Patent ID: 8575343
Filing Date: 2013-11-05
Classification: C07D

Abstract:
1. A process for the preparation of (E)-N-(4-(4-fluorophenyl)-6-isopropyl-5-(3-oxoprop-1-enyl)pyrimidin-2-yl)-N-methylmethanesulfonamide of formula I which comprises: (a) Treating N-(4-(4-fluorophenyl)-5-formyl-6-isopropylpyrimidin-2-yl)-N-methyl methane-sulfonamide of formula III with a compound selected from wherein R Y is selected from M, MX, BR wherein M is selected from alkali, Zn, Mg, Sn and Si; X is selected from CI, Br and I; R wherein R′ is a group of formula V with R R″ is a heteroaryl group, in an inert solvent, optionally in the presence of a promoter, to obtain compound of formula VI: (b) oxidative cleavage of the aliphatic carbon-carbon double bond of the obtained compound of formula VI and optionally isolating intermediate of formula VII; (c) dehydration of intermediate of formula VII; and (d) isolation of compound of formula I.