd\u8981\u780c\u5757\u3002\u901a\u5e38\uff0c\u901a\u8fc7\u82b3\u57fa\u91d1\u5c5e\u8bd5\u5242 (Li\u6216Mg)\u4e0e\u4e09\u6c1f\u4e59\u9170\u57fa\u884d\u751f\u7269\u4e4b\u95f4\u7684\u4eb2\u6838\u53d6\u4ee3\u53cd\u5e94\u7b56\u7565\uff0c\u80fd\u591f\u8f83\u597d\u5730\u5b8c\u6210\u4e00\u7cfb\u5217\u4e09\u6c1f\u7532\u57fa\u916e\u5206\u5b50\u7684\u5408\u6210[1]\u3002\u7136\u800c\uff0c\u7531\u4e8e\u5176\u8f83\u4e3a\u82db\u523b\u7684\u53cd\u5e94\u6761\u4ef6\uff0c\u8fdb\u800c\u4f7f\u4e0a\u8ff0\u7b56\u7565\u7684\u8fdb\u4e00\u6b65\u5e94\u7528\u53d7\u5230\u9650\u5236\u3002\u540c\u65f6\uff0c\u7814\u7a76\u8868\u660e\uff0c\u91c7\u7528\u5bcc\u7535\u5b50\u82b3\u57fa\u5e95\u7269\u53c2\u4e0e\u7684Friedel-Crafts\u9170\u5316\u53cd\u5e94\u65b9\u6cd5\u5b66[2]\uff0c\u5219\u5b58\u5728\u5e95\u7269\u5e94\u7528\u8303\u56f4\u8f83\u4e3a\u6709\u9650\u4ee5\u53ca\u7f3a\u4e4f\u826f\u597d\u7684\u533a\u57df\u9009\u62e9\u6027\u63a7\u5236\u7b49\u95ee\u9898\u3002\u56e0\u6b64\uff0c\u6709\u673a\u5408\u6210\u5316\u5b66\u5bb6\u81f4\u529b\u4e8e\u53d1\u5c55\u4e00\u7cfb\u5217\u66f4\u4e3a\u6709\u6548\u7684\u53cd\u5e94\u7b56\u7565\uff0c\u5b9e\u73b0\u4e09\u6c1f\u7532\u57fa\u916e\u5206\u5b50\u7684\u9ad8\u6548\u5236\u5907 (Scheme 1)\u00a0[3]\u3002\u76ee\u524d\uff0c\u5df2\u7ecf\u6210\u529f\u5f00\u53d1\u51fa\u91c7\u7528\u8fc7\u6e21\u91d1\u5c5e\u50ac\u5316\u7684\u82b3\u5364\u6216\u82b3\u9999\u62df\u5364\u4ee3\u7269\u53c2\u4e0e\u7684\u4e09\u6c1f\u4e59\u9170\u5316\u53cd\u5e94\u65b9\u6cd5\u5b66\uff0c\u5e76\u8fdb\u4e00\u6b65\u5e94\u7528\u4e8e\u4e09\u6c1f\u7532\u57fa\u916e\u7c7b\u5316\u5408\u7269\u7684\u5236\u5907[4]\u3002\u540c\u65f6\uff0c\u901a\u8fc7\u03b1-\u4e09\u6c1f\u7532\u9187\u7684\u6c27\u5316\u53cd\u5e94\u65b9\u6cd5\u5b66\uff0c\u540c\u6837\u80fd\u591f\u5b9e\u73b0\u76f8\u5e94\u4e09\u6c1f\u7532\u57fa\u916e\u7c7b\u5316\u5408\u7269\u7684\u5408\u6210[5]\uff0c\u7136\u800c\uff0c\u5728\u8fd9\u4e00\u7b56\u7565\u4e2d\uff0c\u9700\u8981\u9009\u62e9\u8f83\u4e0d\u7a33\u5b9a\u7684\u919b\u4f5c\u4e3a\u8d77\u59cb\u539f\u6599\uff0c\u8fdb\u884c\u76f8\u5e94\u9187\u5e95\u7269\u7684\u9884\u5148\u5408\u6210\u3002\u5e76\u4e14\uff0c\u53cd\u5e94\u8fc7\u7a0b\u4e2d\u901a\u5e38\u9700\u8981\u9009\u62e9\u8d85\u5316\u5b66\u8ba1\u91cf (overstoichiometric)\u7684\u7279\u6b8a\u6c27\u5316\u5242\u3002\u4e3a\u6709\u6548\u89e3\u51b3\u4e0a\u8ff0\u7b56\u7565\u4e2d\u5b58\u5728\u7684\u8bf8\u591a\u5c40\u9650\uff0c\u8fd9\u91cc\uff0c\u672c\u6587\u5c06\u62a5\u9053\u4e00\u79cd\u82ef\u7532\u9178\u4e0eTMSCF3\u4e4b\u95f4\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u53cd\u5e94\u65b9\u6cd5\u5b66\uff0c\u8fdb\u800c\u4ee5\u826f\u597d\u81f3\u4f18\u826f\u7684\u53cd\u5e94\u6536\u7387\uff0c\u83b7\u5f97\u4e00\u7cfb\u5217\u76f8\u5e94\u7684\u82b3\u57fa\u4e09\u6c1f\u7532\u57fa\u916e\u7c7b\u5206\u5b50 (Scheme 1)\u3002\u5e76\u4e14\uff0c\u8fd9\u4e00\u5168\u65b0\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u7b56\u7565\u5177\u6709\u5b9e\u9a8c\u64cd\u4f5c\u7b80\u6d01\u3001\u53cd\u5e94\u6761\u4ef6\u6e29\u548c\u3001\u539f\u6599\u6613\u5f97\u4ee5\u53ca\u5e95\u7269\u5e94\u7528\u8303\u56f4\u5e7f\u6cdb\u7b49\u4f18\u52bf\u3002 \u9996\u5148\uff0c\u4f5c\u8005\u91c7\u75284-\u82ef\u57fa\u82ef\u7532\u91781a\u4e0eTMSCF3\u4f5c\u4e3a\u6a21\u578b\u5e95\u7269\uff0c\u8fdb\u884c\u76f8\u5173\u53cd\u5e94\u6761\u4ef6\u7684\u4f18\u5316\u7b5b\u9009 (Table 1)\u3002\u8fdb\u800c\u786e\u5b9a\u6700\u4f73\u7684\u53cd\u5e94\u6761\u4ef6\u4e3a\uff1a\u91c7\u7528DMAP\u4f5c\u4e3a\u78b1\uff0c\u82ef\u7532\u919a\u4f5c\u4e3a\u53cd\u5e94\u6eb6\u5242\uff0c\u540c\u65f6\u52a0\u5165TFAA\u4e0eCsF\uff0c\u5728\u53cd\u5e94\u6e29\u5ea6\u4e3a120\u2103\u7684\u6761\u4ef6\u4e0b\u8fdb\u884c\u53cd\u5e94\uff0c\u6700\u7ec8\u83b7\u5f9790%\u6536\u7387\u7684\u76ee\u6807\u4ea7\u72693a\u3002   \u5728\u83b7\u5f97\u4e0a\u8ff0\u7684\u6700\u4f73\u53cd\u5e94\u6761\u4ef6\u4e4b\u540e\uff0c\u4f5c\u8005\u5f00\u59cb\u5bf9\u7fa7\u9178\u5e95\u7269\u7684\u5e94\u7528\u8303\u56f4\u8fdb\u884c\u8003\u5bdf (Table 2)\u3002\u7814\u7a76\u8868\u660e\uff0c\u82ef\u73af\u4e2d\u5177\u6709\u4e0d\u540c\u5438\u7535\u5b50\u4e0e\u4f9b\u7535\u5b50\u57fa\u56e2\u53d6\u4ee3\u7684\u82ef\u7532\u9178\u5e95\u7269\uff0c\u5747\u80fd\u591f\u987a\u5229\u5730\u53c2\u4e0e\u4e0a\u8ff0\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u8fc7\u7a0b\uff0c\u5e76\u83b7\u5f97