{"id":41606,"date":"2022-04-15T08:00:38","date_gmt":"2022-04-15T00:00:38","guid":{"rendered":"\/\/www.gsbet888.com\/?p=41606"},"modified":"2022-04-11T17:08:12","modified_gmt":"2022-04-11T09:08:12","slug":"green-chem-%ef%bc%9atempo%e5%82%ac%e5%8c%96%e7%9a%84%e7%94%b5%e5%8c%96%e5%ad%a6%e5%8e%bb%e6%b0%a2%e7%8e%af%e7%bc%a9%e5%90%88%e5%8f%8d%e5%ba%94%e6%96%b9%e6%b3%95%e5%ad%a6","status":"publish","type":"post","link":"\/\/www.gsbet888.com\/%e5%8c%96%e5%ad%a6%e6%9d%82%e8%ae%b0\/recentpaper\/2022\/04\/green-chem-%ef%bc%9atempo%e5%82%ac%e5%8c%96%e7%9a%84%e7%94%b5%e5%8c%96%e5%ad%a6%e5%8e%bb%e6%b0%a2%e7%8e%af%e7%bc%a9%e5%90%88%e5%8f%8d%e5%ba%94%e6%96%b9%e6%b3%95%e5%ad%a6.html","title":{"rendered":"Green Chem.\uff1aTEMPO\u50ac\u5316\u7684\u7535\u5316\u5b66\u53bb\u6c22\u73af\u7f29\u5408\u53cd\u5e94\u65b9\u6cd5\u5b66"},"content":{"rendered":"
\u672c\u6587\u4f5c\u8005:\u6749\u6749<\/p>\n
\u8fd1\u65e5\uff0c\u6e29\u5dde\u533b\u79d1\u5927\u5b66\u7684\u8521\u4e91\u745e\u8bfe\u9898\u7ec4\u5728Green Chem.<\/em>\u4e2d\u53d1\u8868\u8bba\u6587\uff0c\u62a5\u9053\u4e00\u79cd\u5168\u65b0\u7684\u91c7\u7528TEMPO\u50ac\u5316\u5242\u4fc3\u8fdb\u7684\u901a\u8fc7\u4e00\u7cfb\u5217\u90bb\u6c28\u57fa\u82ef\u915a\u7c7b\u5e95\u7269\u53c2\u4e0e\u7684\u7535\u5316\u5b66\u53bb\u6c22\u73af\u7f29\u5408\u53cd\u5e94 (dehydrogenative cyclocondensation)\u65b9\u6cd5\u5b66\u3002\u8fd9\u4e00\u5168\u65b0\u7684\u7535\u5316\u5b66\u53bb\u6c22\u73af\u7f29\u5408\u53cd\u5e94\u7b56\u7565\u5177\u6709\u6e29\u548c\u7684\u53cd\u5e94\u6761\u4ef6\u3001\u65e0\u9700\u9009\u62e9\u5316\u5b66\u8ba1\u91cf\u7684\u6c27\u5316\u5242\u4ee5\u53ca\u50ac\u5316\u5242\u5ec9\u4ef7\u6613\u5f97\u7b49\u4f18\u52bf\u3002<\/p>\n TEMPO-Catalyzed Electrochemical Dehydrogenative Cyclocondensation of o<\/em>-Aminophenols: Synthesis of Aminophenoxazinones as Antiproliferative Agents<\/p>\n Zhou, Z. Ma, C. Shonhe, S. Ji, Y. Cai, Green Chem.<\/em> 2021<\/strong>, 23<\/em><\/strong>, 8566. doi: 10.1039\/D1GC02908H<\/a>.