\u7532\u57fa\u5316<\/strong><\/a>\u200b\u53cd\u5e94<\/p>\n\u7b80\u8ff0<\/p>\n
\u5728\u5408\u6210\u5b9e\u9a8c\u5ba4\uff0c\u5927\u5bb6\u7ecf\u5e38\u4f1a\u63a5\u89e6\u5230\u7532\u57fa\u5316\u53cd\u5e94\uff0c\u4e00\u822c\u7ecf\u5e38\u4f1a\u5bf9\u6c2e\u3001\u6c27\u3001\u786b\u4ee5\u53ca\u78b3\u8fdb\u884c\u7532\u57fa\u5316(\u4e5f\u53ef\u80fd\u5bf9\u7845\uff0c\u78f7\u7b49\uff0c\u8fd9\u91cc\u4e0d\u505a\u4ecb\u7ecd)\uff1b\u7ecf\u5e38\u7528\u5230\u7684\u7532\u57fa\u5316\u8bd5\u5242\u4e00\u822c\u4e3a\u7898\u7532\u70f7\u3001\u786b\u9178\u4e8c\u7532\u916f\u3001\u78b3\u9178\u4e8c\u7532\u916f\u3001\u4e8c\u78b3\u9178\u4e8c\u7532\u916f\u3001\u7532\u9187\u3001\u91cd\u6c2e\u7532\u70f7(\u8f83\u5371\u9669)\u3001\u91cd\u6c2e\u7532\u70f7\u4e09\u7532\u57fa\u7845\u70f7\u3001\u7532\u919b\u3001\u4e09\u7532\u57fa\u94dd\u53ca\u7532\u57fa\u787c\u9178\u3001\u7532\u57fa\u683c\u6c0f\u8bd5\u5242\u3001\u56db\u7532\u57fa\u9521\u53ca\u7532\u57fa\u950c\u8bd5\u5242\u7b49\u3002<\/p>\n
<\/p>\n
\u7532\u57fa\u5316\u53cd\u5e94<\/p>\n
\u5408\u6210\u4e2d\u7ecf\u5e38\u4f1a\u5bf9\u7fa7\u57fa\uff0c\u7f9f\u57fa\uff0c\u5def\u57fa\uff0c\u80fa\u57fa\u4ee5\u53ca\u78b3\u8fdb\u884c\u7532\u57fa\u5316\uff0c\u4e0b\u9762\u5c06\u5206\u7c7b\u8fdb\u884c\u7b80\u5355\u4ecb\u7ecd\u3002<\/p>\n
\u6c27\u6216\u786b\u7684\u7532\u57fa\u5316<\/p>\n
\u7fa7\u57fa\u7684\u7532\u57fa\u5316\u53cd\u5e94\u6bd4\u8f83\u5e38\u89c1\uff0c\u6240\u7528\u7684\u8bd5\u5242\u4e5f\u5f88\u591a\uff0c\u5982\u7898\u7532\u70f7\u3001\u786b\u9178\u4e8c\u7532\u916f\u3001\u78b3\u9178\u4e8c\u7532\u916f\u3001\u4e8c\u78b3\u9178\u4e8c\u7532\u916f\u3001\u7532\u9187\u3001\u91cd\u6c2e\u7532\u70f7(\u8f83\u5371\u9669)\u3001\u91cd\u6c2e\u7532\u70f7\u4e09\u7532\u57fa\u7845\u70f7\u7b49\uff1b\u6bd4\u8f83\u5e38\u7528\u7684\u6709\u786b\u9178\u4e8c\u7532\u916f\uff0c\u7898\u7532\u70f7\uff0c\u7532\u9187\u7b49\u3002<\/p>\n
1.\u8349\u9170\u6c2f, DMF, DCM, 0\u5ea6to rt,\u00a0 \u00a0 \u00a0 \u00a00.5h \uff08\u5236\u5907\u9170\u6c2f\uff09<\/p>\n
2.\u7532\u9187, rt, 12h\u00a0 \u00a099% yield<\/p>\n
WO2021151014 A1<\/p>\n
\u6c2f\u5316\u4e9a\u781c, \u7532\u9187, ref, 18h\u00a0 \u00a0 78% yield<\/p>\n
DOI:10.1016\/j.bioorg.2021.105185<\/p>\n
<\/p>\n
\u786b\u9178\u4e8c\u7532\u916f\u3001\u78b3\u9178\u4e8c\u7532\u916f\u3001\u4e8c\u78b3\u9178\u4e8c\u7532\u916f\u4f5c\u4e3a\u7532\u57fa\u5316\u8bd5\u5242\u7684\u4f8b\u5b50<\/p>\n
