{"id":12959,"date":"2017-02-02T07:20:14","date_gmt":"2017-02-01T23:20:14","guid":{"rendered":"\/\/www.gsbet888.com\/?p=12959"},"modified":"2019-08-02T18:53:35","modified_gmt":"2019-08-02T10:53:35","slug":"c%ce%b1-%e5%a4%a7%e4%bd%8d%e9%98%bb%e4%b8%8e%e7%bc%ba%e7%94%b5%e5%ad%90%e9%85%b0%e8%83%ba%e7%9a%84%e5%90%88%e6%88%90","status":"publish","type":"post","link":"\/\/www.gsbet888.com\/%e5%8c%96%e5%ad%a6%e6%9d%82%e8%ae%b0\/recentpaper\/2017\/02\/c%ce%b1-%e5%a4%a7%e4%bd%8d%e9%98%bb%e4%b8%8e%e7%bc%ba%e7%94%b5%e5%ad%90%e9%85%b0%e8%83%ba%e7%9a%84%e5%90%88%e6%88%90.html","title":{"rendered":"C\u03b1-\u5927\u4f4d\u963b\u4e0e\u7f3a\u7535\u5b50\u9170\u80fa\u7684\u5408\u6210"},"content":{"rendered":"

\u9170\u80fa\u952e\u662f\u4e00\u7c7b\u91cd\u8981\u7684\u5b98\u80fd\u56e2\uff0c\u4e0d\u4ec5\u5e7f\u6cdb\u5b58\u5728\u4e8e\u533b\u836f\u4e2d\u95f4\u4f53\uff0c\u6d3b\u6027\u5929\u7136\u4ea7\u7269\u4ee5\u53ca\u529f\u80fd\u6750\u6599\u5206\u5b50\u7684\u7ed3\u6784\u4e4b\u4e2d\uff0c\u800c\u4e14\u4e5f\u662f\u86cb\u767d\u8d28\u7ed3\u6784\u4e2d\u7684\u91cd\u8981\u5316\u5b66\u7ebd\u5e26\u3002\u9170\u80fa\u952e\u7684\u6784\u7b51\u4e00\u76f4\u662f\u65b9\u6cd5\u5b66\u7814\u7a76\u7684\u6d3b\u8dc3\u9886\u57df\uff0c\u4f20\u7edf\u7684\u9170\u80fa\u952e\u7684\u5408\u6210\u65b9\u6cd5\u4e3b\u8981\u6d89\u53ca\u5230\u7fa7\u9178\u7684\u6d3b\u5316\uff0c\u5c06\u5176\u8f6c\u5316\u4e3a\u9170\u5364\uff0c\u9178\u9150\u7b49\u884d\u751f\u7269\u540e\u518d\u4e0e\u80fa\u7247\u6bb5\u53cd\u5e94\uff0c\u6216\u8005\u5229\u7528\u5404\u7c7b\u7f29\u5408\u5242\u4fc3\u8fdb\u7fa7\u9178\u4e0e\u80fa\u7684\u7f29\u5408\uff0c\u6b64\u5916\uff0c\u8fd1\u5e74\u6765\u8fd8\u9646\u7eed\u62a5\u9053\u4e86\u8bf8\u5982\u82b3\u5364\u4e0e\u80fa\u5728\u91d1\u5c5e\u50ac\u5316\u4e0b\u6784\u5efa\u9170\u80fa\u952e\u7b49\u65b0\u7684\u7b56\u7565\u3002<\/p>\n

\u9170\u80fa\u5408\u6210\u7814\u7a76\u80cc\u666f\u53ca\u610f\u4e49<\/h4>\n

\u9170\u80fa\u7684\u5408\u6210\u5728\u836f\u7269\u5316\u5b66\u7814\u7a76\u4e2d\u66f4\u662f\u5360\u6709\u4e3e\u8db3\u8f7b\u91cd\u7684\u5730\u4f4d\uff0c\u8fd1\u51e0\u5e74\u591a\u7bc7\u5bf9\u4e8e\u836f\u5316\u9886\u57df\u7684\u5927\u6570\u636e\u5206\u6790\u8bba\u6587\u90fd\u6beb\u65e0\u4f8b\u5916\u5730\u53cd\u6620\u4e86\u8fd9\u4e00\u70b9\u3002\u6bd4\u5982\u4ece2016\u5e74AstraZeneca\u7684Brown\u7b49[1]<\/sup>\u5bf92014\u5e74\u4ee5\u53ca1984\u5e74\u4e24\u5e74\u4e2d\u836f\u5316\u9886\u57df\u6700\u5e38\u4f7f\u7528\u7684\u5408\u6210\u53cd\u5e94\u8fdb\u884c\u7684\u5206\u6790\u4e2d\u53ef\u4ee5\u53d1\u73b0\uff0c\u51e0\u4e4e\u540c\u4e09\u5341\u5e74\u524d\u7684\u60c5\u51b5\u76f8\u5dee\u65e0\u51e0\uff0c\u6d89\u53ca\u9170\u80fa\u5408\u6210\u7684\u53cd\u5e94\u5728\u7ed3\u679c\u4e2d\u4f4d\u5217\u524d\u8305\u3002\uff08\u89c1Figure 1.\uff09<\/p>\n

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

Figure 1.<\/p>\n

\u00a0 2016\u5e74\uff0cGilead\u548cPfizer\u7684\u5de5\u827a\u7814\u7a76\u4eba\u5458\u5171\u540c\u5728OPRD\u4e0a\u53d1\u8868\u4e86\u5173\u4e8e\u9178\u4e0e\u80fa\u53cd\u5e94\u751f\u6210\u9170\u80fa\u7684\u7efc\u8ff0\uff0c[2]<\/sup>\u4e0e\u4e4b\u524d\u5176\u4ed6\u5df2\u7ecf\u53d1\u8868\u7684\u5404\u7c7b\u7efc\u8ff0\u76f8\u6bd4\uff0c\u8be5\u6587\u7684\u7279\u8272\u662f\u6240\u5176\u8bc4\u8ff0\u53cd\u5e94\u7684\u89c4\u6a21\u5747\u8fbe\u5230100 mmol\u4ee5\u4e0a\u7684\u53cd\u5e94\u91cf\uff0c\u53ef\u4ee5\u8bf4\u8fd9\u7bc7\u7efc\u8ff0\u662f\u76ee\u524d\u5173\u4e8e\u5b9e\u9a8c\u5ba4\u6216\u8005\u5de5\u4e1a\u4e2d\u5927\u91cf\u5236\u5907\u9170\u80fa\u65b9\u6cd5\u7684\u6700\u6709\u4ef7\u503c\u7684\u53c2\u8003\u6587\u732e\u3002\u6587\u4e2d\u5217\u51fa\u4f4d\u4e8e\u7edf\u8ba1\u524d\u5217\u7684SOCl2<\/sub>\uff0c(COCl)2<\/sub>\uff0cEDCI, CDI\u7b49\u4f5c\u4e3a\u6d3b\u5316\u8bd5\u5242\u7684\u53cd\u5e94\u53ef\u4ee5\u8bf4\u662f\u5f53\u524d\u5bf9\u4e8e\u9170\u80fa\u5408\u6210\u6700\u4e3a\u7ecf\u5178\u4ee5\u53ca\u53ef\u9760\u7684\u5b9e\u9a8c\u65b9\u6cd5\u3002\uff08\u89c1Figure 2.\uff09<\/p>\n

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

Figure 2.<\/p>\n

\u9170\u80fa\u5408\u6210\u9762\u4e34\u7684\u56f0\u96be\u6311\u6218<\/h4>\n

\u867d\u7136\u5316\u5b66\u5bb6\u5bf9\u4e8e\u9170\u80fa\u7684\u5408\u6210\u65b9\u6cd5\u5df2\u7ecf\u6709\u4e86\u76f8\u5f53\u6570\u91cf\u7684\u9009\u62e9\u7a7a\u95f4\u5e76\u4e14\u79ef\u7d2f\u4e86\u8db3\u591f\u7684\u7ecf\u9a8c\uff0c\u4f46\u662f\u4ecd\u7136\u7ecf\u5e38\u4f1a\u5728\u7814\u7a76\u8fc7\u7a0b\u4e2d\u51fa\u73b0\u76ee\u6807\u9170\u80fa\u7684\u5408\u6210\u53d7\u963b\u6216\u8005\u4e0d\u5982\u9884\u671f\u6548\u679c\u7684\u60c5\u51b5\u3002\u5f88\u591a\u65f6\u5019\u8fd9\u79cd\u56f0\u96be\u5728\u4e8b\u5148\u5e76\u4e0d\u4f1a\u88ab\u5145\u5206\u4f30\u8ba1\u5230\uff0c\u8fd9\u4e5f\u5c31\u662f\u4e3a\u4f55\u8bb8\u591a\u7814\u7a76\u4eba\u5458\u5728\u6587\u7ae0\u4e2d\u5199\u5230\u6b64\u5904\u65f6\u90fd\u4f1a\u5982\u6b64\u63cf\u8ff0\u2014\u2014\u201cThis seemingly trivial transformation to produce XXX was plagued with poor isolated yields or low conversions\u201d\u2014\u2014\u81f3\u5c11\u8bf4\u660e\u5728\u8d77\u521d\u8bbe\u8ba1\u65f6\uff0c\u9170\u80fa\u7684\u5408\u6210\u5728\u5927\u90e8\u5206\u7814\u7a76\u8005\u770b\u6765\u662f\u5b8c\u5168\u4e0d\u4f1a\u6709\u95ee\u9898\u7684\u3002\u6839\u636e\u5df2\u6709\u6587\u732e\u7684\u62a5\u9053\u4ee5\u53ca\u5c0f\u7f16\u672c\u4eba\u5728\u79d1\u7814\u4e2d\u7684\u4f53\u4f1a\uff0c\u53d1\u73b0\u5728\u9170\u80fa\uff08\u6216\u591a\u80bd\uff09\u7684\u5236\u5907\u4e2d\uff0c\u9664\u4e86\u5bf9\u4e8e\u624b\u6027\u5e95\u7269\u7f29\u5408\u65f6\u5bb9\u6613\u53d1\u751f\u6d88\u65cb\u5316\u8fd9\u4e2a\u95ee\u9898\u4e4b\u5916\uff0c\u51fa\u73b0\u610f\u5916\u9891\u7387\u6700\u9ad8\u7684\u662f\u6709C\u03b1<\/sup>\u4f4d\u5b58\u5728\u5927\u4f4d\u963b\u7fa7\u9178\u4ee5\u53ca\u7f3a\u7535\u5b50\u82b3\u80fa\u53c2\u4e0e\u7684\u9170\u80fa\u5408\u6210\u53cd\u5e94\u3002\u4e0b\u9762\uff0c\u5c0f\u7f16\u5c31\u5c06\u4ece\u8fd1\u5e74\u6765\u7684\u51e0\u7bc7\u6587\u732e\u5165\u624b\uff0c\u7ed3\u5408\u5176\u4e2d\u7684\u7814\u7a76\u5b9e\u4f8b\uff0c\u6765\u8c08\u8c08\u5982\u4f55\u89e3\u51b3\u8fd9\u4e2a\u95ee\u9898\uff0c\u4e5f\u5e0c\u671b\u6587\u732e\u4e2d\u63d0\u4f9b\u7684\u601d\u8def\u80fd\u5bf9\u5927\u5bb6\u81ea\u5df1\u7684\u8bfe\u9898\u6709\u6240\u501f\u9274\u3002<\/p>\n

