One‐pot synthesis of <i>N</i>²‐aminoprotected 6‐substituted and cycloalka[<i>d</i>] 4‐trifluoromethyl‐2‐acetylaminopyrimidines

Abstract

Abstract magnified image The one‐pot synthesis of a novel series of amino‐protected 6‐alkyl‐, 6‐aryl‐, 6‐heteroaryl‐ and 5,6‐fused‐cycloalkane 4‐trifluoromethyl‐2‐acetylaminopyrimidines, where alkyl = Me; aryl = Ph, 4‐CH 3 Ph, 4‐FPh, 4‐ClPh, 4‐BrPh, 4‐OCH 3 Ph, 4‐NO 2 Ph, 4,4′‐biphenyl, 1‐naphthyl; heteroaryl = 2‐thienyl, 2‐furyl and cycloalkyl = c ‐C 6 H 4 , c ‐C 7 H 5 from the reaction of substituted 4‐methoxy‐1,1,1‐trifluoroalk‐3‐en‐2‐ones with 1‐acetylguanidine in acetonitrile or propan‐2‐ol as solvent, is reported. The acetylamino group of 2‐acetylaminopyrimidines was hydrolyzed under three different conditions to afford the corresponding free 2‐aminopyrimidines.