A New Multicomponent Domino Transformation of 1,3-Dicarbonyl Compounds: One-Pot Regio-, Chemo- and Stereoselective Access to Valuable α,γ-Difunctionalized α-Ketoesters and Amides

A new multi-component transformation between 1,3-dicarbonyls 1, aldehydes 2, and allylic, propargylic or benzylic halides 3 is described. It provides a regio-, chemo- and stereoselective one-pot access to α,γ-difunctionalized α-ketoesters and amides 4, bearing a quaternary center valuable for further synthetic transformations via ring-closing metathesis to give azaspiro systems found in bioactive natural products.