Aza-Povarov Reaction. A Method for the Synthesis of Fused Tetracyclic Chromeno[4,3-d]pyrido[1,2-a]pyrimidines.

Abstract

A cornerstone in drug discovery is the development of strategies to provide privileged small molecules with specific structural and stereochemical complexity, allowing access to new potential therapeutic entities. In this work, a new strategy based on the [4 + 2] Povarov reaction involving 1,3-diazadiene was developed. This approach is applied for a straightforward procedure in the preparation of chromeno[4,3-d]pyrido[1,2-a]pyrimidine derivatives, with accessible substrates, 2-aminopyridine and unsaturated aldehydes, and excellent atom economy to obtain four fused ring heterocycles, in a regio- and diastereoselective way.