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\u7d27\u63a5\u7740\uff0c\u4f5c\u8005\u4e5f\u5bf9\u55b9\u5549N<\/em>-\u6c27\u5316\u7269\u5e95\u7269\u8303\u56f4\u8fdb\u884c\u4e86\u6269\u5c55\u3002\u5f53\u5728C-4\u6216C-7\u4f4d\u5177\u6709-CH3<\/sub>\u6216-OMe\u57fa\u65f6\uff0c\u5747\u4ee5\u4e2d\u7b49\u6536\u7387\u83b7\u5f97\u6240\u9700\u4ea7\u72693t<\/strong>–3v<\/strong>\u30025-Cl\u30014,7-C2<\/sub>\u62168-Br\u53d6\u4ee3\u7684\u55b9\u5549N<\/em>-\u6c27\u5316\u7269\uff0c\u4e5f\u53ef\u4ee540-68\uff05\u7684\u6536\u7387\u83b7\u5f97\u76ee\u6807\u4ea7\u72693w<\/strong>–3y<\/strong>\u3002\u7136\u800c\uff0c\u4f7f\u7528\u70f7\u57fa\u70ef\u70c3\u3001\u5421\u5576N<\/em>-\u6c27\u5316\u7269\u62162-\u82ef\u57fa\u5421\u5576N-<\/em>\u6c27\u5316\u7269\u4f5c\u4e3a\u5e95\u7269\u65f6\uff0c\u65e0\u6cd5\u83b7\u5f97\u6240\u9700\u7684\u4ea7\u7269\u3002<\/p>\n \u53d7\u4e0a\u8ff0\u7ed3\u679c\u7684\u542f\u53d1\uff0c\u4f5c\u8005\u8bbe\u60f3\uff0c\u662f\u5426\u53ef\u4ee5\u901a\u8fc7\u4f7f\u7528\u4e0d\u540c\u6dfb\u52a0\u5242\uff0c\u4ee5\u8131\u6c27\u7684\u65b9\u5f0f\u5f62\u6210\u6240\u9700\u7684\u787c\u5316\u4ea7\u7269\uff08Scheme 3\uff09\u3002\u968f\u540e\uff0c\u4f5c\u8005\u5f00\u59cb\u5bf9\u4e0d\u540c\u7684\u78b1\u8fdb\u884c\u4e86\u7b5b\u9009\uff08\u5982NaHCO3<\/sub>\uff0cNa2<\/sub>CO3<\/sub>\uff0cK3<\/sub>PO4<\/sub>\uff0cKOt<\/sup><\/em>Bu\u7b49\uff09\uff0c\u5176\u4e2dKOt<\/sup><\/em>Bu\u4f5c\u4e3a\u6700\u4f73\u7684\u78b1\u3002\u56e0\u6b64\uff0c\u4f5c\u8005\u4ee5\u82ef\u4e59\u70ef1a<\/strong>\u548c8-\u7532\u57fa\u55b9\u5549N<\/em>-\u6c27\u5316\u72692b<\/strong>\u4e3a\u5e95\u7269\uff0c\u5728\u7b2c\u4e8c\u6b65\u6dfb\u52a0KOt<\/sup><\/em>Bu\u5e76\u572880 \u2103\u6405\u62cc3 h\u540e\uff0c\u4ee580\uff05NMR\u6536\u7387\u5f62\u6210\u9884\u671f\u7684\u787c\u70f74a<\/strong>\uff08\u5206\u79bb\u4ea7\u7387\u4e3a60\uff05\uff09\u3002\u7531\u4e8e\u67d0\u4e9b\u542b\u787c\u70f7\u7684\u4ea7\u7269\u5728\u8272\u8c31\u67f1\u5206\u79bb\u540e\u53ef\u80fd\u4e0d\u7a33\u5b9a\uff0c\u56e0\u6b64\u5927\u591a\u6570\u4ea7\u72694<\/strong>\u7684NMR\u6536\u7387\u90fd\u5f97\u5230\u4e86\u4fdd\u8bc1\u3002\u82b3\u57fa\u73af\u4e0a\u7684\u4f9b\u7535\u5b50\u57fa\u