Patent ID: 7563888
Filing Date: 2009-07-21
Classification: A61P,C07D,Y02P

Abstract:
1. A process for the preparing of diphenylazetidinone derivative of formula (I), wherein: X is OH; R R R R n is an integers from 4 to 16; R R m is an integers from 1 to 5; comprising (a) reacting a compound of formula (II) wherein: Y is H, OH; H, O-acetyl; H, OSi(alkyl) with an imine of formula (III) wherein R R to give a compound of formula (IV) (b) hydrolyzing the compound of formula (IV) to give a compound of formula (V) wherein R (c) optionally converting the compound of formula (V) wherein R 9 is H into a compound of formula (V) wherein R 9 is (C 1 -C 4 )alkyl, CO(C 1 -C 4 )alkyl, COO(C 1 -C 4 )alkyl, or SO 2 aryl, or into a corresponding anhydride; (d) cyclizing the compound of formula (V) wherein R 9 is H, (C 1 -C 4 )alkyl, CO(C 1 -C 4 )alkyl, COO(C 1 -C 4 )alkyl, or SO 2 aryl, or the anhydride to give a lactam of formula (VI) (e) optionally deprotecting the compound of formula (VI) wherein Y is H, O-acetyl; H, OSi(alkyl) R R to give the compound of formula (I) wherein R 2 is F, CH 2 CH 3 , or CH 2 NH 2 ; and (f) optionally reacting the compound of formula (I) wherein R 2 is CH 2 NH 2 with a compounds of formula (XV) or (XVI) to give the compound of the formula (I) wherein R 2 is CH 2 NHR 4 ; and R 4 is H, CO—(CH 2 —) n CO—R 5 , or CO—(CH 2 —) n NHR 6 .