Patent ID: 6261830
Filing Date: 2001-07-17
Classification: A61P,C07C,C12P

Abstract:
A method of preparing an enantiomer of 3,3,3-trifluoro-2-hydroxy-2-methyl propanoic acid from a racemic compound of Formula VII ##STR21##wherein:A is selected from CN, COH, CH(OR.sup.3).sub.2, COR.sup.4, COOR.sup.5, CONH.sub.2, CONHR.sup.6 and CONR.sup.7 R.sup.8 ;R.sup.3, R.sup.4, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 are selected from alkyl, aryl, and aralkyl, wherein R.sup.3, R.sup.4, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 may at each occurrence be substituted with one or more substituents selected from hydroxy, halogen, cyano, (C.sub.1 -C.sub.4)alkoxy, (C.sub.1 -C.sub.4)alkylamino and (C.sub.1 -C.sub.4)dialkylamino, andR.sup.5 is selected from (C.sub.1 -C.sub.10)alkyl, (C.sub.1 -C.sub.4)alkoxy and phenyl; said method comprising the steps of:a) treating said compound of Formula VII with a stereoselective hydrolase enzyme to provide a mixture of an alcohol of Formula VIII and an ester of Formula IX ##STR22##wherein A and R.sup.9 are as defined above, and * is an optically active chiral center;b) separating said compounds of formula VIII and Formula IX, andc) converting said compound of Formula VIII to an acid by converting moiety A to a carboxyl group.