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氟伐他汀钠的合成
引用本文:蔡正艳,宁奇,周伟澄. 氟伐他汀钠的合成[J]. 中国医药工业杂志, 2007, 38(2): 73-75
作者姓名:蔡正艳  宁奇  周伟澄
作者单位:上海医药工业研究院,上海,200437
摘    要:氟苯和氯乙酰氯经付-克酰化、与N-异丙基苯胺缩合后环合,得3-(4-氟苯基)-1-异丙基-1H-吲哚,再经Vilsmeier-Haack反应、与乙酰乙酸甲酯缩合、选择性还原后水解成盐得HMG CoA还原酶抑制剂类降血脂药氟伐他汀钠,总收率约26%。

关 键 词:氟伐他汀钠  HMG CoA还原酶抑制剂  降血脂药  合成
文章编号:1001-8255(2007)02-0073-03
修稿时间:2006-10-19

Synthesis of Fluvastatin Sodium
CAI Zheng-yan,NING Qi,ZHOU Wei-cheng. Synthesis of Fluvastatin Sodium[J]. , 2007, 38(2): 73-75
Authors:CAI Zheng-yan  NING Qi  ZHOU Wei-cheng
Affiliation:Shanghai Institute of Pharmaceutical Industry, Shanghai 200437
Abstract:Fluvastatin sodium, an antihypercholesterolemic HMG CoA reductase inhibitor, was synthesized from fluorobenzene by Friedel-Crafts acylation with chloroacetyl chloride, followed by condensation with N-isopropyl aniline and cyclization to give 3-(4-fluorophenyl)-1-isopropyl-1H-indole, which was subjected to Vilsmeier-Haack reaction, condensation with methyl acetoacetate, selective reduction, hydrolysis and salt formation with an overall yield of 26%.
Keywords:fluvastatin sodium   HMG CoA reductase inhibitor   antihypercholesterolemic   synthesis
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