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

Scheme 1.<\/p>\n

\u7814\u7a76\u5b9e\u4f8b<\/h4>\n

2004\u5e74\uff0cDake\u7b49[3]<\/sup>\u5728\u5bf9Nitiol\u7684\u5168\u5408\u6210\u7814\u7a76\u4e2d\u9700\u8981\u5408\u6210Weinreb\u9170\u80fa1<\/strong>\u4f5c\u4e3a\u5176\u4e2d\u4e00\u4e2a\u4e2d\u95f4\u4f53\u4ee5\u4fbf\u4e0b\u4e00\u6b65\u7684\u7814\u7a76\uff0c\u7136\u800c\u5728\u5408\u6210\u4e2d\u53d1\u73b0\u65e0\u8bba\u662f\u4ee5\u7fa7\u91782<\/strong>\u8fd8\u662f\u7532\u916f3<\/strong>\u4e3a\u524d\u4f53\u53c2\u8003\u5df2\u6709\u6587\u732e\u8fdb\u884c\u8f6c\u5316\uff08\u89c1Scheme 1.\uff09\uff0c\u539f\u6599\u6216\u662f\u4e0d\u53cd\u5e94\u6216\u662f\u53ea\u5f97\u5230\u4f4e\u6536\u7387\u7684\u4ea7\u7269\u4ee5\u53ca\u6df7\u5408\u7269\uff0c\u53cd\u5e94\u7ed3\u679c\u4e0d\u4ee4\u4eba\u6ee1\u610f\u3002\u4f5c\u8005\u63a8\u6d4b\u5e94\u8be5\u662f\u7fa7\u57fa\u5468\u56f4\u5e9e\u5927\u7684\u7a7a\u95f4\u4f4d\u963b\u5bfc\u81f4\u4e86\u8be5\u95ee\u9898\u3002\u901a\u8fc7\u8c03\u7814\u6587\u732e\uff0c\u4f5c\u8005\u9009\u62e9\u4e86MsCl\u548cTEA\u4e3a\u53cd\u5e94\u6761\u4ef6\uff0c\u901a\u8fc7\u4e0e\u5e95\u7269\u7fa7\u9178\u5f62\u6210\u6df7\u5408\u9178\u9150\u6765\u8fbe\u5230\u6d3b\u5316\u7684\u76ee\u7684\u3002\u572850 mg\u5c0f\u8bd5\u89c4\u6a21\u53cd\u5e94\u83b7\u5f97\u4e8680 %\u6536\u7387\u7684\u826f\u597d\u7ed3\u679c\uff0c\u800c\u76f4\u63a5\u4ee5\u5c0f\u8bd5\u6761\u4ef6\u653e\u5927\u5230\u514b\u7ea7\u89c4\u6a21\u65f6\uff0c\u7531\u4e8ePMB\u4fdd\u62a4\u57fa\u8131\u9664\u5f15\u8d77\u7684\u526f\u53cd\u5e94\u4f7f\u6536\u7387\u964d\u4f4e\u4e3a55 %\u3002\u7ecf\u8fc7\u4f18\u5316MsCl\u4e0e\u78b1\u7684\u6bd4\u4f8b\uff0c\u8be5\u53cd\u5e94\u57281 g\u89c4\u6a21\u7684\u6536\u7387\u987a\u5229\u8fbe\u523080 %\u3002<\/p>\n

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

Scheme 2.<\/p>\n

\u00a0 \u5c06\u4f18\u5316\u540e\u7684\u53cd\u5e94\u6761\u4ef6\uff08\u89c1Scheme 2\uff09\u5e94\u7528\u4e8e\u5176\u4ed6\u7acb\u4f53\u969c\u788d\u578b\u7fa7\u9178\u5e95\u72694<\/strong>\u6240\u5bf9\u5e94\u7684Weinreb\u9170\u80fa5<\/strong>\u7684\u5408\u6210\uff0c\u5747\u83b7\u5f97\u4e86\u4e2d\u7b49\u81f3\u826f\u597d\u7684\u5206\u79bb\u6536\u7387\uff08\u89c1Table 1\uff09\u3002\u603b\u7684\u6765\u8bf4\uff0c\u6b64\u65b9\u6cd5\u5bf9\u4e8e\u82b3\u9999\u6216\u662f\u8102\u80aa\u7c7b\u7fa7\u9178\u5e95\u7269\u6709\u826f\u597d\u7684\u9002\u5e94\u6027\uff0c\u540c\u65f6\uff0c\u8db3\u591f\u6e29\u548c\u7684\u53cd\u5e94\u6761\u4ef6\u4f7f\u5f97\u624b\u6027\u5e95\u7269\u5e76\u672a\u53d1\u751f\u5dee\u5411\u5f02\u6784\u5316\u3002\u4e0d\u8fc7\uff0c\u9700\u8981\u6307\u51fa\u7684\u662f\uff0c\u8be5\u65b9\u6cd5\u5408\u6210Weinreb\u9170\u80fa\u8fc7\u7a0b\u4e2d\u5bb9\u6613\u5f62\u6210N<\/em>-\u7532\u6c27\u57fa-N<\/em>-\u7532\u57fa\u7532\u78fa\u9170\u80fa\u8fd9\u4e2a\u5728TLC\u4e0a\u4e0d\u6613\u68c0\u6d4b\u7684\u526f\u4ea7\u7269\uff0c\u8f83\u96be\u901a\u8fc7\u67f1\u5c42\u6790\u9664\u53bb\uff0c\u4f5c\u8005\u5c1d\u8bd5\u6700\u6210\u529f\u7684\u65b9\u6cd5\u662f\u5229\u7528\u52a0\u70ed\u771f\u7a7a\u5e72\u71e5\u8fc7\u591c\uff0c\u53ef\u4ee5\u9664\u53bb\u7edd\u5927\u90e8\u5206\u8be5\u6742\u8d28\u3002<\/p>\n

