Patent ID: 8158806
Filing Date: 2012-04-17
Classification: A61P,C07D

Abstract:
1. A process for preparing diaminoketothiazole (DAT1), of the following formula, wherein Ar represents 4-OMe-C 6 H 4 and Ar′ represents C 6 H 5 comprising: reacting aminomethylpolystyrene beads and 1-[N-(arylthiocarbamoyl) amidino]-3,5-dimethylpyrazole to produce N-(N-arylthiocarbamoyl)-N-guanidinomethyl polystyrene; reacting said N-(N-arylthiocarbamoyl)-N-guanidinomethyl polystyrene with an α-haloketone in the presence of a base which produces an acyclic S-alkyl intermediate derivative; subjecting the acyclic S-alkyl intermediate derivative to the step of cyclisation to obtain an intermediate cyclic thiazoline; subjecting the cyclic thiazoline intermediate to the step of eliminative aromatization to produce diaminoketothiazole in a solution; filtering said solution to remove impurities; and then isolating 5-aroyl-4-amino-2-arylaminothiazoles from the solution by precipitation.