盐酸乙氟利嗪的合成 |
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引用本文: | 杜翔宇,王晰婷,孙海龙,马丽芳.盐酸乙氟利嗪的合成[J].中国医药工业杂志,2011,42(5). |
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作者姓名: | 杜翔宇 王晰婷 孙海龙 马丽芳 |
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作者单位: | 四川大学化学工程学院,四川成都,610065 |
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摘 要: | 1-双(4-氟苯基)甲基]哌嗪和氯乙氧基乙酸乙酯在碘化钾催化下,以三乙胺作缚酸剂,于二甲苯中缩合制得2-2-4-双(4-氟苯基)甲基]-1-哌嗪基]乙氧基]乙酸乙酯,再经水解、成盐酸盐制得组胺H<,1>受体拮抗剂盐酸乙氟利嗪,总收率约78%.
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关 键 词: | 盐酸乙氟利嗪 组胺H1受体拮抗剂 合成 |
Synthesis of Efletirizine Hydrochloride |
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Authors: | DU Xiangyu WANG Xiting SUN Hailong MA Lifang |
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Institution: | DU Xiangyu,WANG Xiting,SUN Hailong,MA Lifang(College of Chemical Engineering,Sichuan University,Chengdu 610065) |
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Abstract: | Efletirizine hydrochloride,a histamine H1 receptor antagonist,was synthesized from ethyl(2-chloroethoxy)acetate by condensation with 1-bis(4-fluorophenyl)methyl]piperazine in the presence of potassium iodide and triethylamine in xylene to give ethyl 2-2-4-bis(4-fluorophenyl)methyl]-1-piperazinyl]ethoxy]acetate,followed by hydrolysis and salt formation with an overall yield of about 78%. |
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Keywords: | efletirizine hydrochloride histamine H1 receptor antagonist |
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