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

Table 1.<\/p>\n

\u00a0 \u5b9e\u9645\u4e0a\uff0cDake\u7b49\u4eba\u6240\u53c2\u8003\u5229\u7528\u7684\u6d3b\u5316\u65b9\u6cd5\uff0c\u6b63\u662f\u4e4b\u524dK.C. Nicolaou\u4ee5\u53ca Phil. S. Baran\u5728CP\u5206\u5b50\u5168\u5408\u6210\u4e2d\u6240\u53d1\u5c55\u7684\u65b9\u6cd5\uff0c\u533a\u522b\u53ea\u5728\u4e8e\uff0c Baran\u4ee5\u6b64\u6d3b\u5316\u4e86\u5927\u4f4d\u963b\u7fa7\u9178\u540e\u5236\u5907\u7684\u662f\u03b1-\u91cd\u6c2e\u916e\u7c7b\u5316\u5408\u7269\u3002[4]<\/sup>\u5728CP\u5206\u5b50\u7684\u5168\u5408\u6210\u4e2d\uff0cBaran\u5e0c\u671b\u5f97\u5230\u03b1-\u91cd\u6c2e\u916e7<\/strong>\u6765\u8fdb\u884cArndt-Eistert\u53cd\u5e94\u4ece\u800c\u6784\u5efa\u8d77\u76ee\u6807\u5206\u5b50\u4e2d\u7684\u5b63\u78b3\u4e2d\u5fc3\uff0c\u4f46\u5728\u4ece\u7fa7\u91786<\/strong>\u5236\u59077<\/strong>\u7684\u8fc7\u7a0b\u4e2d\u9047\u5230\u4e86\u56f0\u96be\uff08\u89c1Scheme 3.\uff09\u3002\u8003\u5bdf6<\/strong>\u7684\u7a7a\u95f4\u7ed3\u6784\u53ef\u4ee5\u53d1\u73b0\uff0c\u5176\u7fa7\u9178\u57fa\u56e2\u5468\u56f4\u7684\u7a7a\u95f4\u4f4d\u963b\u969c\u788d\u6781\u5176\u5927\uff0c\u800c\u7fa7\u9178\u53c8\u5904\u4e8e\u5206\u5b50\u4e2d\u51f9\u7684\u4f4d\u7f6e\uff0c\u5bfc\u81f4\u5e38\u89c4\u7684\u6d3b\u5316\u65b9\u5f0f\u5bf9\u5176\u4e0d\u8d77\u4f5c\u7528\u3002\u4f8b\u5982\u4ee5\u9170\u6c2f\u5236\u6210\u6df7\u5408\u9178\u9150\u65b9\u6cd5\u4e2d\uff0c\u91cd\u6c2e\u7532\u70f7\u5bf9\u4e24\u4e2a\u7fb0\u57fa\u4f4d\u7f6e\u90fd\u6709\u8fdb\u653b\uff0c\u800c\u7528Vilsmeir\u8bd5\u5242\u5728\u5267\u70c8\u6761\u4ef6\u4e0b\u5c1d\u8bd5\u6d3b\u5316\u5219\u5bfc\u81f4\u4e86\u539f\u6599\u7684\u5206\u89e3\u4ee5\u53ca\u7532\u916f\u7684\u751f\u6210\u3002\u5728\u8fd9\u79cd\u56f0\u5883\u4e0b\uff0cBaran\u5fc5\u987b\u8981\u53d1\u5c55\u65b0\u7684\u6539\u826f\u65b9\u6cd5\u624d\u80fd\u89e3\u51b3\u8fd9\u4e2a\u95ee\u9898\u3002Nicolaou\u548cBaran\u610f\u8bc6\u5230\u4e00\u4e2a\u76f8\u5bf9\u5c0f\u7684\u8bd5\u5242\uff0c\u4f8b\u5982\u7531MsCl\u548c\u5408\u9002\u7684\u78b1\u539f\u4f4d\u751f\u6210\u7684\u786b\u9170\u70ef\u5316\u5408\u7269\uff08sulfene\uff09\u4e5f\u8bb8\u80fd\u591f\u7a7f\u900fCP\u5206\u5b50\u7cfb\u7edf\u4e2d\u7684\u7acb\u4f53\u969c\u788d\u800c\u5c06\u7fa7\u9178\u8f6c\u5316\u4e3a\u4e0e\u9170\u6c2f\u5177\u6709\u7c7b\u4f3c\u53cd\u5e94\u6d3b\u6027\u7684\u9170\u57fa\u7532\u78fa\u9178\u916f\uff08acyl mesylates\uff09\u3002\u4e8b\u5b9e\u8bc1\u660e\uff0c\u8be5\u65b9\u6cd5\u786e\u5b9e\u6709\u6548\uff0c\u5316\u5408\u72696<\/strong>\u5728\u7528MsCl\u548cTEA\u5904\u7406\u8fc7\u540e\u76f4\u63a5\u52a0\u5165\u91cd\u6c2e\u7532\u70f7\u53cd\u5e94\uff0c\u4ee5\u9ad8\u6536\u7387\u5f97\u5230\u4e86\u76ee\u6807\u4ea7\u72697<\/strong>\u3002<\/p>\n

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

Scheme 3.<\/p>\n

\u00a0 \u8be5\u65b9\u6cd5\u64cd\u4f5c\u7b80\u4fbf\uff0c\u53ef\u4ee5\u65b9\u4fbf\u7684\u5236\u5907\u5927\u4f4d\u963b\u7684\u03b1-\u91cd\u6c2e\u916e\u7c7b\u5316\u5408\u7269\u3002\u5728CP\u5206\u5b50\u7684\u5168\u5408\u6210\u8fc7\u7a0b\u4e2d\uff0cBaran\u6709\u673a\u4f1a\u5c06\u6b64\u65b9\u6cd5\u5728\u4e00\u7cfb\u5217\u7c7b\u4f3c\u7684\u5e95\u7269\u4e0a\u8fdb\u884c\u5c1d\u8bd5\u3002CP\u5168\u5408\u6210\u4e2d\u7684\u5176\u4ed6\u5e95\u7269\uff0c\u5e26\u6709\u7845\u70f7\u4fdd\u62a4\u57fa\u4ee5\u53ca\u7f29\u919b\u7ed3\u6784\u7684\u5bf9\u9178\u654f\u611f\u7684\u5e95\u72699<\/strong>–12<\/strong>\uff0c\u4ee5\u53ca\u540c\u6837\u5bf9\u78b1\u654f\u611f\u7684\u5e95\u72698<\/strong>–10<\/strong>\u548c13<\/strong>\u5728\u8be5\u53cd\u5e94\u6761\u4ef6\u4e0b\u5747\u5177\u6709\u826f\u597d\u7684\u8010\u53d7\u6027\uff0c\u6536\u7387\u826f\u597d\u3002\u5728\u5176\u4ed6\u590d\u6742\u7684\u5927\u4f4d\u963b\u5e95\u7269\u4e0a\u5229\u7528\u8be5\u65b9\u6cd5\u8fdb\u884c\u53cd\u5e94\uff0c\u6548\u679c\u540c\u6837\u4ee4\u4eba\u6ee1\u610f\uff0c\u5c24\u5176\u662f\u4e07\u53e4\u9709\u7d20\u884d\u751f\u726919<\/strong>\uff0c\u5728\u8be5\u5206\u5b50\u4e2d\u81f3\u5c11\u5b58\u5728\u4e5d\u4e2a\u9170\u80fa\u7ed3\u6784\u4ee5\u53ca\u4e00\u7cfb\u5217\u654f\u611f\u800c\u6613\u5dee\u5411\u5f02\u6784\u5316\u7684\u4e2d\u5fc3\uff0c\u5e95\u7269\u4f9d\u7136\u987a\u5229\u8f6c\u5316\u3002\uff08\u89c1Table 2.\uff09<\/p>\n

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

Table 2.<\/p>\n

\u00a0 \u867d\u7136\u4e4b\u524d\u6587\u732e\u4e2d\u4e5f\u6709\u5229\u7528\u9170\u57fa\u7532\u78fa\u9178\u916f\u7684\u62a5\u9053\uff0c\u4f46\u662f\u6587\u732e\u4e2d\u90fd\u6ca1\u6709\u7ed9\u51fa\u786e\u5b9a\u7684\u8bc1\u636e\u8bc1\u660e\u9170\u57fa\u7532\u78fa\u9178\u916f\u5c31\u662f\u5b9e\u9645\u7684\u53cd\u5e94\u4e2d\u95f4\u4f53\u3002Nicolaou\u548cBaran\u91cd\u73b0\u4e86\u4e00\u4e9b\u58f0\u79f0\u5229\u7528\u9170\u57fa\u7532\u78fa\u9178\u916f\u7684\u6587\u732e\u5185\u5bb9\uff0c\u53d1\u73b0\u5927\u90e8\u5206\u53cd\u5e94\u4e2d\uff0c\u78fa\u9170\u6c2f\u4ecb\u5bfc\u7684\u8131\u6c34\u751f\u6210\u7684\u5bf9\u79f0\u6027\u9178\u9150\u624d\u662f\u771f\u6b63\u7684\u4e2d\u95f4\u4f53\u3002\u800cBaran\u901a\u8fc7\u5bf9\u672c\u65b9\u6cd5\u7684\u4e2d\u95f4\u4f53\u5206\u79bb\u540e\u5e76\u8fdb\u884c\u6838\u78c1\u5171\u632f\u8868\u5f81\uff0c\u9996\u6b21\u7528\u5149\u8c31\u624b\u6bb5\u660e\u786e\u4e86\u9170\u57fa\u7532\u78fa\u9178\u916f\u4e2d\u95f4\u4f53\u7684\u5b58\u5728\u3002<\/p>\n

\u7c7b\u4f3c\u7684\uff0c2011\u5e74\u4e0a\u6d77\u533b\u5de5\u9662\u5468\u4f1f\u6f84\u7b49[5]<\/sup>\u5728\u5bf9\u62df\u80bd\u7c7b\u6291\u5236\u5242\u8fdb\u884c\u7814\u7a76\u65f6\uff0c\u501f\u9274\u6b64\u65b9\u6cd5\u987a\u5229\u5b8c\u6210\u4e86\u76ee\u6807\u5206\u5b50\u7684\u5408\u6210\u3002\u5468\u7b49\u6700\u521d\u7684\u5c1d\u8bd5\u662f\u4ee5Cbz\u4fdd\u62a4\u7684Leu\uff0cIle\u548cPhe\u4e09\u79cd\u6c28\u57fa\u9178\u4e3a\u5408\u6210\u780c\u5757\u5206\u522b\u4e0e\u82b3\u80fa\u8fdb\u884c\u7f29\u5408\uff0c\u7136\u800c\u6548\u679c\u4e0d\u4f73\uff0c\u5e38\u89c1\u7f29\u5408\u5242\u624b\u6bb5\u7ed9\u51fa\u7684\u6536\u7387\u8f83\u4f4e\uff0c\u65e0\u6cd5\u6ee1\u8db3\u8fdb\u4e00\u6b65\u7684\u7814\u7a76\u9700\u8981\u3002\u7ecf\u8fc7\u63a8\u6d4b\uff0c\u5468\u8ba4\u4e3a\u662fN<\/em>-\u4fdd\u62a4\u6c28\u57fa\u9178\u7684\u4f4d\u963b\u4ee5\u53ca\u82b3\u80fa\u7684\u4f4e\u4eb2\u6838\u6027\u540c\u65f6\u5bfc\u81f4\u4e86\u4f4e\u6536\u7387\u3002\u5728\u5c1d\u8bd5MsCl\u4e0e\u78b1\u914d\u5408\u6d3b\u5316\u7fa7\u57fa\u65b9\u6cd5\u65f6\uff0c\u4ee5\u4e09\u4e59\u80fa\u6216\u662f\u5421\u5576\u4f5c\u4e3a\u78b1\u7ed9\u51fa\u7684\u7ed3\u679c\u540c\u6837\u6b20\u4f73\u3002\u901a\u8fc7\u5bf9\u78b1\u8fdb\u884c\u7b5b\u9009\uff0c\u5468\u53d1\u73b0\u5229\u7528N<\/em>-\u7532\u57fa\u54aa\u5511\u53ef\u4ee5\u6539\u5584\u53cd\u5e94\u7ed3\u679c\uff0c\uff08\u89c1Table 3.\uff09\u5728\u5bf9\u53cd\u5e94\u6761\u4ef6\u8fdb\u884c\u4f18\u5316\u4e4b\u540e\uff0c\u4e09\u79cd\u5927\u4f4d\u963b\u7684\u6c28\u57fa\u9178\u4e0e\u7f3a\u7535\u5b50\u7684\u82b3\u80fa\u7684\u7f29\u5408\u6536\u7387\u5927\u5e45\u5ea6\u63d0\u9ad8\u3002<\/p>\n

