Title of article :
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
Author/Authors :
Fujino، نويسنده , , Aya and Asano، نويسنده , , Masayoshi and Yamaguchi، نويسنده , , Hitomi and Shirasaka، نويسنده , , Naoki and Sakoda، نويسنده , , Akiko and Ikunaka، نويسنده , , Masaya and Obata، نويسنده , , Rika and Nishiyama، نويسنده , , Shigeru and Sugai، نويسنده , , Takeshi، نويسنده ,
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.
Keywords :
(R)-1-Benzyloxy-2-methylpropane-2 , Bicalutamide , kinetic resolution , 3-diol , Diol , epoxide hydrolase
