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1. Enzyme-catalyzed asymmetric deacylation for the preparation of lasofoxifene (CP-336156), a selective estrogen receptor modulator.

Author

Yang X, Reinhold AR, Rosati RL, and Liu KK

Subjects
Catalysis, Dealkylation, Hydrolysis, Stereoisomerism, X-Ray Diffraction, Pyrrolidines chemical synthesis, Selective Estrogen Receptor Modulators chemical synthesis, Tetrahydronaphthalenes chemical synthesis
Abstract

[structure] selective estrogen receptor modulator (SERM), Lasofoxifene (CP-336156), was prepared by an enzyme-catalyzed asymmetric deacylation with high optical purity and excellent yield even though the hydrolytic site is remote from the chiral centers.

Published
2000
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