Patent ID: 7339058
Filing Date: 2008-03-04
Classification: C07D

Abstract:
1. An improved process for the preparation of an N-([1,2,4]triazolopyrimidin-2-yl)aryl sulfonamide of formula I: wherein X represents CH or N; Y represents CZ or N with the proviso that only one of X or Y is N; W represents H or OR with the proviso that when Y represents CZ, then W represents H; Z represents OR; R represent CH Ar represents wherein A and B independently represent H, halo, CF D represents H, halo or R; E and G represent S or CB with the proviso that one of E or G is S; and R which comprises combining a sulfonyl chloride compound of the formula: wherein Ar is defined as above with an amine compound of the formula: wherein R, X, Y and W are defined as above in the presence of an aromatic tertiary amine base and a catalytic amount of an N-aryl-sulfilimine compound of the formula: wherein R, X, Y and W are defined as above; R R wherein the improvement comprises using 3-picoline or 3,5-lutidine as the aromatic tertiary amine base.