<\/p><\/blockquote>\n 2-\u6c28\u57fa\u5429\u5641\u55ea\u916e (2-aminophenoxazinone)\u9aa8\u67b6\u5355\u5143\u5e7f\u6cdb\u5b58\u5728\u4e8e\u5404\u7c7b\u751f\u7406\u6d3b\u6027\u5929\u7136\u4ea7\u7269\u5206\u5b50\u4e2d\u3002\u56e0\u6b64\uff0c\u5bf9\u4e8e\u6784\u5efa\u6c28\u57fa\u5429\u5641\u55ea\u916e\u7c7b\u9aa8\u67b6\u76f8\u5173\u7684\u5408\u6210\u7b56\u7565\u7814\u7a76\u5df2\u7ecf\u5f00\u59cb\u53d7\u5230\u8bf8\u591a\u7814\u7a76\u56e2\u961f\u7684\u5e7f\u6cdb\u5173\u6ce8 (Scheme 1)[1]-[2]<\/sup>\u3002\u8fd9\u91cc\uff0c\u53d7\u5230\u8fd1\u5e74\u6765\u5bf9\u4e8e\u6709\u673a\u7535\u5316\u5b66\u5408\u6210[3]<\/sup>\u7b56\u7565\u4e2d\u901a\u8fc7\u6c27\u5316\u8fd8\u539f\u5a92\u4ecb (redox mediator)\u5b9e\u73b0\u95f4\u63a5\u7535\u89e3\u7684\u76f8\u5173\u7814\u7a76\u62a5\u9053[4]<\/sup>\u7684\u542f\u53d1\uff0c\u6e29\u5dde\u533b\u79d1\u5927\u5b66\u7684\u8521\u4e91\u745e\u56e2\u961f\u6210\u529f\u8bbe\u8ba1\u51fa\u4e00\u79cd\u5168\u65b0\u7684\u901a\u8fc7TEMPO\u50ac\u5316\u5242\u4fc3\u8fdb\u7684\u91c7\u7528\u90bb\u6c28\u57fa\u82ef\u915a\u7c7b\u5e95\u7269\u53c2\u4e0e\u7684\u7535\u5316\u5b66\u53bb\u6c22\u73af\u7f29\u5408\u53cd\u5e94\u65b9\u6cd5\u5b66\uff0c\u8fdb\u800c\u987a\u5229\u5b8c\u6210\u4e00\u7cfb\u52172-\u6c28\u57fa\u5429\u5641\u55ea-3-\u916e\u7c7b\u5206\u5b50\u7684\u6784\u5efa (Scheme 1C)\u3002<\/p>\n \u9996\u5148\uff0c\u4f5c\u8005\u91c7\u7528\u90bb\u6c28\u57fa\u82ef\u915a1a<\/strong>\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\u7528TEMPO\u4f5c\u4e3a\u50ac\u5316\u5242\uff0cn<\/em>Bu4<\/sub>NBF4<\/sub>\u4f5c\u4e3a\u652f\u6301\u7535\u89e3\u8d28\uff0c\u5728\u65e0\u9694\u819c\u7535\u89e3\u69fd\u4e2d\uff0c\u91c7\u7528RVC (reticulated vitreous carbon)\u4f5c\u4e3a\u9633\u6781\uff0cPt\u677f (Pt plate)\u4f5c\u4e3a\u9634\u6781\uff0cDMF\u4f5c\u4e3a\u53cd\u5e94\u6eb6\u5242\uff0c\u53cd\u5e94\u6e29\u5ea6\u4e3a\u5ba4\u6e29\uff0c\u6700\u7ec8\u83b7\u5f9786%\u6536\u7387\u7684\u53bb\u6c22\u73af\u7f29\u5408\u4ea7\u72692a<\/strong>\u3002<\/p>\n \u540c\u65f6\uff0c\u4f5c\u8005\u901a\u8fc7\u76f8\u5173\u7684CV\u5b9e\u9a8c (Scheme 2A)\u7814\u7a76\u8868\u660e\uff0c\u4e0a\u8ff0\u7684\u7535\u5316\u5b66\u53bb\u6c22\u73af\u7f29\u5408\u8fc7\u7a0b\u4e2d\u53ef\u80fd\u6d89\u53caTEMPO+<\/sup>\u4e2d\u95f4\u4f53\u7684\u53c2\u4e0e\u3002\u4e4b\u540e\uff0c\u8be5\u5c0f\u7ec4\u901a\u8fc7\u4e00\u7cfb\u5217\u63a7\u5236\u5b9e\u9a8c (Scheme 2B)\u7684\u76f8\u5173\u7814\u7a76\u8fdb\u4e00\u6b65\u8bc1\u5b9e\uff0c\u53cd\u5e94\u8fc7\u7a0b\u4e2d\u6d89\u53ca\u81ea\u7531\u57fa\u4e2d\u95f4\u4f53\u7684\u53c2\u4e0e\u3002<\/p>\n \u57fa\u4e8e\u4e0a\u8ff0\u7684\u5b9e\u9a8c\u7814\u7a76\u4ee5\u53ca\u524d\u671f\u7684\u6587\u732e\u62a5\u9053[5]<\/sup>\uff0c\u4f5c\u8005\u63d0\u51fa\u5982\u4e0b\u5408\u7406\u7684\u53cd\u5e94\u673a\u7406 (Scheme 3)\u3002<\/p>\n \u4e4b\u540e\uff0c\u5728\u4e0a\u8ff0\u7684\u6700\u4f73\u53cd\u5e94\u6761\u4ef6\u4e0b\uff0c\u4f5c\u8005\u5bf9\u4e00\u7cfb\u5217\u90bb\u6c28\u57fa\u82ef\u915a\u5e95\u7269\u7684\u5e94\u7528\u8303\u56f4\u8fdb\u884c\u8003\u5bdf (Scheme 4)\u3002\u7814\u7a76\u8868\u660e\uff0c\u5728\u82ef\u73af\u7684C3-\u6216C6-\u4f4d\u7f6e\u5e26\u6709\u4e0d\u540c\u4f9b\u7535\u5b50\u4e0e\u5438\u7535\u5b50\u57fa\u56e2\u53d6\u4ee3\u7684\u90bb\u6c28\u57fa\u82ef\u915a\u5e95\u7269\uff0c\u5747\u80fd\u591f\u8f83\u597d\u5730\u4e0e\u4e0a\u8ff0\u7684\u6807\u51c6\u53cd\u5e94\u6761\u4ef6\u517c\u5bb9\uff0c\u5e76\u4ee5\u4e2d\u7b49\u81f3\u826f\u597d\u7684\u53cd\u5e94\u6536\u7387\uff0c\u83b7\u5f97\u76f8\u5e94\u7684\u53bb\u6c22\u73af\u7f29\u5408\u4ea7\u72692a<\/strong>–2h<\/strong>\u3002\u540c\u65f6\uff0c\u7814\u7a76\u53d1\u73b0\uff0c\u4e0a\u8ff0\u7684\u6700\u4f73\u53cd\u5e94\u6761\u4ef6\u5bf9\u4e8e\u5728\u82ef\u73af\u7684C4-\u6216C5-\u4f4d\u7f6e\u5e26\u6709\u5364\u7d20\u4ee5\u53ca\u78fa\u9178\u57fa\u79bb\u53bb\u57fa\u56e2\u7684\u90bb\u6c28\u57fa\u82ef\u915a\u5e95\u7269\u4ee5\u53ca\u5728\u82ef\u73af\u7684C5-\u4f4d\u7f6e\u5177\u6709\u7532\u57fa\u53d6\u4ee3\u7684\u90bb\u6c28\u57fa\u82ef\u915a\u5e95\u7269\uff0c\u540c\u6837\u80fd\u591f\u6709\u6548\u5730\u517c\u5bb9\u3002<\/p>\n \u540c\u65f6\uff0c\u4f5c\u8005\u8fdb\u4e00\u6b65\u7814\u7a76\u53d1\u73b0\uff0c\u4e0a\u8ff0\u7684\u7535\u5316\u5b66\u53bb\u6c22\u73af\u7f29\u5408\u7b56\u7565\u540c\u6837\u80fd\u591f\u6709\u6548\u5730\u5e94\u7528\u4e8e\u90bb\u82ef\u4e8c\u80fa (1p<\/strong>)\u4ee5\u53ca2-\u82ef\u57fa\u6c28\u57fa\u82ef\u80fa (1q<\/strong>)\u5e95\u7269 (Scheme 5)\u3002 \u7136\u800c\uff0c\u5bf9\u4e8e2-\u6c28\u57fa\u82ef\u786b\u9187(1r<\/strong>)\u30012-\u6c28\u57fa\u5421\u5576-3-\u9187(1s<\/strong>)\u30012-\u6c28\u57fa-3-\u785d\u57fa\u82ef\u915a(1t<\/strong>)\u4ee5\u53ca2-(\u7532\u6c28\u57fa)\u82ef\u915a(1u<\/strong>) \u5e95\u7269\uff0c\u5219\u5747\u672a\u80fd\u83b7\u5f97\u9884\u671f\u7684\u76ee\u6807\u4ea7\u7269 (ESI<\/a>, Fig. S3-S6)\u3002<\/p>\n \u4e4b\u540e\uff0c\u8be5\u5c0f\u7ec4\u901a\u8fc7\u5982\u4e0b\u7684\u5b9e\u9a8c\u88c5\u7f6e\uff0c\u5bf9\u4e8e\u4e0a\u8ff0\u7684\u53bb\u6c22\u73af\u7f29\u5408\u7b56\u7565\u7684\u514b\u7ea7\u89c4\u6a21\u53cd\u5e94\u8fdb\u884c\u8fdb\u4e00\u6b65\u7814\u7a76\uff0c\u8fdb\u800c\u8868\u660e\uff0c\u8fd9\u4e00\u5168\u65b0\u7684\u53bb\u6c22\u73af\u7f29\u5408\u7b56\u7565\u5177\u6709\u6f5c\u5728\u7684\u5408\u6210\u5e94\u7528\u4ef7\u503c (Fig. S7)\u3002<\/p>\n \u540c\u65f6\uff0c\u8be5\u5c0f\u7ec4\u8fdb\u4e00\u6b65\u7814\u7a76\u53d1\u73b0\uff0c\u901a\u8fc7\u4e0a\u8ff0\u7684\u53bb\u6c22\u73af\u7f29\u5408\u7b56\u7565\u83b7\u5f97\u7684\u76ee\u6807\u4ea7\u72692h<\/strong>\u8868\u73b0\u51fa\u4f18\u826f\u7684\u6297\u80bf\u7624\u6d3b\u6027(Fig. 1)\u3002<\/p>\n \u6e29\u5dde\u533b\u79d1\u5927\u5b66\u7684\u8521\u4e91\u745e\u8bfe\u9898\u7ec4\u6210\u529f\u8bbe\u8ba1\u51fa\u4e00\u79cd\u5168\u65b0\u7684\u91c7\u7528TEMPO\u50ac\u5316\u5242\u4fc3\u8fdb\u7684\u901a\u8fc7\u4e00\u7cfb\u5217\u90bb\u6c28\u57fa\u82ef\u915a\u7c7b\u5e95\u7269\u53c2\u4e0e\u7684\u7535\u5316\u5b66\u53bb\u6c22\u73af\u7f29\u5408\u53cd\u5e94\u65b9\u6cd5\u5b66\u3002\u8fd9\u4e00\u5168\u65b0\u7684\u7535\u5316\u5b66\u53bb\u6c22\u73af\u7f29\u5408\u53cd\u5e94\u7b56\u7565\u5177\u6709\u6e29\u548c\u7684\u53cd\u5e94\u6761\u4ef6\u3001\u65e0\u9700\u9009\u62e9\u5316\u5b66\u8ba1\u91cf\u7684\u6c27\u5316\u5242\u4ee5\u53ca\u50ac\u5316\u5242\u5ec9\u4ef7\u6613\u5f97\u4ee5\u53ca\u826f\u597d\u7684\u5408\u6210\u5e94\u7528\u4ef7\u503c\u7b49\u4f18\u52bf\u3002<\/p>\n \u672c\u6587\u7248\u6743\u5c5e\u4e8e\u00a0Chem-Station\u5316\u5b66\u7a7a\u95f4\uff0c \u6b22\u8fce\u70b9\u51fb\u6309\u94ae\u5206\u4eab\uff0c\u672a\u7ecf\u8bb8\u53ef\uff0c\u8c22\u7edd\u8f6c\u8f7d<\/p>\n <\/p>\n","protected":false},"excerpt":{"rendered":"\u672c\u6587\u4f5c\u8005:\u6749\u6749 \u5bfc\u8bfb \u8fd1\u65e5\uff0c\u6e29\u5dde\u533b\u79d1\u5927\u5b66\u7684\u8521\u4e91\u745e\u8bfe\u9898\u7ec4\u5728Green Chem.\u4e2d\u53d1\u8868\u8bba\u6587\uff0c\u62a5\u9053\u4e00\u79cd\u5168\u65b0\u7684\u91c7\u7528TEMPO\u50ac\u5316\u5242\u4fc3\u8fdb\u7684\u901a\u8fc7\u4e00\u7cfb\u5217\u90bb\u6c28\u57fa\u82ef\u915a\u7c7b\u5e95\u7269\u53c2\u4e0e\u7684\u7535\u5316\u5b66\u53bb\u6c22\u73af\u7f29\u5408\u53cd\u5e94 (dehydrogenative