Patent ID: 6562966
Filing Date: 2003-05-13
Classification: C07B,C07C,C07D,Y02P

Abstract:
A method of kinetic resolution represented by Scheme 1: whereinX represents NRâ€², O, or S; Y represents independently for each occurrence O or S; Z represents NRâ€², O, or S; R represents independently for each occurrence hydrogen, or optionally substituted alkyl, aryl, heteroaryl, aralkyl, or heteroaralkyl; Râ€² represents independently for each occurrence R, formyl, acyl, sulfonyl, â€”CO2R, or â€”C(O)NR2; the substrate and the product are chiral; NuH represents water, an alcohol, a thiol, an amine, a &bgr;-keto ester, a malonate, or the conjugate base of any of them; chiral non-racemic catalyst is a chiral non-racemic tertiary amine, phosphine, or arsine; n is 1 or 2; and when said method is completed or interrupted, the enantiomeric excess or diastereomeric excess of the unreacted substrate is greater than that of the substrate prior to the kinetic resolution, the enantiomeric excess or diastereomeric excess of the product is greater than zero, or both.