An efficient method for the large-scale synthesis of atorvastatin calcium

被引：13

作者：

Lee, Hong Woo ^{[1
]}

Kim, Young Min ^{[1
]}

Yoo, Choong Leol ^{[1
]}

Kanq, Sung Kwon ^{[1
]}

Ahn, Soon Kil ^{[1
]}

机构：

[1] Chong Kun Dang Res Inst, Chem Res Grp, Chem Proc Res & Dev Lab, Cheonan 330831, South Korea

来源：

BIOMOLECULES & THERAPEUTICS | 2008年 / 16卷 / 01期

关键词：

atorvastatin; large-scale synthesis; 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor; hydrolysis;

D O I：

10.4062/biomolther.2008.16.1.028

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Atorvastatin calcium salt (1) was obtained through the preparation of lactone compound (8) from 2-((4R,6R)-6-(2-(2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4-(phenylcarbamoyl)-1H-pyrrol-1-yl)-ethyl)-2-phenyl-1,3,2-dioxaborinan-4-yl)acetic acid tert-butyl ester (9) by hydrolysis in basic condition. Efficient hydrolysis of boronate compound 9 aimed at the viable synthesis for commercial production and purification of Atorvastatin calcium is reported. Detail studies of evaluation procedure are also reported.

引用

页码：28 / 33

页数：6

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