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

Table 3.<\/p>\n

\u00a0 2004\u5e74\uff0cGoldman\u5728\u524d\u671f\u5c06\u7fa7\u9178\u91d1\u5c5e\u76d0\u7c7b\u6bd4\u6709\u673a\u916f\u5e76\u4f5c\u4e3a\u9170\u5316\u5242\u4e0e\u80fa\u7684\u53cd\u5e94\u57fa\u7840\u4e0a\uff0c\u4eceZr(IV), Ti(IV)\u548cTa(V)\u4e2d\u9009\u51fa\u6700\u4f18\u7684Ta(V)\u8fdb\u4e00\u6b65\u7814\u7a76\uff0c\u53d1\u73b0TaCl5<\/sub>\u53ef\u4ee5\u4ecb\u5bfc\u5927\u4f4d\u963b\u7fa7\u9178\u4e0e\u80fa\u4e4b\u95f4\u7684\u9170\u80fa\u952e\u5f62\u6210\uff0c\u5e76\u4e14\u5728\u624b\u6027\u7fa7\u9178\u5e95\u7269\u53c2\u4e0e\u7684\u53cd\u5e94\u4e2d\u53ea\u6709\u5f88\u4f4e\u6c34\u5e73\u7684\u6d88\u65cb\u5316\u53d1\u751f\uff0c\u53ef\u80fd\u7684\u53cd\u5e94\u673a\u5236\u5982Scheme 4\u6240\u793a\u3002[6]<\/sup><\/p>\n

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

Scheme 4.<\/p>\n

\u00a0 \u4e0e\u4e4b\u524d\u5927\u591a\u7684\u8131\u6c34\u6027\u7f29\u5408\u601d\u60f3\u4e0d\u540c\uff0c2012\u5e74Bode\u63d0\u51fa\u4e86\u5229\u7528\u683c\u6c0f\u8bd5\u5242\u4e0e\u5f02\u6c30\u9178\u916f\u53cd\u5e94\u6784\u5efa\u9170\u80fa\u952e\u7684\u65b0\u601d\u8def\u3002[7]<\/sup>\u8be5\u65b9\u6cd5\u53cd\u5e94\u6761\u4ef6\u7b80\u4fbf\uff0c\u5bf9\u4e8e\u683c\u6c0f\u8bd5\u5242\u7247\u6bb5\u6216\u8005\u5f02\u6c30\u9178\u916f\u7247\u6bb5\u5747\u6709\u5e7f\u6cdb\u7684\u5e95\u7269\u9002\u5e94\u6027\u4e0e\u517c\u5bb9\u6027\uff0c\u53ef\u4ee5\u9ad8\u6548\u5730\u5236\u5907\u5927\u4f4d\u963b\u4e0e\u7f3a\u7535\u5b50\u9170\u80fa\u3002\uff08\u89c1Table 4.\uff09\u5f53\u5e95\u7269\u4e2d\u5b58\u5728\u916f\u57fa\uff0c\u7fb0\u57fa\u7b49\u53ef\u80fd\u4e0e\u683c\u6c0f\u8bd5\u5242\u53cd\u5e94\u7684\u6f5c\u5728\u7ade\u4e89\u6027\u7684\u5b98\u80fd\u56e2\u65f6\uff0c\u6240\u5f97\u76ee\u6807\u4ea7\u7269\u7684\u4ea7\u7387\u4f9d\u7136\u5f88\u9ad8\u3002\u503c\u5f97\u6ce8\u610f\u7684\u662f\uff0c\u4f7f\u7528\u8be5\u65b9\u6cd5\u65f6\u9700\u8981\u8003\u8651\u6240\u7528\u539f\u6599\u8f6c\u5316\u4e3a\u683c\u6c0f\u8bd5\u5242\u4e0e\u5f02\u6c30\u9178\u916f\u7684\u53ef\u884c\u6027\u95ee\u9898\u3002<\/p>\n

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

Table 4.<\/p>\n

\u00a0 2016\u5e74\uff0cUlven\u7b49\u5728\u91cd\u590d\u6587\u732e\u8fc7\u7a0b\u4e2d\uff0c[8]<\/sup>\u6839\u636e\u6587\u732e\u6761\u4ef6\u4ee5HATU\u4e3a\u7f29\u5408\u5242\uff0c\u5c0620<\/strong>\u4e0e21<\/strong>\u7f29\u5408\u5236\u590722<\/strong>\u65f6\u53cd\u5e94\u8fdb\u884c\u4e0d\u4f73\uff0c\u8fdb\u4e00\u6b65\u5c1d\u8bd5\u5176\u4ed6\u7f29\u5408\u65b9\u6cd5\u4e5f\u65e0\u529f\u800c\u8fd4\u3002\uff08\u89c1Table 5.\uff09\u8be5\u53cd\u5e94\u7684\u96be\u70b9\u5728\u4e8e\u82b3\u80fa\u7684\u4f4e\u4eb2\u6838\u6027\u53ca\u4f4d\u963b\u4e0e\u7fa7\u9178\u5468\u56f4\u7684\u4f4d\u963b\u4e14\u5b58\u5728\u654f\u611f\u7684\u53d4\u4e01\u916f\u57fa\u56e2\u3002<\/p>\n

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

Table 5.<\/p>\n

\u00a0 Ulven\u8003\u8651\u5230\u9700\u8981\u5c06\u7f29\u5408\u8fc7\u7a0b\u4e2d\u7684\u4f4d\u963b\u56e0\u7d20\u964d\u4f4e\u5230\u6700\u5c0f\u624d\u53ef\u80fd\u4f7f\u53cd\u5e94\u6210\u529f\u8fdb\u884c\uff0c\u4e8e\u662f\u51b3\u5b9a\u5f15\u5165\u4f53\u79ef\u8f83\u5c0f\u7684\u9170\u6c1f\u3002\u7ecf\u8fc7\u6bd4\u8f83\u4e4b\u540e\uff0c\u51b3\u5b9a\u4f7f\u7528\u6ca1\u6709\u6bd2\u526f\u4ea7\u7269\u7684BTFFH\u4f5c\u4e3a\u9170\u6c1f\u5316\u8bd5\u5242\u3002\u5229\u7528\u8be5\u65b9\u6cd5\u4e0d\u4ec5\u6210\u529f\u5408\u6210\u4e86\u539f\u6765\u7684\u76ee\u6807\u4ea7\u7269\uff0c\u800c\u4e14\u5728\u539f\u6599\u7684\u7c7b\u4f3c\u7269\u4ee5\u53ca\u5df2\u6709\u6587\u732e\u62a5\u9053\u7684\u4f4e\u6536\u7387\u5927\u4f4d\u963b\u5e95\u7269\u6848\u4f8b\u4e2d\u540c\u6837\u53d6\u5f97\u4e86\u826f\u597d\u7684\u7ed3\u679c\u3002\uff08\u89c1Table 6.\uff09\u4e0d\u8fc7\uff0c\u8be5\u65b9\u6cd5\u5728\u7f3a\u4e4f\u7b2c\u4e8c\u4e2a\u03b1\u53d6\u4ee3\u57fa\u7684\u82b3\u57fa\u4e59\u9178\u7c7b\u5e95\u7269\u4ee5\u53ca\u66f4\u5927\u4f4d\u963b\u7684\u67d0\u4e9b\u5e95\u7269\u4e0a\u6548\u679c\u4e0d\u4f73\uff0c\u800c\u5f53\u5927\u91cf\u5236\u5907\u65f6\uff0cBTFFH\u7684\u6210\u672c\u4e5f\u662f\u9700\u8981\u8003\u8651\u7684\u95ee\u9898\u3002<\/p>\n

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

Table 6.<\/p>\n

\u00a0 \u4ece\u4ee5\u4e0a\u51e0\u7bc7\u5206\u4eab\u7684\u6587\u732e\u4e2d\u53ef\u4ee5\u770b\u51fa\uff0c\u5bf9\u4e8e\u5927\u4f4d\u963b\u7684\u5e95\u7269\uff0c\u5c1d\u8bd5\u5bfb\u627e\u8f83\u5c0f\u4f53\u79ef\u7684\u6d3b\u5316\u7b56\u7565\u5f80\u5f80\u662f\u6bd4\u8f83\u597d\u7684\u529e\u6cd5\uff0c\u5e76\u4e14\u53cd\u5e94\u7684\u6761\u4ef6\u9700\u8981\u8003\u8651\u5e95\u7269\u7684\u8010\u53d7\u6027\u6700\u597d\u5c3d\u91cf\u6e29\u548c\u3002\u800c\u5f53\u5df2\u6709\u65b9\u6cd5\u4e0d\u80fd\u53d6\u5f97\u8f83\u597d\u7ed3\u679c\u65f6\uff0c\u901a\u8fc7\u68b3\u7406\u6587\u732e\u8fdb\u884c\u9002\u5f53\u7684\u6539\u8fdb\u4e5f\u80fd\u53d6\u5f97\u4e0d\u9519\u7684\u6548\u679c\u3002\u5e0c\u671b\u4ee5\u4e0a\u51e0\u70b9\u603b\u7ed3\u80fd\u7ed9\u5404\u4f4d\u8bfb\u8005\u5728\u65e5\u5e38\u79d1\u7814\u751f\u6d3b\u4e2d\u63d0\u4f9b\u4e00\u70b9\u5e2e\u52a9\u3002<\/p>\n

