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Asymmetric Synthesis of CF3-Substituted β-Hydroxyketones and 1,3-Diols by Engineered Ketoreductases
Yangyang Li1, Sizhe Yu1, Yingqian Jiang1
1Wuya College of Innovation, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenhe, Shenyang 110016, People's Republic of China.
Abstract:
Chiral CF3-substituted β-hydroxy ketones and 1,3-diols were prepared via the ketoreductase-catalyzed asymmetric reduction of the corresponding benzoyl trifluoroacetones. The variants of two ketoreductases, LfSDR1 and CgKR1, were screened or engineered for stereocomplementary synthesis of CF3-substituted β-hydroxy ketones with up to >99% conversions and up to >99% enantiomeric excess (ee) values. In addition, the cascade reduction or one pot reduction of diketones could afford the CF3-substituted 1,3-diols with up to >99% ratios and >99% ee values.
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