{"id":28606,"date":"2019-08-27T08:00:47","date_gmt":"2019-08-27T00:00:47","guid":{"rendered":"\/\/www.gsbet888.com\/?p=28606"},"modified":"2019-08-26T18:00:03","modified_gmt":"2019-08-26T10:00:03","slug":"%e7%94%b2%e9%85%b0%e8%83%ba%e6%b4%bb%e5%8c%96%e7%be%a7%e9%85%b8-%e5%90%88%e6%88%90%e9%85%b0%e8%83%ba%e5%92%8c%e9%85%af%e7%9a%84%e5%ae%9e%e7%94%a8%e6%96%b9%e6%b3%95","status":"publish","type":"post","link":"\/\/www.gsbet888.com\/%e5%8c%96%e5%ad%a6%e6%9d%82%e8%ae%b0\/recentpaper\/2019\/08\/%e7%94%b2%e9%85%b0%e8%83%ba%e6%b4%bb%e5%8c%96%e7%be%a7%e9%85%b8-%e5%90%88%e6%88%90%e9%85%b0%e8%83%ba%e5%92%8c%e9%85%af%e7%9a%84%e5%ae%9e%e7%94%a8%e6%96%b9%e6%b3%95.html","title":{"rendered":"\u7532\u9170\u80fa\u6d3b\u5316\u7fa7\u9178–\u5408\u6210\u9170\u80fa\u548c\u916f\u7684\u5b9e\u7528\u65b9\u6cd5"},"content":{"rendered":"

\u672c\u6587\u4f5c\u8005 \u8283\u6d0b\u96ea<\/p>\n

\u7531\u7fa7\u9178\u5408\u6210\u9170\u80fa\u548c\u916f\uff0c\u662f\u6709\u673a\u5316\u5b66\u4e2d\u57fa\u672c\u4e5f\u662f\u91cd\u8981\u7684\u53cd\u5e94\u4e4b\u4e00\u3002\u916f\u952e\u548c\u9170\u80fa\u952e\u5e38\u89c1\u4e8e\u5404\u79cd\u5316\u5b66\u54c1\u79cd\uff0c\u9170\u80fa\u952e\u4e5f\u662f\u591a\u80bd\u548c\u86cb\u767d\u8d28\u7684\u4e3b\u8981\u5b98\u80fd\u56e2\uff0c\u5b83\u4eec\u7684\u5408\u6210\u4e5f\u5f88\u7b80\u5355\uff0c\u5927\u591a\u662f\u7531\u7fa7\u9178\u76f4\u63a5\u548cN-\u6216O-\u7684\u4eb2\u6838\u8bd5\u5242\u76f4\u63a5\u7f29\u5408\u5f97\u5230\uff0c\u5982scheme 1A\u6240\u793a\u3002\u4f46\u76f4\u63a5\u7531\u7fa7\u9178\u53bb\u8f6c\u5316\u8fd8\u662f\u6709\u4e9b\u56f0\u96be\uff0c\u4e00\u822c\u4f1a\u5c06\u7f9f\u57fa\u8f6c\u5316\u4e3a\u6613\u79bb\u53bb\u7684\u57fa\u56e2\uff0c\u4ee5\u5229\u4e8e\u4eb2\u6838\u8bd5\u5242\u7684\u53d6\u4ee3\uff0c\u4f46\u540c\u65f6\u4e5f\u751f\u6210\u4e86\u526f\u4ea7\u7269\u7b49\u5e9f\u5f03\u7269\uff0c\u4e0d\u5229\u4e8e\u73af\u4fdd\u53ca\u53ef\u6301\u7eed\u53d1\u5c55\u3002<\/p>\n

