公开(公告)号：NZ596724A

公开(公告)日：2013-06-28

申请号：NZ59672408

申请日：2008-04-30

Applicant: ABBOTT LAB

Inventor： LIU GANG ,  XIN ZHILI ,  KYM PHILLIP R

IPC: C07D487/04 ,  A61K31/519 ,  A61P3/04 ,  A61P3/10

Abstract: Disclosed herein is a process for preparaing amine and acetylene substituted [1,2,4] triazole [1,5,-a] pyrimidine compounds of general formula (I), wherein the substituents are as defined within the specification, the process comprising: coupling an aromatic halide of formula (1) with an alkyne of formula (2) in the presence of a base, a palladium catalyst and a copper (I) salt, to provide a compound of (3), or deprotonating a compound of formula (3a) in the presence of base and treating the resulting anion with ketones or aldehydes of formula (4) in a solvent, to provide a compound of formula (3b).