富马酸依利色林的合成 |
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引用本文: | 张越,李玲,罗振福,乌恩.富马酸依利色林的合成[J].中国医药工业杂志,2010,41(2). |
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作者姓名: | 张越 李玲 罗振福 乌恩 |
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作者单位: | 1. 内蒙古医学院药学院,内蒙古呼和浩特,010059 2. 天津药物研究院化药部,天津,300193 |
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摘 要: | N-(2-氯乙基)二甲胺盐酸盐和丙酮肟钠反应后水解制得O-(2-二甲胺基乙基)羟胺二盐酸盐(5);另用邻氟苯乙酮和对羟基苯甲醛经缩合得到(E)-1-(2-氟苯基)-3-(4-羟基苯基)-2-丙烯-1-酮(8).5和8缩合得到的依利色林与富马酸成盐,制得镇静催眠药富马酸依利色林,总收率约47%.
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关 键 词: | 富马酸依利色林 镇静催眠药 5-HT_(2A)受体拮抗剂 合成 |
Synthesis of Eplivanserin Fumarate |
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Authors: | ZHANG Yue LI Ling LUO Zhenfu WU En |
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Abstract: | Eplivanserin fumarate,a sedative-hypnotic drug was synthesized from N-(2-chloroethyl)-dimethyl amine hydrochloride by reaction with acetoxime sodium and then hydrolysis to give the key intermediate O-(2-dimethylaminoethyl)hydroxylamine dihydrochloride(5),which was subjected to condensation with(E)-1-(2-fluorophenyl)-3-(4-hydroxyphenyl)-2-propen-1-one(8)followed by treatment with fumaric acid in 47% overall yield. |
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Keywords: | eplivanserin fumarate sedative-hypnotic drug 5-HT_(2A) receptor antagonist synthesis |
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