56e2\uff08\u5982-Me\u3001i<\/sup><\/em>Bu\u548c-OMe\uff09\u3001\u5364\u7d20\uff08\u5982-F\u548c-Cl\uff09\u30012-\u7532\u57fa\u82ef\u4e59\u70ef\u30013,5-(MeO)2<\/sub>-\u53d6\u4ee3\u7684\u82ef\u4e59\u70ef\u3001\u4e59\u70ef\u57fa\u8418\u65f6\uff0c\u5747\u53ef\u83b7\u5f97\u4ea7\u72694b-4k<\/strong>\u3002\u7531\u4e8e\u5728\u55b9\u5549N<\/em>-\u6c27\u5316\u7269\u4e0d\u5e26\u6709\u53d6\u4ee3\u57fa\u6216\u5728\u5176\u4ed6\u4f4d\u7f6e\uff08\u5982C-4\u6216C-7\uff09\u5e26\u6709\u53d6\u4ee3\u57fa\u7684\u60c5\u51b5\u4e0b\uff0c\u787c\u70f7\u4ea7\u7269\u5728\u901a\u8fc7\u7845\u80f6\u67f1\u8272\u8c31\u7eaf\u5316\u65f6\u4e0d\u7a33\u5b9a\uff0c\u56e0\u6b64\uff0c\u4f5c\u8005\u5c06\u5176\u7528NaBO3<\/sub>\u00b74H2<\/sub>O\u6c27\u5316\u4e3a\u9187\u8fdb\u884c\u5206\u79bb\uff085l<\/strong>–5o<\/strong>\uff09\u3002\u5f53\u4f7f\u75285-Cl-\u55b9\u5549N<\/em>-\u6c27\u5316\u7269\u65f6\uff0c\u4ee540\uff05\u7684\u6536\u7387\u83b7\u5f97\u53bb\u787c\u5316\u7684\u4ea7\u72696<\/strong>\u3002\u6b64\u5916\uff0c8-\u6eb4\u55b9\u5549N<\/em>-\u6c27\u5316\u7269\u4e0e\u82ef\u4e59\u70ef\u5145\u5206\u53cd\u5e94\uff0c\u4ee544\uff05\u7684\u6536\u7387\u5f97\u52304q<\/strong>\uff0c\u5e76\u672a\u5f62\u6210\u8131\u787c\u4ea7\u72694q’<\/strong>\u3002<\/p>\n \u4e3a\u4e86\u8fdb\u4e00\u6b65\u8bc1\u660e\u53cd\u5e94\u7684\u5b9e\u7528\u6027\uff0c\u4f5c\u8005\u5bf9\u4ea7\u72694a<\/strong>\u8fdb\u884c\u4e86\u540e\u671f\u7684\u4fee\u9970\uff08Scheme 4\uff09\u3002\u5f53\u4f7f\u7528\u4e59\u70ef\u57fa\u683c\u6c0f\u8bd5\u5242\u53ef\u8fdb\u884c\u4e59\u70ef\u57fa\u5316\uff0c\u83b7\u5f9773\uff05\u6536\u7387\u7684\u4ea7\u72697<\/strong>\u3002\u800c\u5728Pd\u50ac\u5316\u4e0b\uff0c\u53ef\u5b9e\u73b0\u4e0e\u82b3\u57fa\u6eb4\u7684\u4ea4\u53c9\u5076\u8054\u83b7\u5f97\u82b3\u57fa\u5316\u4ea7\u72698<\/strong>\u3002\u82e5\u5728\u6b63\u4e01\u57fa\u9502\u5b58\u5728\u4e0b\u4e0eClCH2<\/sub>Br\u53cd\u5e94\uff0c\u53ef\u83b7\u5f97\u787c\u70f7\u4ea7\u72699<\/strong>\u3002<\/p>\n \u4e3a\u4e86\u9610\u660e\u53cd\u5e94\u673a\u7406\uff0c\u4f5c\u8005\u8fdb\u884c\u4e86\u76f8\u5173\u7684\u5bf9\u7167\u5b9e\u9a8c\uff08Scheme 