\u53c2\u8003\u6587\u732e<\/strong><\/h4>\n
    \n
  1. Brown D G, Bostr\u00f6m J. [J]. J. Med. Chem.<\/em>, 2016<\/strong>, 59<\/em>, 4443~4458.<\/li>\n
  2. Dunetz J R, Magano J, Weisenburger G A. [J]. Org. Process Res. Dev.<\/em>, 2016<\/strong>, 20<\/em>, 140~177.<\/li>\n
  3. Woo J C S, Fenster E, Dake G R. [J]. J. Org. Chem.<\/em>, 2004<\/strong>, 69<\/em>, 8984~8986.<\/li>\n
  4. Nicolaou K C, Baran P S, Zhong Y, et al<\/em>. [J]. Org. Lett.<\/em>, 1999<\/strong>, 1<\/em>, 883~886.<\/li>\n
  5. Mao L, Wang Z, Li Y, et al<\/em>. [J]. Synlett.<\/em>, 2011<\/strong>, 129~133.<\/li>\n
  6. Fang J B, Sanghi R, Kohn J, et al<\/em>. [J]. Inorg. Chim. Acta.<\/em>, 2004<\/strong>, 357<\/em>, 2415~2426.<\/li>\n
  7. Sch\u00e4fer G, Matthey C, Bode J W.[J]. Angew. Chem. Int. Ed.<\/em>, 2012<\/strong>, 51<\/em>, 9173~9175.<\/li>\n
  8. Due-Hansen M E, Pandey S K, Christiansen E, et al<\/em>. [J]. Org. Biomol. Chem<\/em>., 2016<\/strong>, 14<\/em>, 430~433.<\/li>\n<\/ol>\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":"\u9170\u80fa\u952e\u662f\u4e00\u7c7b\u91cd\u8981\u7684\u5b98\u80fd\u56e2\uff0c\u4e0d\u4ec5\u5e7f\u6cdb\u5b58\u5728\u4e8e\u533b\u836f\u4e2d\u95f4\u4f53\uff0c\u6d3b\u6027\u5929\u7136\u4ea7\u7269\u4ee5\u53ca\u529f\u80fd\u6750\u6599\u5206\u5b50\u7684\u7ed3\u6784\u4e4b\u4e2d\uff0c\u800c\u4e14\u4e5f\u662f\u86cb\u767d\u8d28\u7ed3\u6784\u4e2d\u7684\u91cd\u8981\u5316\u5b66\u7ebd\u5e26\u3002\u9170\u80fa\u952e\u7684\u6784\u7b51\u4e00\u76f4\u662f\u65b9\u6cd5\u5b66\u7814\u7a76\u7684\u6d3b\u8dc3\u9886\u57df\uff0c\u4f20\u7edf\u7684\u9170\u80fa\u952e\u7684\u5408\u6210\u65b9\u6cd5\u4e3b\u8981\u6d89\u53ca\u5230\u7fa7\u9178\u7684\u6d3b\u5316\uff0c\u5c06\u5176\u8f6c\u5316\u4e3a\u9170\u5364\uff0c\u9178\u9150\u7b49\u884d\u751f\u7269\u540e\u518d\u4e0e\u80fa\u7247\u6bb5\u53cd\u5e94\uff0c\u6216\u8005\u5229\u7528\u5404\u7c7b\u7f29\u5408\u5242\u4fc3\u8fdb\u7fa7\u9178\u4e0e\u80fa\u7684\u7f29\u5408\uff0c\u6b64\u5916\uff0c\u8fd1\u5e74\u6765\u8fd8\u9646\u7eed\u62a5\u9053\u4e86\u8bf8\u5982\u82b3\u5364\u4e0e\u80fa\u5728\u91d1\u5c5e\u50ac\u5316\u4e0b\u6784\u5efa\u9170\u80fa\u952e\u7b49\u65b0\u7684\u7b56\u7565\u3002 \u9170\u80fa\u5408\u6210\u7814\u7a76\u80cc\u666f\u53ca\u610f\u4e49 \u9170\u80fa\u7684\u5408\u6210\u5728\u836f\u7269\u5316\u5b66\u7814\u7a76\u4e2d\u66f4\u662f\u5360\u6709\u4e3e\u8db3\u8f7b\u91cd\u7684\u5730\u4f4d\uff0c\u8fd1\u51e0\u5e74\u591a\u7bc7\u5bf9\u4e8e\u836f\u5316\u9886\u57df\u7684\u5927\u6570\u636e\u5206\u6790\u8bba\u6587\u90fd\u6beb\u65e0\u4f8b\u5916\u5730\u53cd\u6620\u4e86\u8fd9\u4e00\u70b9\u3002\u6bd4\u5982\u4ece2016\u5e74AstraZeneca\u7684Brown\u7b49[1]\u5bf92014\u5e74\u4ee5\u53ca1984\u5e74\u4e24\u5e74\u4e2d\u836f\u5316\u9886\u57df\u6700\u5e38\u4f7f\u7528\u7684\u5408\u6210\u53cd\u5e94\u8fdb\u884c\u7684\u5206\u6790\u4e2d\u53ef\u4ee5\u53d1\u73b0\uff0c\u51e0\u4e4e\u540c\u4e09\u5341\u5e74\u524d\u7684\u60c5\u51b5\u76f8\u5dee\u65e0\u51e0\uff0c\u6d89\u53ca\u9170\u80fa\u5408\u6210\u7684\u53cd\u5e94\u5728\u7ed3\u679c\u4e2d\u4f4d\u5217\u524d\u8305\u3002\uff08\u89c1Figure 1.\uff09 Figure 1. \u00a0 2016\u5e74\uff0cGilead\u548cPfizer\u7684\u5de5\u827a\u7814\u7a76\u4eba\u5458\u5171\u540c\u5728OPRD\u4e0a\u53d1\u8868\u4e86\u5173\u4e8e\u9178\u4e0e\u80fa\u53cd\u5e94\u751f\u6210\u9170\u80fa\u7684\u7efc\u8ff0\uff0c[2]\u4e0e\u4e4b\u524d\u5176\u4ed6\u5df2\u7ecf\u53d1\u8868\u7684\u5404\u7c7b\u7efc\u8ff0\u76f8\u6bd4\uff0c\u8be5\u6587\u7684\u7279\u8272\u662f\u6240\u5176\u8bc4\u8ff0\u53cd\u5e94\u7684\u89c4\u6a21\u5747\u8fbe\u5230100 mmol\u4ee5\u4e0a\u7684\u53cd\u5e94\u91cf\uff0c\u53ef\u4ee5\u8bf4\u8fd9\u7bc7\u7efc\u8ff0\u662f\u76ee\u524d\u5173\u4e8e\u5b9e\u9a8c\u5ba4\u6216\u8005\u5de5\u4e1a\u4e2d\u5927\u91cf\u5236\u5907\u9170\u80fa\u65b9\u6cd5\u7684\u6700\u6709\u4ef7\u503c\u7684\u53c2\u8003\u6587\u732e\u3002\u6587\u4e2d\u5217\u51fa\u4f4d\u4e8e\u7edf\u8ba1\u524d\u5217\u7684SOCl2\uff0c(COCl)2\uff0cEDCI, CDI\u7b49\u4f5c\u4e3a\u6d3b\u5316\u8bd5\u5242\u7684\u53cd\u5e94\u53ef\u4ee5\u8bf4\u662f\u5f53\u524d\u5bf9\u4e8e\u9170\u80fa\u5408\u6210\u6700\u4e3a\u7ecf\u5178\u4ee5\u53ca\u53ef\u9760\u7684\u5b9e\u9a8c\u65b9\u6cd5\u3002\uff08\u89c1Figure 2.\uff09 Figure 2. \u9170\u80fa\u5408\u6210\u9762\u4e34\u7684\u56f0\u96be\u6311\u6218 \u867d\u7136\u5316\u5b66\u5bb6\u5bf9\u4e8e\u9170\u80fa\u7684\u5408\u6210\u65b9\u6cd5\u5df2\u7ecf\u6709\u4e86\u76f8\u5f53\u6570\u91cf\u7684\u9009\u62e9\u7a7a\u95f4\u5e76\u4e14\u79ef\u7d2f\u4e86\u8db3\u591f\u7684\u7ecf\u9a8c\uff0c\u4f46\u662f\u4ecd\u7136\u7ecf\u5e38\u4f1a\u5728\u7814\u7a76\u8fc7\u7a0b\u4e2d\u51fa\u73b0\u76ee\u6807\u9170\u80fa\u7684\u5408\u6210\u53d7\u963b\u6216\u8005\u4e0d\u5982\u9884\u671f\u6548\u679c\u7684\u60c5\u51b5\u3002\u5f88\u591a\u65f6\u5019\u8fd9\u79cd\u56f0\u96be\u5728\u4e8b\u5148\u5e76\u4e0d\u4f1a\u88ab\u5145\u5206\u4f30\u8ba1\u5230\uff0c\u8fd9\u4e5f\u5c31\u662f\u4e3a\u4f55\u8bb8\u591a\u7814\u7a76\u4eba\u5458\u5728\u6587\u7ae0\u4e2d\u5199\u5230\u6b64\u5904\u65f6\u90fd\u4f1a\u5982\u6b64\u63cf\u8ff0\u2014\u2014\u201cThis seemingly trivial transformation to produce XXX was plagued with poor isolated yields or low