Synthesis of 7-cycloalkylimino substituted 3-amino-6-fluoro-2-methyl-3H- quinazolin-4-ones

Abstract

A versatile pathway for the synthesis of 7-cycloalkylimino substituted 3-amino-6-fluoro-2-methyl-3H-quinazolin-4-ones from 4,5-difluoroanthranylic acid has been advanced. Nucleophilic amination-defluorination reaction of the 6,7-difluoro derivative of 3-amino-2-methyl-3H-quinazolin-4-one has been established to occur at position 7, as shown by X-ray crystallographic analysis. © 2012 Elsevier B.V.