\u76f8\u5e94\u7684\u76ee\u6807\u4ea7\u72693a–3q\u3002\u540c\u65f6\uff0c\u4f5c\u8005\u53d1\u73b0\uff0c\u4e0a\u8ff0\u5bf9\u6807\u51c6\u53cd\u5e94\u6761\u4ef6\u5bf9\u4e8e\u8418\u7532\u9178\u4e0e\u591a\u73af\u82b3\u9999\u7fa7\u9178\u4ee5\u53ca\u6742\u73af\u82b3\u9999\u7fa7\u9178\u5e95\u7269\uff0c\u540c\u6837\u80fd\u591f\u6709\u6548\u5730\u517c\u5bb9\uff0c\u5e76\u83b7\u5f97\u76f8\u5e94\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u4ea7\u72693r–3z\u3002\u6b64\u5916\uff0c\u4f5c\u8005\u8fdb\u4e00\u6b65\u53d1\u73b0\uff0c\u4e0a\u8ff0\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u7b56\u7565\u540c\u6837\u80fd\u591f\u5e94\u7528\u4e8e\u5404\u7c7b\u8102\u80aa\u65cf\u7fa7\u9178\u5e95\u7269\uff0c\u5e76\u83b7\u5f97\u76f8\u5e94\u7684\u4e09\u6c1f\u7532\u57fa\u916e\u4ea7\u72693aa\u4e0e3ab\uff0c\u7136\u800c\uff0c\u5374\u8868\u73b0\u51fa\u53cd\u5e94\u6536\u7387\u7684\u663e\u8457\u964d\u4f4e\uff0c\u53ef\u80fd\u6e90\u81ea\u4e8e\u7fb0\u57fa\u78b3\u7684\u7535\u5b50\u5bc6\u5ea6\u76f8\u5bf9\u8f83\u9ad8\uff0c\u56e0\u800c\uff0c\u4e0d\u5229\u4e8e\u540e\u7eed\u4eb2\u6838\u52a0\u6210\u6b65\u9aa4\u7684\u8fdb\u884c\u3002 \u4e3a\u8fdb\u4e00\u6b65\u9610\u660e\u8fd9\u4e00\u7b56\u7565\u7684\u5408\u6210\u5b9e\u7528\u6027\uff0c\u4f5c\u8005\u53d1\u73b0\uff0c\u91c7\u7528\u4e0a\u8ff0\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u6761\u4ef6\uff0c\u80fd\u591f\u6210\u529f\u5730\u5bf9\u4e00\u7cfb\u5217\u5177\u6709\u751f\u7269\u6d3b\u6027\u7684\u7fa7\u9178\u5206\u5b50\u8fdb\u884c\u76f4\u63a5\u4fee\u9970\uff0c\u5e76\u83b7\u5f97\u76f8\u5e94\u7684\u4e09\u6c1f\u7532\u57fa\u916e\u4ea7\u7269 (Scheme 2)\u3002\u4f8b\u5982\uff0c\u7528\u4e8e\u76ae\u80a4\u75c5\u6cbb\u7597\u7684\u4e34\u5e8a\u836f\u7269adapalin\uff0c\u5728\u4e0a\u8ff0\u7684\u6807\u51c6\u53cd\u5e94\u6761\u4ef6\u4e0b\uff0c\u80fd\u591f\u8f83\u4e3a\u5bb9\u6613\u5730\u8fdb\u884c\u76f8\u5e94\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u8fc7\u7a0b\uff0c\u5e76\u4ee580%\u7684\u6536\u7387\u83b7\u5f97\u76f8\u5e94\u76ee\u6807\u4ea7\u72693ac\u3002\u800c\u4f5c\u4e3a\u6297\u75db\u98ce\u836f\u7269 (antigout drug)\u4ee5\u53ca\u6297\u751f\u7d20\u4f50\u5242 (antibiotic adjuvant)\u7684probenecid\u5206\u5b50\uff0c\u5728\u8fd9\u4e00\u5168\u65b0\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u53cd\u5e94\u6761\u4ef6\u4e0b\uff0c\u80fd\u591f\u4ee590%\u7684\u6536\u7387\u83b7\u5f97\u76f8\u5e94\u7684\u4e09\u6c1f\u7532\u57fa\u916e\u4ea7\u72693ad\u3002\u4e4b\u540e\uff0c\u4f5c\u8005\u53d1\u73b0\uff0c\u5c06\u7528\u4e8e\u51a0\u5fc3\u75c5\u4e34\u5e8a\u6cbb\u7597\u7684\u836f\u7269\u5206\u5b503-\u7532\u57fa\u9ec4\u916e-8-\u7fa7\u9178\u5e94\u7528\u4e8e\u4e0a\u8ff0\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u53cd\u5e94\u65f6\uff0c\u80fd\u591f\u4ee580%\u7684\u6536\u7387\uff0c\u83b7\u5f97\u76f8\u5e94\u7684\u76ee\u6807\u4ea7\u72693ae\u3002\u540c\u65f6\uff0c\u4f5c\u8005\u8fdb\u4e00\u6b65\u53d1\u73b0\uff0c\u6297\u9ad8\u8840\u538b\u836f\u7269telmisartan\u5728\u4e0a\u8ff0\u7684\u6807\u51c6\u53cd\u5e94\u6761\u4ef6\u4e0b\uff0c\u540c\u6837\u80fd\u591f\u4ee554%\u7684\u53cd\u5e94\u6536\u7387\uff0c\u83b7\u5f97\u76f8\u5e94\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u4ea7\u72693af\u3002 \u63a5\u4e0b\u6765\uff0c\u4f5c\u8005\u8fdb\u884c\u4e00\u7cfb\u5217\u514b\u7ea7\u89c4\u6a21\u5b9e\u9a8c\u7684\u7814\u7a76 (Scheme 3)\u3002\u8be5\u5c0f\u7ec4\u53d1\u73b0\uff0c\u91c7\u7528probenecid\u00a01ad\u4f5c\u4e3a\u6a21\u578b\u5e95\u7269\uff0c\u5728\u4e0a\u8ff0\u7684\u6807\u51c6\u53cd\u5e94\u6761\u4ef6\u4e0b\uff0c\u5206\u522b\u8fdb\u884c1mmol\u30012mmol\u4ee5\u53ca5 mmol\u89c4\u6a21\u7684\u53cd\u5e94\u5b9e\u9a8c\u3002\u7814\u7a76\u53d1\u73b0\uff0c\u901a\u8fc7\u4e00\u7cfb\u5217\u76f8\u5173\u7684\u5b9e\u9a8c\u540e\u5904\u7406\u64cd\u4f5c\u4e4b\u540e\uff0c\u9009\u62e9\u7845\u80f6\u67f1\u8272\u8c31\u8fdb\u884c\u5206\u79bb\uff0c\u5747\u80fd\u591f\u83b7\u5f97\u8f83\u9ad8\u6536\u7387\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u4ea7\u72693ad\uff0c\u8fdb\u800c\u8868\u660e\uff0c\u8fd9\u4e00\u5168\u65b0\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u53cd\u5e94\u65b9\u6cd5\u5b66\u5177\u6709\u826f\u597d\u7684\u5408\u6210\u5e94\u7528\u4ef7\u503c\u3002 \u6700\u540e\uff0c\u6839\u636e\u524d\u671f\u7684\u6587\u732e\u62a5\u9053[6]-[9]\uff0c\u4f5c\u8005\u63d0\u51fa\u4e00\u79cd\u5408\u7406\u7684\u53cd\u5e94\u673a\u7406 (Scheme 4)\u3002\u9996\u5148\uff0c\u7fa7\u91781\u901a\u8fc7TFAA\u7684\u539f\u4f4d\u6d3b\u5316\uff0c\u5f62\u6210\u6df7\u5408\u9178\u9150A\u3002\u4e4b\u540e\uff0c\u5728CsF\u4e0e\u00a0DMAP\u7684\u8f85\u52a9\u4e0b\uff0c\u6df7\u5408\u9178\u9150A\u00a0\u4e0eTMSCF3\u7ecf\u5386\u4eb2\u6838\u52a0\u6210-\u6d88\u9664\u8fc7\u7a0b\uff0c\u5f62\u6210\u76f8\u5e94\u7684\u4e09\u6c1f\u7532\u57fa\u916e\u4ea7\u72693\u3002 \u603b\u7ed3 \u6d77\u5357\u5927\u5b66\u9648\u94c1\u6865\u6559\u6388\u8bfe\u9898\u7ec4\u62a5\u9053\u4e00\u79cd\u73af\u5883\u53cb\u597d\u7684\uff0c\u5e76\u901a\u8fc7\u5ec9\u4ef7\u6613\u5f97\u7684\u7fa7\u9178\u4f5c\u4e3a\u8d77\u59cb\u539f\u6599\u8fdb\u884c\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u53cd\u5e94\u65b9\u6cd5\u5b66\uff0c\u5e76\u6210\u529f\u5b8c\u6210\u4e00\u7cfb\u5217\u4e09\u6c1f\u7532\u57fa\u916e\u5206\u5b50\u7684\u6784\u5efa\u3002\u8fd9\u4e00\u5168\u65b0\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u7b56\u7565\u5177\u6709\u5b9e\u9a8c\u64cd\u4f5c\u7b80\u6d01\u3001\u53cd\u5e94\u6761\u4ef6\u6e29\u548c\u3001\u539f\u6599\u6613\u5f97\u3001\u5e95\u7269\u5e94\u7528\u8303\u56f4\u5e7f\u6cdb\u4ee5\u53ca\u4f18\u826f\u7684\u5b98\u80fd\u56e2\u517c\u5bb9\u6027\u7b49\u4f18\u52bf\u3002\u6b64\u5916\uff0c\u8be5\u5c0f\u7ec4\u901a\u8fc7\u5bf9\u4e00\u7cfb\u5217\u5177\u6709\u826f\u597d\u751f\u7269\u6d3b\u6027\u7684\u7fa7\u9178\u5206\u5b50\u7684\u76f4\u63a5\u4fee\u9970\u4ee5\u53ca\u540e\u7eed\u514b\u7ea7\u89c4\u6a21\u5b9e\u9a8c\u7684\u7814\u7a76\uff0c\u8fdb\u4e00\u6b65\u9610\u660e\u8fd9\u4e00\u5168\u65b0\u7684\u4e09\u6c1f\u7532\u57fa\u5316\u7b56\u7565\u5177\u6709\u826f\u597d\u7684\u5408\u6210\u5e94\u7528\u524d\u666f\u3002 \u53c2\u8003\u6587\u732e [1]\u00a0(a) R. J. Andrew, J. M. Mellor, Tetrahedron\u00a02000, 56,\u00a07261. doi:\u00a010.1016\/S0040-4020(00)00597-4. (b) L. Zhu, Z. Miao, C. Sheng, J. Yao, C. Zhuang, W. Zhang, J. Fluorine Chem. 2010, 131, 800. doi:\u00a010.1016\/j.jfluchem.2010.04.002. (c) B. Heinz, D. Djukanovic, M. A. Ganiek, B. Martin, B. Schenkel, P. 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