Synthesis of pseudoindoxyls by asymmetric aza-Heck cyclization

Abstract

Pseudoindoxyl is a nitrogen-containing compound and a kind of the indole derivatives. Numerous natural alkaloids with versatile biological activity contain pseudoindoxyl carbon skeleton. The complex structure of pseudoindoxyl has motivated chemists, prompting the exploration and refinement of various synthetic methods. However, relatively narrow substrate scope extremely limits their application to total synthesis of natural products. Our group is dedicated to develop aza-Heck reaction into various circumstances and we found aza-Heck can be utilized in synthesizing pseudoindoxyls under excellent yield and ee to obtain desired chiral structure. In this document, I will first introduce some well-developed methodologies all over the world and then demonstrate our group and my contribution in the development of pseudoindoxyls syntheses via aza-Heck cyclization.