\"\"<\/p>\n

Scheme 1 \u4e4b\u524d\u548c\u73b0\u5728\u7684\u5de5\u4f5c<\/p>\n

\u8fd1\u5e74\u6765\uff0c\u4e5f\u6709\u7528\u787c\u3001\u94ea\u3001\u9506\u7b49\u8def\u6613\u65af\u9178\u50ac\u5316\u9170\u80fa\u7684\u5408\u6210\uff0c\u5982\u542b\u787c\u660e\u661f\u5206\u5b50dioxaazatriborinane\uff0c\u4e5f\u4f5c\u4e3a\u9170\u80fa\u5316\u53cd\u5e94\u7684\u6709\u673a\u50ac\u5316\u5242\u3002\u867d\u7136\u50ac\u5316C-N\u3001C-O\u952e\u5f62\u6210\u7684\u65b0\u8bd5\u5242\u5c42\u51fa\u4e0d\u7a77\uff0c\u4f46\u5728\u5927\u578b\u836f\u4f01\u4e2d\u4ecd\u7136\u6e34\u6c42\u9170\u80fa\u548c\u916f\u7684\u65b0\u5408\u6210\u65b9\u6cd5\u3002\u76ee\u524d\uff0c\u5316\u5b66\u8ba1\u91cf\u6d3b\u5316\u7fa7\u9178\u4e2d\u7f9f\u57fa\u7684\u8bd5\u5242\u5982\u56fe1B\u6240\u793a\uff0c\u5176\u4e2d\u4e09\u6c2f\u5f02\u6c30\u8132\u9178TCT\uff08<\/strong>trichlorotriazine\uff09\uff0c\u53c8\u79f0\u4e09\u805a\u6c2f\u6c30\u7684\u6210\u672c\u6700\u4e3a\u4f4e\u5ec9\uff0c\u5b83\u6709\u4e09\u4e2a\u6c2f\uff0c\u6240\u4ee5\u5bf9\u7f9f\u57fa\u7684\u5316\u5b66\u8ba1\u91cf\u6bd4\u4e3a3:1\uff0c\u800c\u4e14\u4e0d\u751f\u6210\u6c2f\u5316\u6c22\uff0c\u56e0\u6b64\u5316\u5b66\u517c\u5bb9\u6027\u66f4\u597d\u3002<\/p>\n

\"\"<\/p>\n

\u56fe1B \u5404\u79cd\u6d3b\u5316\u8bd5\u5242\u7684\u4ef7\u683c\u6bd4\u8f83<\/p>\n

33\uff5e40mol%\u7684TCT\u548cN-\u7532\u57fa\u5417\u5549NMM<\/strong>\uff08N-Methylmorpholine\uff09\u8054\u7528\u53ef\u4ee5\u5408\u6210\u9170\u80fa2<\/strong>\uff0c\u91cd\u6c2e\u916e4<\/strong>\u548c\u9170\u57fa\u53e0\u6c2e\u5316\u72695<\/strong>\uff0c\u4f46\u6536\u7387\u4e3a\u4e2d\u7b49\uff0c\u5982\u5408\u6210\u9170\u80fa\u7684\u6536\u7387\u4e3a65-75%\u3002\u540c\u65f6\uff0c\u4f5c\u8005\u53d1\u73b0\u5728\u8def\u6613\u65af\u78b1N-\u7532\u9170\u5421\u54af\u70f7FPyr \uff08N-formylpyrrolidine\uff09\u53ef\u4ee5\u4f5c\u4e3a\u5f3a\u6548\u7684\u8def\u6613\u65af\u78b1\u5728\u82ef\u7532\u9170\u6c2f\u6216TCT\u4f5c\u7528\u4e0b\u8f6c\u5316\u91877\u4e3a\u6c2f\u5316\u72698\uff0c\u5982scheme 1B\u6240\u793a\u3002<\/p>\n

\u7ed3\u5408\u8fd9\u4e9b\u80cc\u666f\u548c\u7ecf\u9a8c\uff0c\u6765\u81ea\u5fb7\u56fdSaarland University<\/strong>\u7684Peter Huy<\/strong>\u8bfe\u9898\u7ec4\uff0c\u5f00\u53d1\u4e86\u57fa\u4e8eTCT\u548c\u9170\u80fa\u4f5c\u7528\u4e0b\uff0c\u50ac\u5316\u9170\u80fa\u548c\u916f\u7684\u5408\u6210\uff0c\u5982scheme1C\u6240\u793a\u3002\u6d3b\u6027\u4e2d\u95f4\u4f53\u4e3a\u9170\u6c2f6\uff0c\u4f17\u6240\u5468\u77e5\uff0c\u5b83\u7684\u6d3b\u6027\u8981\u9ad8\u4e8e\u9178\u9150\uff0c\u56e0\u6b64\u53ef\u80fd\u5177\u6709\u66f4\u5e7f\u6cdb\u7684\u5e94\u7528\u548c\u66f4\u9ad8\u7684\u6536\u7387\u3002\u8bba\u6587<\/p>\n

Formamide catalyzed activation of carboxylic acids \u2013 versatile and cost-efficient amidation and esterification<\/p>\n

Chem. Sci<\/em>., 2019<\/strong>,10<\/em>, 7399-7406\uff0cDOI\uff1a 10.1039\/C9SC02126D<\/a><\/p>\n