conversions\u201d\u2014\u2014\u81f3\u5c11\u8bf4\u660e\u5728\u8d77\u521d\u8bbe\u8ba1\u65f6\uff0c\u9170\u80fa\u7684\u5408\u6210\u5728\u5927\u90e8\u5206\u7814\u7a76\u8005\u770b\u6765\u662f\u5b8c\u5168\u4e0d\u4f1a\u6709\u95ee\u9898\u7684\u3002\u6839\u636e\u5df2\u6709\u6587\u732e\u7684\u62a5\u9053\u4ee5\u53ca\u5c0f\u7f16\u672c\u4eba\u5728\u79d1\u7814\u4e2d\u7684\u4f53\u4f1a\uff0c\u53d1\u73b0\u5728\u9170\u80fa\uff08\u6216\u591a\u80bd\uff09\u7684\u5236\u5907\u4e2d\uff0c\u9664\u4e86\u5bf9\u4e8e\u624b\u6027\u5e95\u7269\u7f29\u5408\u65f6\u5bb9\u6613\u53d1\u751f\u6d88\u65cb\u5316\u8fd9\u4e2a\u95ee\u9898\u4e4b\u5916\uff0c\u51fa\u73b0\u610f\u5916\u9891\u7387\u6700\u9ad8\u7684\u662f\u6709C\u03b1\u4f4d\u5b58\u5728\u5927\u4f4d\u963b\u7fa7\u9178\u4ee5\u53ca\u7f3a\u7535\u5b50\u82b3\u80fa\u53c2\u4e0e\u7684\u9170\u80fa\u5408\u6210\u53cd\u5e94\u3002\u4e0b\u9762\uff0c\u5c0f\u7f16\u5c31\u5c06\u4ece\u8fd1\u5e74\u6765\u7684\u51e0\u7bc7\u6587\u732e\u5165\u624b\uff0c\u7ed3\u5408\u5176\u4e2d\u7684\u7814\u7a76\u5b9e\u4f8b\uff0c\u6765\u8c08\u8c08\u5982\u4f55\u89e3\u51b3\u8fd9\u4e2a\u95ee\u9898\uff0c\u4e5f\u5e0c\u671b\u6587\u732e\u4e2d\u63d0\u4f9b\u7684\u601d\u8def\u80fd\u5bf9\u5927\u5bb6\u81ea\u5df1\u7684\u8bfe\u9898\u6709\u6240\u501f\u9274\u3002 Scheme 1. \u7814\u7a76\u5b9e\u4f8b 2004\u5e74\uff0cDake\u7b49[3]\u5728\u5bf9Nitiol\u7684\u5168\u5408\u6210\u7814\u7a76\u4e2d\u9700\u8981\u5408\u6210Weinreb\u9170\u80fa1\u4f5c\u4e3a\u5176\u4e2d\u4e00\u4e2a\u4e2d\u95f4\u4f53\u4ee5\u4fbf\u4e0b\u4e00\u6b65\u7684\u7814\u7a76\uff0c\u7136\u800c\u5728\u5408\u6210\u4e2d\u53d1\u73b0\u65e0\u8bba\u662f\u4ee5\u7fa7\u91782\u8fd8\u662f\u7532\u916f3\u4e3a\u524d\u4f53\u53c2\u8003\u5df2\u6709\u6587\u732e\u8fdb\u884c\u8f6c\u5316\uff08\u89c1Scheme 1.\uff09\uff0c\u539f\u6599\u6216\u662f\u4e0d\u53cd\u5e94\u6216\u662f\u53ea\u5f97\u5230\u4f4e\u6536\u7387\u7684\u4ea7\u7269\u4ee5\u53ca\u6df7\u5408\u7269\uff0c\u53cd\u5e94\u7ed3\u679c\u4e0d\u4ee4\u4eba\u6ee1\u610f\u3002\u4f5c\u8005\u63a8\u6d4b\u5e94\u8be5\u662f\u7fa7\u57fa\u5468\u56f4\u5e9e\u5927\u7684\u7a7a\u95f4\u4f4d\u963b\u5bfc\u81f4\u4e86\u8be5\u95ee\u9898\u3002\u901a\u8fc7\u8c03\u7814\u6587\u732e\uff0c\u4f5c\u8005\u9009\u62e9\u4e86MsCl\u548cTEA\u4e3a\u53cd\u5e94\u6761\u4ef6\uff0c\u901a\u8fc7\u4e0e\u5e95\u7269\u7fa7\u9178\u5f62\u6210\u6df7\u5408\u9178\u9150\u6765\u8fbe\u5230\u6d3b\u5316\u7684\u76ee\u7684\u3002\u572850 mg\u5c0f\u8bd5\u89c4\u6a21\u53cd\u5e94\u83b7\u5f97\u4e8680 %\u6536\u7387\u7684\u826f\u597d\u7ed3\u679c\uff0c\u800c\u76f4\u63a5\u4ee5\u5c0f\u8bd5\u6761\u4ef6\u653e\u5927\u5230\u514b\u7ea7\u89c4\u6a21\u65f6\uff0c\u7531\u4e8ePMB\u4fdd\u62a4\u57fa\u8131\u9664\u5f15\u8d77\u7684\u526f\u53cd\u5e94\u4f7f\u6536\u7387\u964d\u4f4e\u4e3a55 %\u3002\u7ecf\u8fc7\u4f18\u5316MsCl\u4e0e\u78b1\u7684\u6bd4\u4f8b\uff0c\u8be5\u53cd\u5e94\u57281 g\u89c4\u6a21\u7684\u6536\u7387\u987a\u5229\u8fbe\u523080 %\u3002 Scheme 2. \u00a0 \u5c06\u4f18\u5316\u540e\u7684\u53cd\u5e94\u6761\u4ef6\uff08\u89c1Scheme 2\uff09\u5e94\u7528\u4e8e\u5176\u4ed6\u7acb\u4f53\u969c\u788d\u578b\u7fa7\u9178\u5e95\u72694\u6240\u5bf9\u5e94\u7684Weinreb\u9170\u80fa5\u7684\u5408\u6210\uff0c\u5747\u83b7\u5f97\u4e86\u4e2d\u7b49\u81f3\u826f\u597d\u7684\u5206\u79bb\u6536\u7387\uff08\u89c1Table 1\uff09\u3002\u603b\u7684\u6765\u8bf4\uff0c\u6b64\u65b9\u6cd5\u5bf9\u4e8e\u82b3\u9999\u6216\u662f\u8102\u80aa\u7c7b\u7fa7\u9178\u5e95\u7269\u6709\u826f\u597d\u7684\u9002\u5e94\u6027\uff0c\u540c\u65f6\uff0c\u8db3\u591f\u6e29\u548c\u7684\u53cd\u5e94\u6761\u4ef6\u4f7f\u5f97\u624b\u6027\u5e95\u7269\u5e76\u672a\u53d1\u751f\u5dee\u5411\u5f02\u6784\u5316\u3002\u4e0d\u8fc7\uff0c\u9700\u8981\u6307\u51fa\u7684\u662f\uff0c\u8be5\u65b9\u6cd5\u5408\u6210Weinreb\u9170\u80fa\u8fc7\u7a0b\u4e2d\u5bb9\u6613\u5f62\u6210N-\u7532\u6c27\u57fa-N-\u7532\u57fa\u7532\u78fa\u9170\u80fa\u8fd9\u4e2a\u5728TLC\u4e0a\u4e0d\u6613\u68c0\u6d4b\u7684\u526f\u4ea7\u7269\uff0c\u8f83\u96be\u901a\u8fc7\u67f1\u5c42\u6790\u9664\u53bb\uff0c\u4f5c\u8005\u5c1d\u8bd5\u6700\u6210\u529f\u7684\u65b9\u6cd5\u662f\u5229\u7528\u52a0\u70ed\u771f\u7a7a\u5e72\u71e5\u8fc7\u591c\uff0c\u53ef\u4ee5\u9664\u53bb\u7edd\u5927\u90e8\u5206\u8be5\u6742\u8d28\u3002 Table 1. \u00a0 \u5b9e\u9645\u4e0a\uff0cDake\u7b49\u4eba\u6240\u53c2\u8003\u5229\u7528\u7684\u6d3b\u5316\u65b9\u6cd5\uff0c\u6b63\u662f\u4e4b\u524dK.C. Nicolaou\u4ee5\u53ca Phil. S. Baran\u5728CP\u5206\u5b50\u5168\u5408\u6210\u4e2d\u6240\u53d1\u5c55\u7684\u65b9\u6cd5\uff0c\u533a\u522b\u53ea\u5728\u4e8e\uff0c Baran\u4ee5\u6b64\u6d3b\u5316\u4e86\u5927\u4f4d\u963b\u7fa7\u9178\u540e\u5236\u5907\u7684\u662f\u03b1-\u91cd\u6c2e\u916e\u7c7b\u5316\u5408\u7269\u3002[4]\u5728CP\u5206\u5b50\u7684\u5168\u5408\u6210\u4e2d\uff0cBaran\u5e0c\u671b\u5f97\u5230\u03b1-\u91cd\u6c2e\u916e7\u6765\u8fdb\u884cArndt-Eistert\u53cd\u5e94\u4ece\u800c\u6784\u5efa\u8d77\u76ee\u6807\u5206\u5b50\u4e2d\u7684\u5b63\u78b3\u4e2d\u5fc3\uff0c\u4f46\u5728\u4ece\u7fa7\u91786\u5236\u59077\u7684\u8fc7\u7a0b\u4e2d\u9047\u5230\u4e86\u56f0\u96be\uff08\u89c1Scheme 3.