\u91cd\u6c2e\u7532\u70f7(\u8f83\u5371\u9669)\u3001\u91cd\u6c2e\u7532\u70f7\u4e09\u7532\u57fa\u7845\u70f7\u4e5f\u53ef\u4f5c\u4e3a\u7532\u57fa\u5316\u8bd5\u5242\uff0c\u7531\u4e8e\u91cd\u6c2e\u7532\u70f7\u6bd4\u8f83\u5371\u9669\uff0c\u4e00\u822c\u662f\u4ee5\u4e00\u79cd\u524d\u4f53\u7684\u5f62\u5f0f\u5b58\u653e\u4e8e\u51b0\u7bb1\uff0c\u4e00\u822c\u90fd\u662f\u73b0\u505a\u73b0\u7528\uff0c\u4f7f\u7528\u65f6\u4e00\u5b9a\u8981\u6ce8\u610f\u5b89\u5168\u3002<\/p>\n
\u7f9f\u57fa\u6216\u5def\u57fa\u7684\u7532\u57fa\u5316\uff0c\u4e00\u822c\u8f83\u4e3a\u5e38\u7528\u7684\u8bd5\u5242\u4e3a\u7898\u7532\u70f7\u3001\u786b\u9178\u4e8c\u7532\u916f\u3001\u78b3\u9178\u4e8c\u7532\u916f\u4ee5\u53ca\u91cd\u6c2e\u7532\u70f7\u7b49\uff0c\u4e5f\u4f1a\u7528\u5230\u4e00\u4e9b\u5176\u5b83\u8bd5\u5242\uff0c\u7531\u4e8e\u7528\u9014\u6709\u9650\uff0c\u8fd9\u91cc\u5c31\u4e0d\u518d\u4ecb\u7ecd\u3002<\/p>\n
\u82ef\u915a\u7c7b\u53ca\u82ef\u786b\u915a\u7c7b\u5316\u5408\u7269\u7684\u7532\u57fa\u5316\uff0c\u6240\u7528\u8bd5\u5242\u4e00\u822c\u4e3a\u7898\u7532\u70f7\uff0c\u78f7\u9178\u4e09\u7532\u916f\u3001\u786b\u9178\u4e8c\u7532\u916f\u3001\u78b3\u9178\u4e8c\u7532\u916f\u4ee5\u53ca\u91cd\u6c2e\u7532\u70f7\u7b49\uff0c\u53cd\u5e94\u7c7b\u578b\u6bd4\u8f83\u7b80\u5355\uff0c\u4e00\u822c\u4e0d\u4f1a\u51fa\u73b0\u526f\u4ea7\u7269\u3002<\/p>\n
\u9187\u6216\u786b\u9187\u7c7b\u7684\u7532\u57fa\u5316\u6240\u7528\u8bd5\u5242\u4e0e\u82ef\u915a\u7c7b\u7532\u57fa\u5316\u8bd5\u5242\u8f83\u7c7b\u4f3c\uff0c\u4e00\u822c\u4e5f\u4e0d\u4f1a\u51fa\u73b0\u526f\u4ea7\u7269\u3002<\/p>\n
\u5982\u679c\u5e95\u7269\u4e0a\u7684\u6c2e\u3001\u6c27\u53ca\u786b\u90fd\u53ef\u4ee5\u88ab\u7532\u57fa\u5316\uff0c\u5982\u4f55\u53ea\u5355\u4e00\u7684\u5bf9\u6c27\u6216\u786b\u7532\u57fa\u5316\uff0c\u800c\u6c2e\u4e0d\u88ab\u7532\u57fa\u5316\uff1f\u7531\u4e8e\u786b\u7684\u4eb2\u6838\u80fd\u529b\u5f3a\u4e8e\u6c27\u548c\u6c2e\uff0c\u56e0\u6b64\u7532\u57fa\u5316\u8bd5\u5242\u4f18\u5148\u5bf9\u786b\u8fdb\u884c\u7532\u57fa\u5316\uff1b\u5f53\u5e95\u7269\u4e0a\u53ea\u6709\u6c2e\u548c\u6c27\u53ef\u4ee5\u88ab\u7532\u57fa\u5316\u65f6\uff0c\u4e00\u822c\u91c7\u7528\u4e0b\u9762\u4e24\u79cd\u65b9\u6cd5\uff0c\u53ef\u4ee5\u5927\u53ef\u80fd\u7684\u5bf9\u6c27\u8fdb\u884c\u7532\u57fa\u5316\u3002<\/p>\n