Peter H. Huy and Christelle Mbouhoma<\/p><\/blockquote>\n

 <\/p>\n

\u53cd\u5e94\u6761\u4ef6\u4f18\u5316<\/strong><\/h4>\n

\u4ee5\u5bf9\u7532\u82ef\u78fa\u91781<\/strong>\u751f\u6210\u9170\u80fa2<\/strong>\u4e3a\u4f8b\uff0c\u8fdb\u884c\u53cd\u5e94\u6761\u4ef6\u7684\u6478\u7d22\uff0c\u7ed3\u679c\u5982\u88681\u6240\u793a\u3002\u5176\u4e2d\u5c3d\u7ba1\u4e59\u9178\u4e59\u916f\u7684\u6536\u7387\u4e5f\u8f83\u9ad8\uff0c\u4f46\u8fd8\u662f\u4ee5\u4e59\u8148\u4f5c\u4e3a\u4f18\u9009\u6eb6\u5242\u3002\u53cd\u5e94\u6e29\u5ea6\u8f83\u9ad8\u598280 o<\/sup>C\u65f6\uff0c\u53ef\u4ee5\u7f29\u77ed\u53cd\u5e94\u65f6\u95f4\u57284h\u4ee5\u5185\uff0c\u50ac\u5316\u5242FPyr\u7684\u7528\u91cf\u53ef\u4ee5\u4f4e\u81f35%\uff0c\u6216\u8005\u88ab\u4e24\u500d\u7684DMF\u53d6\u4ee3\u3002\u5bf9\u5e95\u7269\u800c\u8a00\uff0c\u8102\u80aa\u65cf\u6bd4\u82b3\u9999\u65cf\u66f4\u6d3b\u6cfc\uff0c40%\u7684TCT\u7528\u91cf\u662f\u5173\u952e\uff0c\u63d0\u9ad8\u7528\u91cf\u5982\u81f360%\u53cd\u800c\u964d\u4f4e\u4e86\u6536\u7387\u3002\u5c061<\/strong>\u8f6c\u5316\u4e3a\u9170\u6c2f6<\/strong>\u7684\u8fc7\u7a0b\u4e2d\uff0c\u4f17\u591a\u7684\u8def\u6613\u65af\u78b1\u4e2d\uff0c\u5982OPPh3<\/sub>\u3001DMSO\u3001tropon\u3001cyclopropenone\u73af\u7b49\uff0cFPyr\u6700\u6709\u6548\u3002\u4e0e\u7f9f\u57fa\u8f6c\u5316\u4e3a\u6c2f\u76f8\u6bd4\uff0c\u7fa7\u9178\u8f6c\u5316\u4e3a\u9170\u6c2f\u7684TCT\u7528\u91cf\u548c\u53cd\u5e94\u65f6\u95f4\u90fd\u6709\u6240\u589e\u52a0\uff0c\u9664\u6b64\u4e4b\u5916\uff0c\u6eb6\u5242\u7684\u7528\u91cf\uff0c\u5373\u6d53\u5ea6\u59821M\u4e5f\u662f\u653e\u5927\u548c\u53ef\u6301\u7eed\u6027\u751f\u4ea7\u7684\u5173\u952e\u56e0\u7d20\u3002<\/p>\n

\"\"<\/p>\n

\u88681 \u5408\u6210\u9170\u80fa21a<\/sub>\u7684\u5de5\u827a\u53c2\u6570\u4f18\u5316<\/p>\n

\u5408\u6210\u9170\u80fa<\/strong><\/h4>\n

\u7fa7\u9178\u7684\u5e95\u7269\u8303\u56f4\u5f88\u5e7f\uff0c\u591a\u79cd\u7ed3\u6784\u7684\u7fa7\u9178\u90fd\u53ef\u4ee5\u53cd\u5e94\uff0c\u5305\u62ec\u03b1\u78b3\u4e3a\u4f2f\u3001\u4ef2\u3001\u5b63\u78b3\u539f\u5b50,\u90fd\u53ef\u8f6c\u5316\u4e3a\u9170\u80fa.\uff08scheme 3B\uff09,\u4ee5\u53ca\u82b3\u9999\u65cf\uff083C\uff09\uff0c\u03b1,\u03b2-\u4e0d\u9971\u548c\u7fa7\u9178\uff083D\uff09\uff0c\u751f\u7269\u6d3b\u6027\u5206\u5b50moclobemide\u548cmodafinil\uff083F\uff09\uff0c\u517c\u5bb9\u591a\u79cd\u5b98\u80fd\u56e2\uff083E\uff09\u3002\u8fd9\u4e2a\u5408\u6210\u65b9\u6cd5\u53ef\u4ee5\u653e\u5927\u81f3500 mmol,\u6240\u7528\u7684\u73bb\u7483\u4eea\u5668\u22641L\u3002E-\u56e0\u5b50\u662f\u7eff\u8272\u5316\u5b66\u4e2d\u7684\u5e38\u7528\u6307\u6807\uff0c\u6307\u4ea7\u54c1\u548c\u540c\u65f6\u4ea7\u751f\u5e9f\u7269\u7684\u8d28\u91cf\u6bd4\uff0c\u672c\u6587\u5408\u6210\u9170\u80fa\u7684E-\u56e0\u5b50\u53ef\u4ee5\u4f4e\u81f33.5\u3002<\/p>\n