\uff09\u3002\u8003\u5bdf6\u7684\u7a7a\u95f4\u7ed3\u6784\u53ef\u4ee5\u53d1\u73b0\uff0c\u5176\u7fa7\u9178\u57fa\u56e2\u5468\u56f4\u7684\u7a7a\u95f4\u4f4d\u963b\u969c\u788d\u6781\u5176\u5927\uff0c\u800c\u7fa7\u9178\u53c8\u5904\u4e8e\u5206\u5b50\u4e2d\u51f9\u7684\u4f4d\u7f6e\uff0c\u5bfc\u81f4\u5e38\u89c4\u7684\u6d3b\u5316\u65b9\u5f0f\u5bf9\u5176\u4e0d\u8d77\u4f5c\u7528\u3002\u4f8b\u5982\u4ee5\u9170\u6c2f\u5236\u6210\u6df7\u5408\u9178\u9150\u65b9\u6cd5\u4e2d\uff0c\u91cd\u6c2e\u7532\u70f7\u5bf9\u4e24\u4e2a\u7fb0\u57fa\u4f4d\u7f6e\u90fd\u6709\u8fdb\u653b\uff0c\u800c\u7528Vilsmeir\u8bd5\u5242\u5728\u5267\u70c8\u6761\u4ef6\u4e0b\u5c1d\u8bd5\u6d3b\u5316\u5219\u5bfc\u81f4\u4e86\u539f\u6599\u7684\u5206\u89e3\u4ee5\u53ca\u7532\u916f\u7684\u751f\u6210\u3002\u5728\u8fd9\u79cd\u56f0\u5883\u4e0b\uff0cBaran\u5fc5\u987b\u8981\u53d1\u5c55\u65b0\u7684\u6539\u826f\u65b9\u6cd5\u624d\u80fd\u89e3\u51b3\u8fd9\u4e2a\u95ee\u9898\u3002Nicolaou\u548cBaran\u610f\u8bc6\u5230\u4e00\u4e2a\u76f8\u5bf9\u5c0f\u7684\u8bd5\u5242\uff0c\u4f8b\u5982\u7531MsCl\u548c\u5408\u9002\u7684\u78b1\u539f\u4f4d\u751f\u6210\u7684\u786b\u9170\u70ef\u5316\u5408\u7269\uff08sulfene\uff09\u4e5f\u8bb8\u80fd\u591f\u7a7f\u900fCP\u5206\u5b50\u7cfb\u7edf\u4e2d\u7684\u7acb\u4f53\u969c\u788d\u800c\u5c06\u7fa7\u9178\u8f6c\u5316\u4e3a\u4e0e\u9170\u6c2f\u5177\u6709\u7c7b\u4f3c\u53cd\u5e94\u6d3b\u6027\u7684\u9170\u57fa\u7532\u78fa\u9178\u916f\uff08acyl mesylates\uff09\u3002\u4e8b\u5b9e\u8bc1\u660e\uff0c\u8be5\u65b9\u6cd5\u786e\u5b9e\u6709\u6548\uff0c\u5316\u5408\u72696\u5728\u7528MsCl\u548cTEA\u5904\u7406\u8fc7\u540e\u76f4\u63a5\u52a0\u5165\u91cd\u6c2e\u7532\u70f7\u53cd\u5e94\uff0c\u4ee5\u9ad8\u6536\u7387\u5f97\u5230\u4e86\u76ee\u6807\u4ea7\u72697\u3002 Scheme 3. \u00a0 \u8be5\u65b9\u6cd5\u64cd\u4f5c\u7b80\u4fbf\uff0c\u53ef\u4ee5\u65b9\u4fbf\u7684\u5236\u5907\u5927\u4f4d\u963b\u7684\u03b1-\u91cd\u6c2e\u916e\u7c7b\u5316\u5408\u7269\u3002\u5728CP\u5206\u5b50\u7684\u5168\u5408\u6210\u8fc7\u7a0b\u4e2d\uff0cBaran\u6709\u673a\u4f1a\u5c06\u6b64\u65b9\u6cd5\u5728\u4e00\u7cfb\u5217\u7c7b\u4f3c\u7684\u5e95\u7269\u4e0a\u8fdb\u884c\u5c1d\u8bd5\u3002CP\u5168\u5408\u6210\u4e2d\u7684\u5176\u4ed6\u5e95\u7269\uff0c\u5e26\u6709\u7845\u70f7\u4fdd\u62a4\u57fa\u4ee5\u53ca\u7f29\u919b\u7ed3\u6784\u7684\u5bf9\u9178\u654f\u611f\u7684\u5e95\u72699–12\uff0c\u4ee5\u53ca\u540c\u6837\u5bf9\u78b1\u654f\u611f\u7684\u5e95\u72698–10\u548c13\u5728\u8be5\u53cd\u5e94\u6761\u4ef6\u4e0b\u5747\u5177\u6709\u826f\u597d\u7684\u8010\u53d7\u6027\uff0c\u6536\u7387\u826f\u597d\u3002\u5728\u5176\u4ed6\u590d\u6742\u7684\u5927\u4f4d\u963b\u5e95\u7269\u4e0a\u5229\u7528\u8be5\u65b9\u6cd5\u8fdb\u884c\u53cd\u5e94\uff0c\u6548\u679c\u540c\u6837\u4ee4\u4eba\u6ee1\u610f\uff0c\u5c24\u5176\u662f\u4e07\u53e4\u9709\u7d20\u884d\u751f\u726919\uff0c\u5728\u8be5\u5206\u5b50\u4e2d\u81f3\u5c11\u5b58\u5728\u4e5d\u4e2a\u9170\u80fa\u7ed3\u6784\u4ee5\u53ca\u4e00\u7cfb\u5217\u654f\u611f\u800c\u6613\u5dee\u5411\u5f02\u6784\u5316\u7684\u4e2d\u5fc3\uff0c\u5e95\u7269\u4f9d\u7136\u987a\u5229\u8f6c\u5316\u3002\uff08\u89c1Table 2.\uff09 Table 2. \u00a0 \u867d\u7136\u4e4b\u524d\u6587\u732e\u4e2d\u4e5f\u6709\u5229\u7528\u9170\u57fa\u7532\u78fa\u9178\u916f\u7684\u62a5\u9053\uff0c\u4f46\u662f\u6587\u732e\u4e2d\u90fd\u6ca1\u6709\u7ed9\u51fa\u786e\u5b9a\u7684\u8bc1\u636e\u8bc1\u660e\u9170\u57fa\u7532\u78fa\u9178\u916f\u5c31\u662f\u5b9e\u9645\u7684\u53cd\u5e94\u4e2d\u95f4\u4f53\u3002Nicolaou\u548cBaran\u91cd\u73b0\u4e86\u4e00\u4e9b\u58f0\u79f0\u5229\u7528\u9170\u57fa\u7532\u78fa\u9178\u916f\u7684\u6587\u732e\u5185\u5bb9\uff0c\u53d1\u73b0\u5927\u90e8\u5206\u53cd\u5e94\u4e2d\uff0c\u78fa\u9170\u6c2f\u4ecb\u5bfc\u7684\u8131\u6c34\u751f\u6210\u7684\u5bf9\u79f0\u6027\u9178\u9150\u624d\u662f\u771f\u6b63\u7684\u4e2d\u95f4\u4f53\u3002\u800cBaran\u901a\u8fc7\u5bf9\u672c\u65b9\u6cd5\u7684\u4e2d\u95f4\u4f53\u5206\u79bb\u540e\u5e76\u8fdb\u884c\u6838\u78c1\u5171\u632f\u8868\u5f81\uff0c\u9996\u6b21\u7528\u5149\u8c31\u624b\u6bb5\u660e\u786e\u4e86\u9170\u57fa\u7532\u78fa\u9178\u916f\u4e2d\u95f4\u4f53\u7684\u5b58\u5728\u3002 \u7c7b\u4f3c\u7684\uff0c2011\u5e74\u4e0a\u6d77\u533b\u5de5\u9662\u5468\u4f1f\u6f84\u7b49[5]\u5728\u5bf9\u62df\u80bd\u7c7b\u6291\u5236\u5242\u8fdb\u884c\u7814\u7a76\u65f6\uff0c\u501f\u9274\u6b64\u65b9\u6cd5\u987a\u5229\u5b8c\u6210\u4e86\u76ee\u6807\u5206\u5b50\u7684\u5408\u6210\u3002\u5468\u7b49\u6700\u521d\u7684\u5c1d\u8bd5\u662f\u4ee5Cbz\u4fdd\u62a4\u7684Leu\uff0cIle\u548cPhe\u4e09\u79cd\u6c28\u57fa\u9178\u4e3a\u5408\u6210\u780c\u5757\u5206\u522b\u4e0e\u82b3\u80fa\u8fdb\u884c\u7f29\u5408\uff0c\u7136\u800c\u6548\u679c\u4e0d\u4f73\uff0c\u5e38\u89c1\u7f29\u5408\u5242\u624b\u6bb5\u7ed9\u51fa\u7684\u6536\u7387\u8f83\u4f4e\uff0c\u65e0\u6cd5\u6ee1\u8db3\u8fdb\u4e00\u6b65\u7684\u7814\u7a76\u9700\u8981\u3002\u7ecf\u8fc7\u63a8\u6d4b\uff0c\u5468\u8ba4\u4e3a\u662fN-\u4fdd\u62a4\u6c28\u57fa\u9178\u7684\u4f4d\u963b\u4ee5\u53ca\u82b3\u80fa\u7684\u4f4e\u4eb2\u6838\u6027\u540c\u65f6\u5bfc\u81f4\u4e86\u4f4e\u6536\u7387\u3002\u5728\u5c1d\u8bd5MsCl\u4e0e\u78b1\u914d\u5408\u6d3b\u5316\u7fa7\u57fa\u65b9\u6cd5\u65f6\uff0c\u4ee5\u4e09\u4e59\u80fa\u6216\u662f\u5421\u5576\u4f5c\u4e3a\u78b1\u7ed9\u51fa\u7684\u7ed3\u679c\u540c\u6837\u6b20\u4f73\u3002\u901a\u8fc7\u5bf9\u78b1\u8fdb\u884c\u7b5b\u9009\uff0c\u5468\u53d1\u73b0\u5229\u7528N-\u7532\u57fa\u54aa\u5511\u53ef\u4ee5\u6539\u5584\u53cd\u5e94\u7ed3\u679c\uff0c\uff08\u89c1Table 3.