PROCESS FOR PREPARING 1-(6-METHYLPYRIDIN-3-YL)-2- (4-(METHYLSULPHONYL) PHENYL] ETHANONE

摘要

A five-step process for preparing 1-(6-methylpyridin-3-yl) -2-[(4-methylsulphonyl)phenyl] -ethanone of formula (I) described; characterized in that a) 4-(methylthio) benzyl alcohol is converted with hydrochloric acid into 4-(methylthio) benzyl chloride, b) 4-(methylthio) benzyl chloride is converted with an alkali metal cyanide into 4-(methylthio) phenylacetonitrile, c) 4-(methylthio) -phenylacetonitrile is condensed with a 6-methylnicotinic ester to give 3-[2- (4-methylthio) phenyl) -2-cyanoacetyl] (6-methyl) -pyridine, d) 3-[2-(4-methylthio) phenyl)-2-cyanoacetyl] (6-methyl) -pyridine is hydrolysed and decarboxylated under acidic conditions to give 3-[2-(4-methylthio) phenyl) acetyl] (6-methyl) pyridine and, e) 3-[2(4-(methylthio) phenyl) acetyl] (6-methyl) pyridine is oxidized to give the end product. The compound of formula (I) is an intermediate for preparing COX-2 inhibitors, pharmaceutically active compounds having analgesic and antiinflammatory action.