\"\"<\/p>\n

Scheme 3 \u5408\u62102\u7c7b\u578b\u7684\u9170\u80fa\u7ed3\u6784<\/p>\n

\u5408\u6210\u916f <\/strong><\/h4>\n

\u9187\u7684\u4eb2\u6838\u6027\u66f4\u5f31\uff0c\u56e0\u800c\u6311\u6218\u6027\u4e5f\u66f4\u5927\uff0c\u76ee\u524d\u5c11\u6709\u7528TCT\u5408\u6210\u916f\u7684\u62a5\u9053\u3002\u4f46\u5728\u8fd9\u4e2a\u53cd\u5e94\u6761\u4ef6\u4e0b\uff0c\u82b3\u9999\u65cf\u548c\u8102\u80aa\u65cf\u7684\u9187\u90fd\u53ef\u4ee5\u53cd\u5e94,\u6536\u7387\u572873-89%\uff0c\u5176\u4e2d\u4e5f\u5305\u62ec\u4e24\u4e2a3-5g\u89c4\u6a21\u7684\u5408\u6210\uff0c\u5373\u4f7f\u662f\u4f4d\u963b\u975e\u5e38\u5927\u7684\u9187\uff0c\u4e5f\u80fd\u8fbe\u523047-60%\u7684\u4e2d\u7b49\u6536\u7387\uff08scheme 5\uff09\u3002\u76f8\u6bd4\u6587\u732e\u62a5\u9053\u7684\u7c7b\u4f3c\u65b9\u6cd5\uff0c\u8fd9\u4e2a\u6761\u4ef6\u6536\u7387\u660e\u663e\u63d0\u9ad8\u3002<\/p>\n

\"\"<\/p>\n

\"\"<\/p>\n

\"\"<\/p>\n

Scheme 5 \u5408\u6210\u916f<\/p>\n

\u53cd\u5e94\u673a\u7406<\/strong><\/h4>\n

\u672c\u6587\u4e2d\uff0c\u4f5c\u8005\u63a8\u6d4b\u4e86\u53cd\u5e94\u7684\u673a\u7406\uff0c\u5173\u952e\u8fd8\u662f\u5f62\u6210\u6d3b\u6cfc\u7684\u9170\u6c2f\u3002\u53ef\u80fd\u673a\u7406\u4e3a\u7532\u9170\u80fa\u548cTCT\u901a\u8fc7\u7c7b\u4f3cSN<\/sub>Ar\u82b3\u9999\u4eb2\u6838\u53d6\u4ee3\u53cd\u5e94,\u751f\u6210\u5173\u952e\u7684\u6d3b\u6cfc\u4e2d\u95f4\u4f53\u2162<\/strong>\uff0c\u5b83\u7c7b\u4f3c\u4e8eVilsmeier-Haack\u8bd5\u5242\uff0c\u53d6\u4ee3\u5e95\u7269\u7fa7\u91781<\/strong>\u4e0a\u7684\u4e09\u5511\u90e8\u4f4d\u3002\u63a5\u4e0b\u6765\uff0c\u4e2d\u95f4\u4f53\u2163<\/strong>\u88ab\u6c2f\u53d6\u4ee3,\u751f\u6210\u9170\u6c2f6<\/strong>\u5e76\u91cd\u751fFPyr\u3002\u5c11\u4e00\u4e2a\u6c2f\u7684\u2164<\/strong>\u53ef\u4ee5\u518d\u8fdb\u884c\u4e24\u4e2a\u5faa\u73af\uff0c\u76f4\u5230\u6c2f\u90fd\u88ab\u7f9f\u57fa\u53d6\u4ee3\uff0c\u56e0\u6b6440 mol%\u7684TCT\u7528\u91cf\u76f8\u5f53\u4e8e1.2 eq\u3002\u4f5c\u8005\u66fe\u8bc1\u5b9e\u8fc7\u5173\u952e\u7684\u70f7\u6c27\u76d0\u2163<\/strong>\u4f5c\u4e3a\u5173\u952e\u4e2d\u95f4\u4f53,\u5982\u679c\u7f3a\u4e4fFPyr,\u82ef\u4e59\u9178\u4e0d\u80fd\u751f\u6210\u9170\u6c2f64<\/sub><\/strong>\u3002\u52a0\u5165\u5e38\u89c1\u7684Br\u00f8nsted\u9178\u82ef\u78fa\u9178\u4e5f\u4e0d\u80fd\u50ac\u5316\u82ef\u4e59\u9178\u751f\u6210\u9170\u6c2f\uff0c\u4f46\u78b1\u53ef\u4ee5\uff0c\u53ef\u4ee5\u6392\u9664Br\u00f8nsted \u9178\u5171\u50ac\u5316\u3002\u7528\u7ed3\u6784\u7c7b\u4f3c\u7684CDMT\u4ee3\u66ffTCT ,\u5e76\u6ca1\u6709\u751f\u6210\u9170\u6c2f\uff0c\u6240\u4ee5TCT\u4e2d\u7684\u6700\u540e\u4e00\u4e2a\u6c2f\u539f\u5b50\u7684\u53d6\u4ee3\uff0c\u5177\u4f53\u673a\u7406\u8fd8\u672a\u77e5\u3002\u8fd8\u6709\u503c\u5f97\u6ce8\u610f\uff0c14<\/sub><\/strong>\u5728CDCl3<\/sub>\u4e2d\uff0c\u6ca1\u6709\u751f\u6210\u9170\u6c2f\u800c\u662f\u751f\u6210\u4e8626%\u7684\u9178\u9150\uff0c\u53ef\u80fd\u8fd8\u6709\u5176\u4ed6\u673a\u7406\u89e3\u91ca\u3002<\/p>\n

