Bacillus subtilis epoxide hydrolase-catalyzed preparation of enantiopure 2-methylpropane-1,2,3-triol monobenzyl ether and its application to expeditious synthesis of (R)-bicalutamide |
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| Authors: | Aya Fujino Hitomi Yamaguchi Akiko Sakoda Rika Obata Takeshi Sugai |
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| Affiliation: | a Department of Chemistry, Keio University, 3-14-1, Hiyoshi, Kohoku-ku, Yokohama 223-8522, Japan
b Research and Development Center, Nagase & Co., 2-2-3, Murotani, Nishi-ku, Kobe 651-2241, Japan |
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| Abstract: | Expeditious synthesis of (R)-bicalutamide (1), a synthetic antiandrogen, from enantiopure 2-methylpropane-1,2,3-triol monobenzyl ether (4) was achieved. An engineered Bacillus subtilis epoxide hydrolase worked enantioselectively on the racemic epoxide (7) to provide the above starting material in highly enantiomerically enriched state. |
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| Keywords: | Epoxide hydrolase (R)-1-Benzyloxy-2-methylpropane-2,3-diol Kinetic resolution Diol Bicalutamide |
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