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1. (WO2011029762) PROCESS FOR PREPARING ALPHA-CARBOXAMIDE DERIVATIVES

Pub. No.:    WO/2011/029762    International Application No.:    PCT/EP2010/062826
Publication Date: Fri Mar 18 00:59:59 CET 2011 International Filing Date: Thu Sep 02 01:59:59 CEST 2010
IPC: C07D 207/16
Applicants: CONVERGENCE PHARMACEUTICALS LIMITED
ZAJAC, Matthew, Allen
Inventors: ZAJAC, Matthew, Allen
Title: PROCESS FOR PREPARING ALPHA-CARBOXAMIDE DERIVATIVES
Abstract:
The present application provides a process for the preparation of α-carboxamide pyrrolidine derivatives of formula (I), wherein R1 and R2 are independently hydrogen, C1-6alkyl or C3-6cycloalkylC1-6alkyl; or such R1 and R2, together with the nitrogen to which they are attached, may form an unsubstituted 3-, 4-, 5- or 6-membered saturated ring; X is carbon or nitrogen; n is 0, 1 or 2, wherein when present each R5 is independently selected from the list consisting of C1-3alkyl, halogen, cyano, haloC1-3alkyl, hydroxy, C1-3alkoxy and C1-3haloalkoxy; either R6 or R7 is -O-R8, -OCHR9R8, -NCH2R8 or -(CH2)2R8 wherein the other R6 or R7 is hydrogen or R5; and wherein R8 is a phenyl ring or wherein the phenyl ring is optionally substituted by one or more groups independently selected from the list consisting of C1-3alkyl, halogen, cyano, haloC1-3alkyl, hydroxy, C1-3alkoxy and C1-3haloalkoxy; and R9 is hydrogen or C1-3alkyl.