\"\"<\/p>\n

\"\"<\/p>\n

Scheme 7 A\u673a\u7406\u63a8\u6d4b\u548cB-E\u5bf9\u6bd4\u5b9e\u9a8c<\/p>\n

\u603b\u7ed3<\/strong>\uff1a<\/h4>\n

\u4f5c\u8005\u5f00\u53d1\u4e86\u4f7f\u7528\u7684\u7532\u9170\u80fa\u50ac\u5316\u7684\u7fa7\u9178\u8f6c\u5316\u4e3a\u9170\u6c2f\u3001\u9170\u80fa\u3001\u916f\u548c\u786b\u916f\u7684\u5b9e\u7528\u65b9\u6cd5\uff0c\u6240\u7528\u7684TCT\u662f\u5ec9\u4ef7\u7684\u7f9f\u57fa\u6d3b\u5316\u8bd5\u5242\uff0c\u4e0e\u5149\u6c14\u7c7b\u4f3c\uff0c\u6469\u5c14\u7528\u91cf\u4e3a\u4ec540mol%\uff0c\u5177\u6709\u4ee5\u4e0b\u4f18\u70b9\uff1a\uff081\uff09\u8d39\u7528\u66f4\u7ecf\u6d4e\uff1b\uff082\uff09\u89c4\u6a21\u53ef\u4ee5\u653e\u5927\uff1b\uff083\uff09\u591a\u79cd\u5b98\u80fd\u56e2\u7684\u517c\u5bb9\u6027\uff1b\uff084\uff09\u4e09\u5e9f\u8f83\u5c11\uff0cE-\u56e0\u5b50\u57283\u4ee5\u4e0b\uff1b\uff085\uff09\u64cd\u4f5c\u7b80\u5355\uff0c\u4e0d\u9700\u989d\u5916\u7684\u5e72\u71e5\u3002\u5e76\u4e14\u4e0e\u5176\u4ed6\u4f7f\u7528TCT\u7684\u65b9\u6cd5\u76f8\u6bd4\uff0c\u672c\u6587\u5927\u5e45\u63d0\u9ad8\u4e86\u6536\u7387\u3002\u4ee5\u540e\u9047\u5230\u5408\u6210\u9170\u80fa\u6216\u916f\u7684\u53cd\u5e94\uff0c\u53ef\u4ee5\u8bd5\u8bd5\u672c\u6587\u7684\u53cd\u5e94\u6761\u4ef6\u3002<\/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 \u8283\u6d0b\u96ea \u7531\u7fa7\u9178\u5408\u6210\u9170\u80fa\u548c\u916f\uff0c\u662f\u6709\u673a\u5316\u5b66\u4e2d\u57fa\u672c\u4e5f\u662f\u91cd\u8981\u7684\u53cd\u5e94\u4e4b\u4e00\u3002\u916f\u952e\u548c\u9170\u80fa\u952e\u5e38\u89c1\u4e8e\u5404\u79cd\u5316\u5b66\u54c1\u79cd\uff0c\u9170\u80fa\u952e\u4e5f\u662f\u591a\u80bd\u548c\u86cb\u767d\u8d28\u7684\u4e3b\u8981\u5b98\u80fd\u56e2\uff0c\u5b83\u4eec\u7684\u5408\u6210\u4e5f\u5f88\u7b80\u5355\uff0c\u5927\u591a\u662f\u7531\u7fa7\u9178\u76f4\u63a5\u548cN-\u6216O-\u7684\u4eb2\u6838\u8bd5\u5242\u76f4\u63a5\u7f29\u5408\u5f97\u5230\uff0c\u5982scheme 1A\u6240\u793a\u3002\u4f46\u76f4\u63a5\u7531\u7fa7\u9178\u53bb\u8f6c\u5316\u8fd8\u662f\u6709\u4e9b\u56f0\u96be\uff0c\u4e00\u822c\u4f1a\u5c06\u7f9f\u57fa\u8f6c\u5316\u4e3a\u6613\u79bb\u53bb\u7684\u57fa\u56e2\uff0c\u4ee5\u5229\u4e8e\u4eb2\u6838\u8bd5\u5242\u7684\u53d6\u4ee3\uff0c\u4f46\u540c\u65f6\u4e5f\u751f\u6210\u4e86\u526f\u4ea7\u7269\u7b49\u5e9f\u5f03\u7269\uff0c\u4e0d\u5229\u4e8e\u73af\u4fdd\u53ca\u53ef\u6301\u7eed\u53d1\u5c55\u3002 Scheme 1 \u4e4b\u524d\u548c\u73b0\u5728\u7684\u5de5\u4f5c \u8fd1\u5e74\u6765\uff0c\u4e5f\u6709\u7528\u787c\u3001\u94ea\u3001\u9506\u7b49\u8def\u6613\u65af\u9178\u50ac\u5316\u9170\u80fa\u7684\u5408\u6210\uff0c\u5982\u542b\u787c\u660e\u661f\u5206\u5b50dioxaazatriborinane\uff0c\u4e5f\u4f5c\u4e3a\u9170\u80fa\u5316\u53cd\u5e94\u7684\u6709\u673a\u50ac\u5316\u5242\u3002\u867d\u7136\u50ac\u5316C-N\u3001C-O\u952e\u5f62\u6210\u7684\u65b0\u8bd5\u5242\u5c42\u51fa\u4e0d\u7a77\uff0c\u4f46\u5728\u5927\u578b\u836f\u4f01\u4e2d\u4ecd\u7136\u6e34\u6c42\u9170\u80fa\u548c\u916f\u7684\u65b0\u5408\u6210\u65b9\u6cd5\u3002\u76ee\u524d\uff0c\u5316\u5b66\u8ba1\u91cf\u6d3b\u5316\u7fa7\u9178\u4e2d\u7f9f\u57fa\u7684\u8bd5\u5242\u5982\u56fe1B\u6240\u793a\uff0c\u5176\u4e2d\u4e09\u6c2f\u5f02\u6c30\u8132\u9178TCT\uff08trichlorotriazine\uff09\uff0c\u53c8\u79f0\u4e09\u805a\u6c2f\u6c30\u7684\u6210\u672c\u6700\u4e3a\u4f4e\u5ec9\uff0c\u5b83\u6709\u4e09\u4e2a\u6c2f\uff0c\u6240\u4ee5\u5bf9\u7f9f\u57fa\u7684\u5316\u5b66\u8ba1\u91cf\u6bd4\u4e3a3:1\uff0c\u800c\u4e14\u4e0d\u751f\u6210\u6c2f\u5316\u6c22\uff0c\u56e0\u6b64\u5316\u5b66\u517c\u5bb9\u6027\u66f4\u597d\u3002 \u56fe1B \u5404\u79cd\u6d3b\u5316\u8bd5\u5242\u7684\u4ef7\u683c\u6bd4\u8f83 33\uff5e40mol%\u7684TCT\u548cN-\u7532\u57fa\u5417\u5549NMM\uff08N-Methylmorpholine\uff09\u8054\u7528\u53ef\u4ee5\u5408\u6210\u9170\u80fa2\uff0c\u91cd\u6c2e\u916e4\u548c\u9170\u57fa\u53e0\u6c2e\u5316\u72695\uff0c\u4f46\u6536\u7387\u4e3a\u4e2d\u7b49\uff0c\u5982\u5408\u6210\u9170\u80fa\u7684\u6536\u7387\u4e3a65-75%\u3002\u540c\u65f6\uff0c\u4f5c\u8005\u53d1\u73b0\u5728\u8def\u6613\u65af\u78b1N-\u7532\u9170\u5421\u54af\u70f7FPyr \uff08N-formylpyrrolidine\uff09\u53ef\u4ee5\u4f5c\u4e3a\u5f3a\u6548\u7684\u8def\u6613\u65af\u78b1\u5728\u82ef\u7532\u9170\u6c2f\u6216TCT\u4f5c\u7528\u4e0b\u8f6c\u5316\u91877\u4e3a\u6c2f\u5316\u72698\uff0c\u5982scheme 1B\u6240\u793a\u3002 \u7ed3\u5408\u8fd9\u4e9b\u80cc\u666f\u548c\u7ecf\u9a8c\uff0c\u6765\u81ea\u5fb7\u56fdSaarland University\u7684Peter Huy\u8bfe\u9898\u7ec4\uff0c\u5f00\u53d1\u4e86\u57fa\u4e8eTCT\u548c\u9170\u80fa\u4f5c\u7528\u4e0b\uff0c\u50ac\u5316\u9170\u80fa\u548c\u916f\u7684\u5408\u6210\uff0c\u5982scheme1C\u6240\u793a\u3002\u6d3b\u6027\u4e2d\u95f4\u4f53\u4e3a\u9170\u6c2f6\uff0c\u4f17\u6240\u5468\u77e5\uff0c\u5b83\u7684\u6d3b\u6027\u8981\u9ad8\u4e8e\u9178\u9150\uff0c\u56e0\u6b64\u53ef\u80fd\u5177\u6709\u66f4\u5e7f\u6cdb\u7684\u5e94\u7528\u548c\u66f4\u9ad8\u7684\u6536\u7387\u3002\u8bba\u6587 