Method A: \u53cd\u5e94\u4e2d\u4f7f\u7528\u78b3\u9178\u94f6, \u7531\u4e8e\u94f6\u4f1a\u548c\u6c27\u4f1a\u5f62\u6210\u7279\u6b8a\u7684\u7ed3\u6784\uff0c\u56e0\u6b64\u78b3\u9178\u94f6\u7684\u4f7f\u7528\u53ef\u4ee5\u5927\u9650\u5ea6(\u4e0d\u80fd\u5b8c\u5168\u4fdd\u8bc1)\u4fdd\u8bc1\u53ea\u5bf9\u6c27\u8fdb\u884c\u7532\u57fa\u5316\u3002<\/p>\n
Method B: \u5f53\u4f7f\u7528\u4e09\u7532\u57fa\u53d4\u6c27\u76d0\u4f5c\u4e3a\u7532\u57fa\u5316\u8bd5\u5242\u65f6\uff0c\u53ea\u80fd\u5355\u4e00\u7684\u5bf9\u6c27\u6216\u786b\u8fdb\u884c\u7532\u57fa\u5316\u3002<\/p>\n
<\/p>\n
\u6c2e\u7684\u7532\u57fa\u5316\u53cd\u5e94<\/p>\n
\u6c2e\u7684\u7532\u57fa\u5316\u5e38\u7528\u7684\u65b9\u6cd5\u6709\u7898\u7532\u70f7(\u53ca\u5176\u5b83\u7532\u57fa\u5316\u8bd5\u5242)\u3001\u8fd8\u539f\u80fa\u5316\u3001Eschweiler\u2013Clarke\u53cd\u5e94\u7b49\uff0c\u8fd9\u91cc\u8981\u63d0\u9192\u4e00\u4e0b:\u7528\u7898\u7532\u70f7\u7532\u57fa\u5316\u65f6\uff0c\u5f53\u5fc3\u4f1a\u6709\u5b63\u94f5\u76d0\u751f\u6210\u7684\u98ce\u9669\uff1bEschweiler\u2013Clarke\u53cd\u5e94\u53ea\u80fd\u5bf9\u6c28\u57fa\u8fdb\u884c\u7532\u57fa\u5316\uff0c\u7f9f\u57fa\u548c\u5def\u57fa\u4e0d\u53d7\u5f71\u54cd\uff0c\u4f46\u662f\u8be5\u53cd\u5e94\u7684\u7532\u57fa\u5316\u6548\u679c\u6bd4\u8f83\u5f7b\u5e95\uff0c\u53ea\u80fd\u4ee5\u53d4\u6c2e\u5f62\u5f0f\u5b58\u5728\uff0c\u4f46\u662f\u4e0d\u4f1a\u751f\u6210\u5b63\u94f5\u76d0\u3002\u6c2e\u7684\u7532\u57fa\u5316\u5c31\u4e0d\u518d\u4e3e\u5b9e\u4f8b\u4e86\u3002<\/p>\n
\u78b3\u7684\u7532\u57fa\u5316<\/p>\n
\u70f7\u57fa\u78b3\u8981\u8fdb\u884c\u7532\u57fa\u5316\u53cd\u5e94\uff0c\u4e00\u822c\u60c5\u51b5\u4e0b\u8be5\u78b3\u539f\u5b50\u4e0a\u8981\u6709\u5438\u7535\u5b50\u57fa\u56e2\u4e14\u8be5\u78b3\u539f\u5b50\u4e0a\u8981\u6709\u6c22\u3002\u6240\u7528\u78b1\u4e00\u822c\u4e3a\u5f3a\u78b1\uff0c\u5982\u4e01\u57fa\u9502\u3001\u94a0\u6c22\u3001HMDSLi(Na, K)\u53caLDA\u7b49\uff0c\u6240\u7528\u7532\u57fa\u5316\u8bd5\u5242\u4e00\u822c\u4e3a\u7898\u7532\u70f7(\u5e38\u7528)\u3001\u4e09\u6c1f\u7532\u78fa\u9178\u7532\u916f\u3001\u786b\u9178\u4e8c\u7532\u916f\u7b49\u3002<\/p>\n