cyclocondensation)\u65b9\u6cd5\u5b66\u3002\u8fd9\u4e00\u5168\u65b0\u7684\u7535\u5316\u5b66\u53bb\u6c22\u73af\u7f29\u5408\u53cd\u5e94\u7b56\u7565\u5177\u6709\u6e29\u548c\u7684\u53cd\u5e94\u6761\u4ef6\u3001\u65e0\u9700\u9009\u62e9\u5316\u5b66\u8ba1\u91cf\u7684\u6c27\u5316\u5242\u4ee5\u53ca\u50ac\u5316\u5242\u5ec9\u4ef7\u6613\u5f97\u7b49\u4f18\u52bf\u3002 TEMPO-Catalyzed Electrochemical Dehydrogenative Cyclocondensation of o-Aminophenols: Synthesis of Aminophenoxazinones as Antiproliferative Agents Zhou, Z. Ma, C. Shonhe, S. Ji, Y. Cai, Green Chem. 2021, 23, 8566. doi: 10.1039\/D1GC02908H. \u6b63\u6587 2-\u6c28\u57fa\u5429\u5641\u55ea\u916e (2-aminophenoxazinone)\u9aa8\u67b6\u5355\u5143\u5e7f\u6cdb\u5b58\u5728\u4e8e\u5404\u7c7b\u751f\u7406\u6d3b\u6027\u5929\u7136\u4ea7\u7269\u5206\u5b50\u4e2d\u3002\u56e0\u6b64\uff0c\u5bf9\u4e8e\u6784\u5efa\u6c28\u57fa\u5429\u5641\u55ea\u916e\u7c7b\u9aa8\u67b6\u76f8\u5173\u7684\u5408\u6210\u7b56\u7565\u7814\u7a76\u5df2\u7ecf\u5f00\u59cb\u53d7\u5230\u8bf8\u591a\u7814\u7a76\u56e2\u961f\u7684\u5e7f\u6cdb\u5173\u6ce8 (Scheme 1)[1]-[2]\u3002\u8fd9\u91cc\uff0c\u53d7\u5230\u8fd1\u5e74\u6765\u5bf9\u4e8e\u6709\u673a\u7535\u5316\u5b66\u5408\u6210[3]\u7b56\u7565\u4e2d\u901a\u8fc7\u6c27\u5316\u8fd8\u539f\u5a92\u4ecb (redox mediator)\u5b9e\u73b0\u95f4\u63a5\u7535\u89e3\u7684\u76f8\u5173\u7814\u7a76\u62a5\u9053[4]\u7684\u542f\u53d1\uff0c\u6e29\u5dde\u533b\u79d1\u5927\u5b66\u7684\u8521\u4e91\u745e\u56e2\u961f\u6210\u529f\u8bbe\u8ba1\u51fa\u4e00\u79cd\u5168\u65b0\u7684\u901a\u8fc7TEMPO\u50ac\u5316\u5242\u4fc3\u8fdb\u7684\u91c7\u7528\u90bb\u6c28\u57fa\u82ef\u915a\u7c7b\u5e95\u7269\u53c2\u4e0e\u7684\u7535\u5316\u5b66\u53bb\u6c22\u73af\u7f29\u5408\u53cd\u5e94\u65b9\u6cd5\u5b66\uff0c\u8fdb\u800c\u987a\u5229\u5b8c\u6210\u4e00\u7cfb\u52172-\u6c28\u57fa\u5429\u5641\u55ea-3-\u916e\u7c7b\u5206\u5b50\u7684\u6784\u5efa (Scheme 1C)\u3002 \u9996\u5148\uff0c\u4f5c\u8005\u91c7\u7528\u90bb\u6c28\u57fa\u82ef\u915a1a\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\u7528TEMPO\u4f5c\u4e3a\u50ac\u5316\u5242\uff0cnBu4NBF4\u4f5c\u4e3a\u652f\u6301\u7535\u89e3\u8d28\uff0c\u5728\u65e0\u9694\u819c\u7535\u89e3\u69fd\u4e2d\uff0c\u91c7\u7528RVC (reticulated vitreous carbon)\u4f5c\u4e3a\u9633\u6781\uff0cPt\u677f (Pt