5\uff09\u3002\u9996\u5148\uff0c\u5728\u6807\u51c6\u6761\u4ef6\u4e0b\uff0c\u4e0e\u55b9\u5549\u53cd\u5e94\u5e76\u672a\u83b7\u5f973a<\/strong>\uff0c\u8868\u660e\u8be5\u53cd\u5e94\u9700\u8981\u55b9\u5549N<\/em>-\u6c27\u5316\u7269\uff081\uff09\u3002\u5f53\u5728\u7b2c\u4e00\u6b65\u53cd\u5e94\u4e4b\u540e\uff0c\u5411\u53cd\u5e94\u6df7\u5408\u7269\u4e2d\u6dfb\u52a0\u81ea\u7531\u57fa\u6291\u5236\u5242TEMPO\uff0c3g<\/strong>\u6536\u7387\u964d\u4f4e\uff0c\u8bf4\u660e\u6d89\u53ca\u81ea\u7531\u57fa\u673a\u7406\uff082\uff09\u3002\u5206\u79bb\u51fa\u7684\u787c\u70f74a<\/strong>\u5728\u6807\u51c6\u6761\u4ef6\u4e0b\u4e0e\u82ef\u918c\u6216KOt<\/sup><\/em>Bu\u53cd\u5e94\uff0c\u5e76\u4e0d\u80fd\u8f6c\u5316\u4e3a3g<\/strong>\uff0c\u8868\u660e\u787c\u70f74a<\/strong>\u4e0d\u662f\u70ef\u70c33g<\/strong>\u7684\u4e2d\u95f4\u4f53\uff083-4\uff09\u3002<\/p>\n \u57fa\u4e8e\u524d\u4eba\u7684\u5de5\u4f5c\u4ee5\u53ca\u4e0a\u8ff0\u7684\u5bf9\u7167\u5b9e\u9a8c\uff0c\u4f5c\u8005\u63d0\u51fa\u4e86\u53ef\u80fd\u7684\u53cd\u5e94\u673a\u7406\uff08Scheme 6\uff09\u3002\u9996\u5148\uff0c\u70f7\u6c27\u57fa\u94dc\u914d\u5408\u726910<\/strong>\u4e0eB2<\/sub>pin2<\/sub>\u53cd\u5e94\uff0c\u5f62\u6210L-Cu-Bpin\u4e2d\u95f4\u4f5311<\/strong>\u300211<\/strong>\u4e0e\u70ef\u70c31a<\/strong>\u7684\u533a\u57df\u9009\u62e9\u6027\u52a0\u6210\uff0c\u5f62\u6210\u70f7\u57fa\u94dc\u4e2d\u95f4\u4f5312<\/strong>\u3002\u968f\u540e\uff0c\u55b9\u5549N<\/em>-\u6c27\u5316\u72692b<\/strong>\u4e2d\u7684\u4e9a\u80fa\u79bb\u5b50\u4e0e12<\/strong>\u53d1\u751f\u4eb2\u6838\u8fdb\u653b\uff0c\u5f62\u6210\u4e2d\u95f4\u4f5313<\/strong>\uff08\u8be5\u4e2d\u95f4\u4f53\u53ef\u4e0eB2<\/sub>pin2<\/sub>\u53cd\u5e94\u83b7\u5f97\u4e2d\u95f4\u4f5314<\/strong>\uff0c\u5e76\u518d\u751fL-Cu-Bpin\u914d\u5408\u726911<\/strong>\uff09\u3002\u6700\u540e\uff0c\u4e2d\u95f4\u4f5314<\/strong>\u82b3\u6784\u5316\u540e\uff0c\u7528KOt<\/sup><\/em>Bu\u6d88\u9664BpinOH\uff0c\u5f97\u52304a<\/strong>\u3002\u82e5\u5728\u82ef\u918c\u5b58\u5728\u4e0b\uff0c\u5219\u83b7\u5f973g<\/strong>\u3002\u5bf9\u4e8e14<\/strong>\u81f33g<\/strong>\u7684\u8be6\u7ec6\u673a\u5236\u5c1a\u4e0d\u6e05\u695a\u3002<\/p>\n<\/a><\/p>\n
\u6b63\u6587<\/h4>\n
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