General synthesis of substituted 1,2-dihydropyridines

Abstract

A general and practical metal-free protocol for the synthesis of 1,2-dihydropyridines with wide structural/functional diversity at the ring and featuring mono, double, or spiro substitution at the sp3 position is described. The protocol entails a microwave-assisted domino reaction of a propargyl vinyl ether (secondary or tertiary) and a primary amine (aliphatic or aromatic) in toluene or methanol. © 2014 American Chemical Society.This research was supported by the Spanish Ministerio de Economı́a y Competitividad (MICINN) and the European Regional Development Fund (CTQ2011-28417-C02-02). L.C. and G.M.-A. thank the Spanish MEC for FPI and FPU grants, respectively.Peer Reviewe