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.
Original language | English |
---|---|
Pages (from-to) | 979-983 |
Number of pages | 5 |
Journal | Tetrahedron Letters |
Volume | 48 |
Issue number | 6 |
DOIs | |
Publication status | Published - 2007 Feb 5 |
Keywords
- (R)-1-Benzyloxy-2-methylpropane-2,3-diol
- Bicalutamide
- Diol
- Epoxide hydrolase
- Kinetic resolution
ASJC Scopus subject areas
- Biochemistry
- Drug Discovery
- Organic Chemistry