KMID : 0606920080160010028
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Biomolecules & Therapeutics 2008 Volume.16 No. 1 p.28 ~ p.33
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An Efficient Method for the Large-Scale Synthesis of Atorvastatin Calcium
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Kim Young-Min
Yoo Chong-Leol Kang Sung-Kwon Ahn Soon-Kil Lee Hong-Woo
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Abstract
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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.
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KEYWORD
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Atorvastatin, Large-scale synthesis, 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor, Hydrolysis
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