Chiral 1,4-Oxazino[4,3-a]indoles as a Challenging Scaffold: Syntheses and Properties

Abstract

AbstractIn the last few decades, there has been an increasing interest in the development of new syntheses of oxazinoindoles, a tricyclic backbone bearing an indole core structure fused with a morpholine ring, in particular because these molecules have interesting bioactive properties, such as antidepressant, anti-inflammatory, or antitumor activity. There are a few reported racemic strategies for the synthesis of oxazinoindoles, but only four reports of enantioselective syntheses. This short review presents an overview of these enantioselective strategies as well as the evaluation of chiral oxazinoindoles for their bioactive properties.1 Introduction2 Racemic Syntheses and Evaluation of Chiral Oxazinoindoles after Separation3 Enantioselective Catalytic Syntheses of Oxazinoindoles4 Conclusion