| 摘要 |
PURPOSE:To profitably obtain the subject optically active compound useful as a raw material for the intermediates of medicines such as a calcium- antagonistic agent, etc., by reacting a 3-hydroxypyrrolidine compound with a carboxylic acid ester in the presence of an esterase. CONSTITUTION:A pyrrolidine compound of formula I (R is alkyl, aryl, aralkyl) (e.g. N-benzyl-3-pyrrolidinol) is reacted with a carboxylic acid ester (e.g. vinyl acetate) of formula: R<1>COOR<2> (R<1> is 1-5C alkyl which may be halogenated; R<2> is alkenyl which may be replaced with an aryl group) in the presence of an esterase such as the lipase of the genus Arthrobacter bacterium at 25 deg.C with stirring, and the reaction is stopped at the time of 55hrs after the start of the stirring. The reaction product is filtered, and the filtrate is concentrated under vacuum and subsequently subjected to separation and purification treatments by column chromatography to obtain the mixture of the optically active pyrrolidine compound of formula II with the optically active pyrrolidine compound of formula III. |