\uff09\u5728\u5bf9\u53cd\u5e94\u6761\u4ef6\u8fdb\u884c\u4f18\u5316\u4e4b\u540e\uff0c\u4e09\u79cd\u5927\u4f4d\u963b\u7684\u6c28\u57fa\u9178\u4e0e\u7f3a\u7535\u5b50\u7684\u82b3\u80fa\u7684\u7f29\u5408\u6536\u7387\u5927\u5e45\u5ea6\u63d0\u9ad8\u3002 Table 3. \u00a0 2004\u5e74\uff0cGoldman\u5728\u524d\u671f\u5c06\u7fa7\u9178\u91d1\u5c5e\u76d0\u7c7b\u6bd4\u6709\u673a\u916f\u5e76\u4f5c\u4e3a\u9170\u5316\u5242\u4e0e\u80fa\u7684\u53cd\u5e94\u57fa\u7840\u4e0a\uff0c\u4eceZr(IV), Ti(IV)\u548cTa(V)\u4e2d\u9009\u51fa\u6700\u4f18\u7684Ta(V)\u8fdb\u4e00\u6b65\u7814\u7a76\uff0c\u53d1\u73b0TaCl5\u53ef\u4ee5\u4ecb\u5bfc\u5927\u4f4d\u963b\u7fa7\u9178\u4e0e\u80fa\u4e4b\u95f4\u7684\u9170\u80fa\u952e\u5f62\u6210\uff0c\u5e76\u4e14\u5728\u624b\u6027\u7fa7\u9178\u5e95\u7269\u53c2\u4e0e\u7684\u53cd\u5e94\u4e2d\u53ea\u6709\u5f88\u4f4e\u6c34\u5e73\u7684\u6d88\u65cb\u5316\u53d1\u751f\uff0c\u53ef\u80fd\u7684\u53cd\u5e94\u673a\u5236\u5982Scheme 4\u6240\u793a\u3002[6] Scheme 4. \u00a0 \u4e0e\u4e4b\u524d\u5927\u591a\u7684\u8131\u6c34\u6027\u7f29\u5408\u601d\u60f3\u4e0d\u540c\uff0c2012\u5e74Bode\u63d0\u51fa\u4e86\u5229\u7528\u683c\u6c0f\u8bd5\u5242\u4e0e\u5f02\u6c30\u9178\u916f\u53cd\u5e94\u6784\u5efa\u9170\u80fa\u952e\u7684\u65b0\u601d\u8def\u3002[7]\u8be5\u65b9\u6cd5\u53cd\u5e94\u6761\u4ef6\u7b80\u4fbf\uff0c\u5bf9\u4e8e\u683c\u6c0f\u8bd5\u5242\u7247\u6bb5\u6216\u8005\u5f02\u6c30\u9178\u916f\u7247\u6bb5\u5747\u6709\u5e7f\u6cdb\u7684\u5e95\u7269\u9002\u5e94\u6027\u4e0e\u517c\u5bb9\u6027\uff0c\u53ef\u4ee5\u9ad8\u6548\u5730\u5236\u5907\u5927\u4f4d\u963b\u4e0e\u7f3a\u7535\u5b50\u9170\u80fa\u3002\uff08\u89c1Table 4.\uff09\u5f53\u5e95\u7269\u4e2d\u5b58\u5728\u916f\u57fa\uff0c\u7fb0\u57fa\u7b49\u53ef\u80fd\u4e0e\u683c\u6c0f\u8bd5\u5242\u53cd\u5e94\u7684\u6f5c\u5728\u7ade\u4e89\u6027\u7684\u5b98\u80fd\u56e2\u65f6\uff0c\u6240\u5f97\u76ee\u6807\u4ea7\u7269\u7684\u4ea7\u7387\u4f9d\u7136\u5f88\u9ad8\u3002\u503c\u5f97\u6ce8\u610f\u7684\u662f\uff0c\u4f7f\u7528\u8be5\u65b9\u6cd5\u65f6\u9700\u8981\u8003\u8651\u6240\u7528\u539f\u6599\u8f6c\u5316\u4e3a\u683c\u6c0f\u8bd5\u5242\u4e0e\u5f02\u6c30\u9178\u916f\u7684\u53ef\u884c\u6027\u95ee\u9898\u3002 Table 4. \u00a0 2016\u5e74\uff0cUlven\u7b49\u5728\u91cd\u590d\u6587\u732e\u8fc7\u7a0b\u4e2d\uff0c[8]\u6839\u636e\u6587\u732e\u6761\u4ef6\u4ee5HATU\u4e3a\u7f29\u5408\u5242\uff0c\u5c0620\u4e0e21\u7f29\u5408\u5236\u590722\u65f6\u53cd\u5e94\u8fdb\u884c\u4e0d\u4f73\uff0c\u8fdb\u4e00\u6b65\u5c1d\u8bd5\u5176\u4ed6\u7f29\u5408\u65b9\u6cd5\u4e5f\u65e0\u529f\u800c\u8fd4\u3002\uff08\u89c1Table 5.\uff09\u8be5\u53cd\u5e94\u7684\u96be\u70b9\u5728\u4e8e\u82b3\u80fa\u7684\u4f4e\u4eb2\u6838\u6027\u53ca\u4f4d\u963b\u4e0e\u7fa7\u9178\u5468\u56f4\u7684\u4f4d\u963b\u4e14\u5b58\u5728\u654f\u611f\u7684\u53d4\u4e01\u916f\u57fa\u56e2\u3002 Table 5. \u00a0 Ulven\u8003\u8651\u5230\u9700\u8981\u5c06\u7f29\u5408\u8fc7\u7a0b\u4e2d\u7684\u4f4d\u963b\u56e0\u7d20\u964d\u4f4e\u5230\u6700\u5c0f\u624d\u53ef\u80fd\u4f7f\u53cd\u5e94\u6210\u529f\u8fdb\u884c\uff0c\u4e8e\u662f\u51b3\u5b9a\u5f15\u5165\u4f53\u79ef\u8f83\u5c0f\u7684\u9170\u6c1f\u3002\u7ecf\u8fc7\u6bd4\u8f83\u4e4b\u540e\uff0c\u51b3\u5b9a\u4f7f\u7528\u6ca1\u6709\u6bd2\u526f\u4ea7\u7269\u7684BTFFH\u4f5c\u4e3a\u9170\u6c1f\u5316\u8bd5\u5242\u3002\u5229\u7528\u8be5\u65b9\u6cd5\u4e0d\u4ec5\u6210\u529f\u5408\u6210\u4e86\u539f\u6765\u7684\u76ee\u6807\u4ea7\u7269\uff0c\u800c\u4e14\u5728\u539f\u6599\u7684\u7c7b\u4f3c\u7269\u4ee5\u53ca\u5df2\u6709\u6587\u732e\u62a5\u9053\u7684\u4f4e\u6536\u7387\u5927\u4f4d\u963b\u5e95\u7269\u6848\u4f8b\u4e2d\u540c\u6837\u53d6\u5f97\u4e86\u826f\u597d\u7684\u7ed3\u679c\u3002\uff08\u89c1Table 6.\uff09\u4e0d\u8fc7\uff0c\u8be5\u65b9\u6cd5\u5728\u7f3a\u4e4f\u7b2c\u4e8c\u4e2a\u03b1\u53d6\u4ee3\u57fa\u7684\u82b3\u57fa\u4e59\u9178\u7c7b\u5e95\u7269\u4ee5\u53ca\u66f4\u5927\u4f4d\u963b\u7684\u67d0\u4e9b\u5e95\u7269\u4e0a\u6548\u679c\u4e0d\u4f73\uff0c\u800c\u5f53\u5927\u91cf\u5236\u5907\u65f6\uff0cBTFFH\u7684\u6210\u672c\u4e5f\u662f\u9700\u8981\u8003\u8651\u7684\u95ee\u9898\u3002 Table 6. \u00a0 \u4ece\u4ee5\u4e0a\u51e0\u7bc7\u5206\u4eab\u7684\u6587\u732e\u4e2d\u53ef\u4ee5\u770b\u51fa\uff0c\u5bf9\u4e8e\u5927\u4f4d\u963b\u7684\u5e95\u7269\uff0c\u5c1d\u8bd5\u5bfb\u627e\u8f83\u5c0f\u4f53\u79ef\u7684\u6d3b\u5316\u7b56\u7565\u5f80\u5f80\u662f\u6bd4\u8f83\u597d\u7684\u529e\u6cd5\uff0c\u5e76\u4e14\u53cd\u5e94\u7684\u6761\u4ef6\u9700\u8981\u8003\u8651\u5e95\u7269\u7684\u8010\u53d7\u6027\u6700\u597d\u5c3d\u91cf\u6e29\u548c\u3002\u800c\u5f53\u5df2\u6709\u65b9\u6cd5\u4e0d\u80fd\u53d6\u5f97\u8f83\u597d\u7ed3\u679c\u65f6\uff0c\u901a\u8fc7\u68b3\u7406\u6587\u732e\u8fdb\u884c\u9002\u5f53\u7684\u6539\u8fdb\u4e5f\u80fd\u53d6\u5f97\u4e0d\u9519\u7684\u6548\u679c\u3002\u5e0c\u671b\u4ee5\u4e0a\u51e0\u70b9\u603b\u7ed3\u80fd\u7ed9\u5404\u4f4d\u8bfb\u8005\u5728\u65e5\u5e38\u79d1\u7814\u751f\u6d3b\u4e2d\u63d0\u4f9b\u4e00\u70b9\u5e2e\u52a9\u3002 \u53c2\u8003\u6587\u732e Brown D G, Bostr\u00f6m J. [J]. J. Med. Chem., 2016, 59, 4443~4458. 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