A “neat” synthesis of substituted 2-hydroxy-pyrido[1,2-a]pyrimidin-4-ones

Abstract

We report the synthesis of a series of substituted 2-hydroxy-pyrido[1,2-a]pyrimidin-4-ones through a condensation of 2-aminopyridines and diethyl malonate. This method is contrasted with three reported general procedures for the preparation of these compounds, revealing that simple, “neat” synthesis conditions are suitable for a number of derivatives, including halogenated compounds suitable for further functionalization. Environmental, safety, and economic factors were considered in exploring this effective and robust synthetic method.