Metal-free decarboxylative acylation of isoquinolines using α-keto acids in water

Abstract

An efficient method for acylation of isoquinolines has been developed using α-ketoacids under metal- and additive-free conditions in water. The protocol involves C(sp2)–H functionalization of isoquinolines providing an easy access to C1-benzoylated isoquinolines, which constitute the core structure of a number of biological active compounds and serve as key intermediate in the synthesis of many alkaloids. © 2017 Elsevier Ltd