Formamide catalyzed activation of carboxylic acids \u2013 versatile and cost-efficient amidation and esterification Chem. Sci., 2019,10, 7399-7406\uff0cDOI\uff1a 10.1039\/C9SC02126D Peter H. Huy and Christelle Mbouhoma   \u53cd\u5e94\u6761\u4ef6\u4f18\u5316 \u4ee5\u5bf9\u7532\u82ef\u78fa\u91781\u751f\u6210\u9170\u80fa2\u4e3a\u4f8b\uff0c\u8fdb\u884c\u53cd\u5e94\u6761\u4ef6\u7684\u6478\u7d22\uff0c\u7ed3\u679c\u5982\u88681\u6240\u793a\u3002\u5176\u4e2d\u5c3d\u7ba1\u4e59\u9178\u4e59\u916f\u7684\u6536\u7387\u4e5f\u8f83\u9ad8\uff0c\u4f46\u8fd8\u662f\u4ee5\u4e59\u8148\u4f5c\u4e3a\u4f18\u9009\u6eb6\u5242\u3002\u53cd\u5e94\u6e29\u5ea6\u8f83\u9ad8\u598280 oC\u65f6\uff0c\u53ef\u4ee5\u7f29\u77ed\u53cd\u5e94\u65f6\u95f4\u57284h\u4ee5\u5185\uff0c\u50ac\u5316\u5242FPyr\u7684\u7528\u91cf\u53ef\u4ee5\u4f4e\u81f35%\uff0c\u6216\u8005\u88ab\u4e24\u500d\u7684DMF\u53d6\u4ee3\u3002\u5bf9\u5e95\u7269\u800c\u8a00\uff0c\u8102\u80aa\u65cf\u6bd4\u82b3\u9999\u65cf\u66f4\u6d3b\u6cfc\uff0c40%\u7684TCT\u7528\u91cf\u662f\u5173\u952e\uff0c\u63d0\u9ad8\u7528\u91cf\u5982\u81f360%\u53cd\u800c\u964d\u4f4e\u4e86\u6536\u7387\u3002\u5c061\u8f6c\u5316\u4e3a\u9170\u6c2f6\u7684\u8fc7\u7a0b\u4e2d\uff0c\u4f17\u591a\u7684\u8def\u6613\u65af\u78b1\u4e2d\uff0c\u5982OPPh3\u3001DMSO\u3001tropon\u3001cyclopropenone\u73af\u7b49\uff0cFPyr\u6700\u6709\u6548\u3002\u4e0e\u7f9f\u57fa\u8f6c\u5316\u4e3a\u6c2f\u76f8\u6bd4\uff0c\u7fa7\u9178\u8f6c\u5316\u4e3a\u9170\u6c2f\u7684TCT\u7528\u91cf\u548c\u53cd\u5e94\u65f6\u95f4\u90fd\u6709\u6240\u589e\u52a0\uff0c\u9664\u6b64\u4e4b\u5916\uff0c\u6eb6\u5242\u7684\u7528\u91cf\uff0c\u5373\u6d53\u5ea6\u59821M\u4e5f\u662f\u653e\u5927\u548c\u53ef\u6301\u7eed\u6027\u751f\u4ea7\u7684\u5173\u952e\u56e0\u7d20\u3002 \u88681 \u5408\u6210\u9170\u80fa21a\u7684\u5de5\u827a\u53c2\u6570\u4f18\u5316 \u5408\u6210\u9170\u80fa \u7fa7\u9178\u7684\u5e95\u7269\u8303\u56f4\u5f88\u5e7f\uff0c\u591a\u79cd\u7ed3\u6784\u7684\u7fa7\u9178\u90fd\u53ef\u4ee5\u53cd\u5e94\uff0c\u5305\u62ec\u03b1\u78b3\u4e3a\u4f2f\u3001\u4ef2\u3001\u5b63\u78b3\u539f\u5b50,\u90fd\u53ef\u8f6c\u5316\u4e3a\u9170\u80fa.