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http://dx.doi.org/10.4062/biomolther.2008.16.1.028

An Efficient Method for the Large-Scale Synthesis of Atorvastatin Calcium  

Lee, Hong-Woo (Chemical Process Research and Development Laboratory, Chemical Research Group, Chong Kun Dang Research Institute)
Kim, Young-Min (Chemical Process Research and Development Laboratory, Chemical Research Group, Chong Kun Dang Research Institute)
Yoo, Choong-Leol (Chemical Process Research and Development Laboratory, Chemical Research Group, Chong Kun Dang Research Institute)
Kang, Sung-Kwon (Chemical Process Research and Development Laboratory, Chemical Research Group, Chong Kun Dang Research Institute)
Ahn, Soon-Kil (Chemical Process Research and Development Laboratory, Chemical Research Group, Chong Kun Dang Research Institute)
Publication Information
Biomolecules & Therapeutics / v.16, no.1, 2008 , pp. 28-33 More about this Journal
Abstract
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.
Keywords
Atorvastatin; Large-scale synthesis; 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor; Hydrolysis;
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