| 3-(2,3-二氢苯并呋喃-5-基)丙酸的合成 |
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| 引用本文： | 万杰,吴成龙,李梅,邓勇.3-(2,3-二氢苯并呋喃-5-基)丙酸的合成[J].中国医药工业杂志,2010,41(1). |
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| 作者姓名： | 万杰 吴成龙 李梅 邓勇 |
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| 作者单位： | 四川大学华西药学院,四川成都,610041 |
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| 摘 要： | 对甲苯酚在无水碳酸钾作用下与2-溴乙醛缩二乙醇缩合后经Friedel-Crafts反应、NBS溴代、与乌洛托品进行Sommelet反应,得苯并呋喃-5-甲醛,与丙二酸缩合后经10%钯炭在常压下催化氢化还原得雷美替胺的关键中间体3-(2,3-二氢苯并呋喃-5-基)丙酸,总收率约49%.
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| 关 键 词： | 3-(2 3-二氢苯并呋喃-5-基)丙酸 雷美替胺 褪黑素受体激动剂 失眠 中间体 合成 |
Synthesis of 3-(2,3-Dihydrobenzofuran-5-y1)propanoic Acid |
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| Authors: | WAN Jie WU Chenglong LI Mei DENG Yong |
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| Abstract: | 3-(2,3-Dihydrobenzofuran-5-y1)propanoic acid,a key intermediate for preparation of ramelteon,was synthesized by condensation of p-cresol with bromoacetaldehyde diethyl acetal in the presence of K_2CO_3,Friedel-Crafts reaction,bromination bv NBS and Sommelet reaction with hexamethylene tetramine to afford benzofuran-5-carbaldehyde,which was subsequently subjected to condensation with malonic acid and then hydrogenation under atmosphere pressure in the presence of 10% Pd-C with an overall yield ofabout 49%. |
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| Keywords: | 3-(2 3-dihydrobenzofuran-5-y1)propanoic acid ramelteon melatonin receptor agonist insomnia intermediate synthesis |
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