plate)\u4f5c\u4e3a\u9634\u6781\uff0cDMF\u4f5c\u4e3a\u53cd\u5e94\u6eb6\u5242\uff0c\u53cd\u5e94\u6e29\u5ea6\u4e3a\u5ba4\u6e29\uff0c\u6700\u7ec8\u83b7\u5f9786%\u6536\u7387\u7684\u53bb\u6c22\u73af\u7f29\u5408\u4ea7\u72692a\u3002 \u540c\u65f6\uff0c\u4f5c\u8005\u901a\u8fc7\u76f8\u5173\u7684CV\u5b9e\u9a8c (Scheme 2A)\u7814\u7a76\u8868\u660e\uff0c\u4e0a\u8ff0\u7684\u7535\u5316\u5b66\u53bb\u6c22\u73af\u7f29\u5408\u8fc7\u7a0b\u4e2d\u53ef\u80fd\u6d89\u53caTEMPO+\u4e2d\u95f4\u4f53\u7684\u53c2\u4e0e\u3002\u4e4b\u540e\uff0c\u8be5\u5c0f\u7ec4\u901a\u8fc7\u4e00\u7cfb\u5217\u63a7\u5236\u5b9e\u9a8c (Scheme 2B)\u7684\u76f8\u5173\u7814\u7a76\u8fdb\u4e00\u6b65\u8bc1\u5b9e\uff0c\u53cd\u5e94\u8fc7\u7a0b\u4e2d\u6d89\u53ca\u81ea\u7531\u57fa\u4e2d\u95f4\u4f53\u7684\u53c2\u4e0e\u3002 \u57fa\u4e8e\u4e0a\u8ff0\u7684\u5b9e\u9a8c\u7814\u7a76\u4ee5\u53ca\u524d\u671f\u7684\u6587\u732e\u62a5\u9053[5]\uff0c\u4f5c\u8005\u63d0\u51fa\u5982\u4e0b\u5408\u7406\u7684\u53cd\u5e94\u673a\u7406 (Scheme 3)\u3002 \u4e4b\u540e\uff0c\u5728\u4e0a\u8ff0\u7684\u6700\u4f73\u53cd\u5e94\u6761\u4ef6\u4e0b\uff0c\u4f5c\u8005\u5bf9\u4e00\u7cfb\u5217\u90bb\u6c28\u57fa\u82ef\u915a\u5e95\u7269\u7684\u5e94\u7528\u8303\u56f4\u8fdb\u884c\u8003\u5bdf (Scheme 4)\u3002\u7814\u7a76\u8868\u660e\uff0c\u5728\u82ef\u73af\u7684C3-\u6216C6-\u4f4d\u7f6e\u5e26\u6709\u4e0d\u540c\u4f9b\u7535\u5b50\u4e0e\u5438\u7535\u5b50\u57fa\u56e2\u53d6\u4ee3\u7684\u90bb\u6c28\u57fa\u82ef\u915a\u5e95\u7269\uff0c\u5747\u80fd\u591f\u8f83\u597d\u5730\u4e0e\u4e0a\u8ff0\u7684\u6807\u51c6\u53cd\u5e94\u6761\u4ef6\u517c\u5bb9\uff0c\u5e76\u4ee5\u4e2d\u7b49\u81f3\u826f\u597d\u7684\u53cd\u5e94\u6536\u7387\uff0c\u83b7\u5f97\u76f8\u5e94\u7684\u53bb\u6c22\u73af\u7f29\u5408\u4ea7\u72692a–2h\u3002\u540c\u65f6\uff0c\u7814\u7a76\u53d1\u73b0\uff0c\u4e0a\u8ff0\u7684\u6700\u4f73\u53cd\u5e94\u6761\u4ef6\u5bf9\u4e8e\u5728\u82ef\u73af\u7684C4-\u6216C5-\u4f4d\u7f6e\u5e26\u6709\u5364\u7d20\u4ee5\u53ca\u78fa\u9178\u57fa\u79bb\u53bb\u57fa\u56e2\u7684\u90bb\u6c28\u57fa\u82ef\u915a\u5e95\u7269\u4ee5\u53ca\u5728\u82ef\u73af\u7684C5-\u4f4d\u7f6e\u5177\u6709\u7532\u57fa\u53d6\u4ee3\u7684\u90bb\u6c28\u57fa\u82ef\u915a\u5e95\u7269\uff0c\u540c\u6837\u80fd\u591f\u6709\u6548\u5730\u517c\u5bb9\u3002 \u540c\u65f6\uff0c\u4f5c\u8005\u8fdb\u4e00\u6b65\u7814\u7a76\u53d1\u73b0\uff0c\u4e0a\u8ff0\u7684\u7535\u5316\u5b66\u53bb\u6c22\u73af\u7f29\u5408\u7b56\u7565\u540c\u6837\u80fd\u591f\u6709\u6548\u5730\u5e94\u7528\u4e8e\u90bb\u82ef\u4e8c\u80fa (1p)\u4ee5\u53ca2-\u82ef\u57fa\u6c28\u57fa\u82ef\u80fa (1q)\u5e95\u7269 (Scheme 5)\u3002 \u7136\u800c\uff0c\u5bf9\u4e8e2-\u6c28\u57fa\u82ef\u786b\u9187(1r)\u30012-\u6c28\u57fa\u5421\u5576-3-\u9187(1s)\u30012-\u6c28\u57fa-3-\u785d\u57fa\u82ef\u915a(1t)\u4ee5\u53ca2-(\u7532\u6c28\u57fa)\u82ef\u915a(1u) \u5e95\u7269\uff0c\u5219\u5747\u672a\u80fd\u83b7\u5f97\u9884\u671f\u7684\u76ee\u6807\u4ea7\u7269 (ESI, Fig. S3-S6)\u3002 \u4e4b\u540e\uff0c\u8be5\u5c0f\u7ec4\u901a\u8fc7\u5982\u4e0b\u7684\u5b9e\u9a8c\u88c5\u7f6e\uff0c\u5bf9\u4e8e\u4e0a\u8ff0\u7684\u53bb\u6c22\u73af\u7f29\u5408\u7b56\u7565\u7684\u514b\u7ea7\u89c4\u6a21\u53cd\u5e94\u8fdb\u884c\u8fdb\u4e00\u6b65\u7814\u7a76\uff0c\u8fdb\u800c\u8868\u660e\uff0c\u8fd9\u4e00\u5168\u65b0\u7684\u53bb\u6c22\u73af\u7f29\u5408\u7b56\u7565\u5177\u6709\u6f5c\u5728\u7684\u5408\u6210\u5e94\u7528\u4ef7\u503c (Fig. S7)\u3002 \u540c\u65f6\uff0c\u8be5\u5c0f\u7ec4\u8fdb\u4e00\u6b65\u7814\u7a76\u53d1\u73b0\uff0c\u901a\u8fc7\u4e0a\u8ff0\u7684\u53bb\u6c22\u73af\u7f29\u5408\u7b56\u7565\u83b7\u5f97\u7684\u76ee\u6807\u4ea7\u72692h\u8868\u73b0\u51fa\u4f18\u826f\u7684\u6297\u80bf\u7624\u6d3b\u6027(Fig. 1)\u3002 \u603b\u7ed3 \u6e29\u5dde\u533b\u79d1\u5927\u5b66\u7684\u8521\u4e91\u745e\u8bfe\u9898\u7ec4\u6210\u529f\u8bbe\u8ba1\u51fa\u4e00\u79cd\u5168\u65b0\u7684\u91c7\u7528TEMPO\u50ac\u5316\u5242\u4fc3\u8fdb\u7684\u901a\u8fc7\u4e00\u7cfb\u5217\u90bb\u6c28\u57fa\u82ef\u915a\u7c7b\u5e95\u7269\u53c2\u4e0e\u7684\u7535\u5316\u5b66\u53bb\u6c22\u73af\u7f29\u5408\u53cd\u5e94\u65b9\u6cd5\u5b66\u3002\u8fd9\u4e00\u5168\u65b0\u7684\u7535\u5316\u5b66\u53bb\u6c22\u73af\u7f29\u5408\u53cd\u5e94\u7b56\u7565\u5177\u6709\u6e29\u548c\u7684\u53cd\u5e94\u6761\u4ef6\u3001\u65e0\u9700\u9009\u62e9\u5316\u5b66\u8ba1\u91cf\u7684\u6c27\u5316\u5242\u4ee5\u53ca\u50ac\u5316\u5242\u5ec9\u4ef7\u6613\u5f97\u4ee5\u53ca\u826f\u597d\u7684\u5408\u6210\u5e94\u7528\u4ef7\u503c\u7b49\u4f18\u52bf\u3002 \u53c2\u8003\u6587\u732e [1] S. Y. Jabri, L. E. Overman, J. Am. Chem. Soc. 2013, 135, 4231. doi: 10.1021\/ja401423j. [2] (a) F. Ferlin, P. M. L. Navarro, Y. Gu, D. Lanari, L. 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