Biomolecules & Therapeutics

The Korean Society of Applied Pharmacology (한국응용약물학회)
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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)
  • Published : 2008.03.28
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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.

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References

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