Preparation of (R)-3-quinuclidinol from (R,S)-3-quinuclidinol

摘要

Preparation of (R)-3-quinuclidinol (Ia) from (R,S)-3-quinuclidinol (I) comprises converting (I) to (S)-3-quinuclidinyl butyrate by reaction with vinyl butyrate in the presence of a subtilisin-protease, so that enantiomerically pure (Ia) is enriched and isolated. A crystalline subtilisin-protease which is crosslinked with glutaraldehyde is preferably used. The amount of enzyme used is 0.5-5 wt.% based on (I). The reaction is carried out in an organic solvent (especially 2-methyl-3-butanol) at -10 to 80 deg C.