Patent ID: 6562967
Filing Date: 2003-05-13
Classification: C07B,C07C,C07D

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; the substrate is racemic; 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, any unreacted substrate is racemic, and the enantiomeric excess of the product is greater than zero.