\u82b3\u73af\u78b3\u7532\u57fa\u5316\u53cd\u5e94\u4e00\u822c\u9700\u8981\u8fdb\u884c\u5076\u8054\u53cd\u5e94\uff0c\u4e00\u822c\u662f\u82b3\u57fa\u5364(\u7898\u6216\u6eb4)\u4ee5\u53caAr-OTf\u53c2\u4e0e\u7684\u5076\u8054\u53cd\u5e94\uff0c\u7532\u57fa\u5316\u8bd5\u5242\u6709\u7532\u57fa\u787c\u9178(\u53ca\u5176\u884d\u751f\u7269)\uff0c\u4e8c\u7532\u57fa\u950c\uff0c\u4e09\u7532\u57fa\u94dd\u7532\u57fa\u950c\u8bd5\u5242\u4ee5\u53ca\u7532\u57fa\u683c\u6c0f\u8bd5\u5242\u7b49\uff1b\u4e5f\u6709\u6587\u732e\u62a5\u9053\u82b3\u73af\u4e0a\u7684\u5364\u7d20\u5148\u548c\u4e01\u57fa\u9502\u6210\u9502\u76d0 \uff0c\u7136\u540e\u518d\u548c\u7532\u57fa\u5316\u8bd5\u5242(\u786b\u9178\u4e8c\u7532\u916f\uff0c\u7898\u7532\u70f7\u7b49)\u53cd\u5e94\uff0c\u8fdb\u884c\u7532\u57fa\u5316\u7684\u65b9\u6cd5\u3002<\/p>\n","protected":false},"excerpt":{"rendered":"
\u7532\u57fa\u5316\u200b\u53cd\u5e94 \u7b80\u8ff0 \u5728\u5408\u6210\u5b9e\u9a8c\u5ba4\uff0c\u5927\u5bb6\u7ecf\u5e38\u4f1a\u63a5\u89e6\u5230\u7532\u57fa\u5316\u53cd\u5e94\uff0c\u4e00\u822c\u7ecf\u5e38\u4f1a\u5bf9\u6c2e\u3001\u6c27\u3001\u786b\u4ee5\u53ca\u78b3\u8fdb\u884c\u7532\u57fa\u5316(\u4e5f\u53ef\u80fd\u5bf9\u7845\uff0c\u78f7\u7b49\uff0c\u8fd9\u91cc\u4e0d\u505a\u4ecb\u7ecd)\uff1b\u7ecf\u5e38… <\/p>\n","protected":false},"author":2,"featured_media":1554,"comment_status":"closed","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[3],"tags":[],"class_list":["post-1553","post","type-post","status-publish","format-standard","has-post-thumbnail","hentry","category-news"],"_links":{"self":[{"href":"http:\/\/www.bdmaee.cn\/wp-json\/wp\/v2\/posts\/1553"}],"collection":[{"href":"http:\/\/www.bdmaee.cn\/wp-json\/wp\/v2\/posts"}],"about":[{"href":"http:\/\/www.bdmaee.cn\/wp-json\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"http:\/\/www.bdmaee.cn\/wp-json\/wp\/v2\/users\/2"}],"replies":[{"embeddable":true,"href":"http:\/\/www.bdmaee.cn\/wp-json\/wp\/v2\/comments?post=1553"}],"version-history":[{"count":1,"href":"http:\/\/www.bdmaee.cn\/wp-json\/wp\/v2\/posts\/1553\/revisions"}],"predecessor-version":[{"id":1557,"href":"http:\/\/www.bdmaee.cn\/wp-json\/wp\/v2\/posts\/1553\/revisions\/1557"}],"wp:featuredmedia":[{"embeddable":true,"href":"http:\/\/www.bdmaee.cn\/wp-json\/wp\/v2\/media\/1554"}],"wp:attachment":[{"href":"http:\/\/www.bdmaee.cn\/wp-json\/wp\/v2\/media?parent=1553"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"http:\/\/www.bdmaee.cn\/wp-json\/wp\/v2\/categories?post=1553"},{"taxonomy":"post_tag","embeddable":true,"href":"http:\/\/www.bdmaee.cn\/wp-json\/wp\/v2\/tags?post=1553"}],"curies":[{"name":"wp","href":"http:\/\/api.w.org\/{rel}","templated":true}]}}