\uff08scheme 3B\uff09,\u4ee5\u53ca\u82b3\u9999\u65cf\uff083C\uff09\uff0c\u03b1,\u03b2-\u4e0d\u9971\u548c\u7fa7\u9178\uff083D\uff09\uff0c\u751f\u7269\u6d3b\u6027\u5206\u5b50moclobemide\u548cmodafinil\uff083F\uff09\uff0c\u517c\u5bb9\u591a\u79cd\u5b98\u80fd\u56e2\uff083E\uff09\u3002\u8fd9\u4e2a\u5408\u6210\u65b9\u6cd5\u53ef\u4ee5\u653e\u5927\u81f3500 mmol,\u6240\u7528\u7684\u73bb\u7483\u4eea\u5668\u22641L\u3002E-\u56e0\u5b50\u662f\u7eff\u8272\u5316\u5b66\u4e2d\u7684\u5e38\u7528\u6307\u6807\uff0c\u6307\u4ea7\u54c1\u548c\u540c\u65f6\u4ea7\u751f\u5e9f\u7269\u7684\u8d28\u91cf\u6bd4\uff0c\u672c\u6587\u5408\u6210\u9170\u80fa\u7684E-\u56e0\u5b50\u53ef\u4ee5\u4f4e\u81f33.5\u3002 Scheme 3 \u5408\u62102\u7c7b\u578b\u7684\u9170\u80fa\u7ed3\u6784 \u5408\u6210\u916f \u9187\u7684\u4eb2\u6838\u6027\u66f4\u5f31\uff0c\u56e0\u800c\u6311\u6218\u6027\u4e5f\u66f4\u5927\uff0c\u76ee\u524d\u5c11\u6709\u7528TCT\u5408\u6210\u916f\u7684\u62a5\u9053\u3002\u4f46\u5728\u8fd9\u4e2a\u53cd\u5e94\u6761\u4ef6\u4e0b\uff0c\u82b3\u9999\u65cf\u548c\u8102\u80aa\u65cf\u7684\u9187\u90fd\u53ef\u4ee5\u53cd\u5e94,\u6536\u7387\u572873-89%\uff0c\u5176\u4e2d\u4e5f\u5305\u62ec\u4e24\u4e2a3-5g\u89c4\u6a21\u7684\u5408\u6210\uff0c\u5373\u4f7f\u662f\u4f4d\u963b\u975e\u5e38\u5927\u7684\u9187\uff0c\u4e5f\u80fd\u8fbe\u523047-60%\u7684\u4e2d\u7b49\u6536\u7387\uff08scheme 5\uff09\u3002\u76f8\u6bd4\u6587\u732e\u62a5\u9053\u7684\u7c7b\u4f3c\u65b9\u6cd5\uff0c\u8fd9\u4e2a\u6761\u4ef6\u6536\u7387\u660e\u663e\u63d0\u9ad8\u3002 Scheme 5 \u5408\u6210\u916f \u53cd\u5e94\u673a\u7406 \u672c\u6587\u4e2d\uff0c\u4f5c\u8005\u63a8\u6d4b\u4e86\u53cd\u5e94\u7684\u673a\u7406\uff0c\u5173\u952e\u8fd8\u662f\u5f62\u6210\u6d3b\u6cfc\u7684\u9170\u6c2f\u3002\u53ef\u80fd\u673a\u7406\u4e3a\u7532\u9170\u80fa\u548cTCT\u901a\u8fc7\u7c7b\u4f3cSNAr\u82b3\u9999\u4eb2\u6838\u53d6\u4ee3\u53cd\u5e94,\u751f\u6210\u5173\u952e\u7684\u6d3b\u6cfc\u4e2d\u95f4\u4f53\u2162\uff0c\u5b83\u7c7b\u4f3c\u4e8eVilsmeier-Haack\u8bd5\u5242\uff0c\u53d6\u4ee3\u5e95\u7269\u7fa7\u91781\u4e0a\u7684\u4e09\u5511\u90e8\u4f4d\u3002\u63a5\u4e0b\u6765\uff0c\u4e2d\u95f4\u4f53\u2163\u88ab\u6c2f\u53d6\u4ee3,\u751f\u6210\u9170\u6c2f6\u5e76\u91cd\u751fFPyr\u3002\u5c11\u4e00\u4e2a\u6c2f\u7684\u2164\u53ef\u4ee5\u518d\u8fdb\u884c\u4e24\u4e2a\u5faa\u73af\uff0c\u76f4\u5230\u6c2f\u90fd\u88ab\u7f9f\u57fa\u53d6\u4ee3\uff0c\u56e0\u6b6440 mol%\u7684TCT\u7528\u91cf\u76f8\u5f53\u4e8e1.2 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