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

Abstract

In the last decades, an increasing interest in the development of new syntheses of oxazinoindoles, a tricyclic backbone bearing an indole core structure fused with a morpholine ring, have been studied. In particular because these molecules often present interesting bioactive properties such as antidepressant, anti-inflammatory or antitumor activity. In the literature, a few racemic strategies have been reported so far but only four publications have discussed the enantioselective synthesis of this type of scaffold. In this short review, an overview of these enantioselective strategies will be discussed as well as the evaluation of chiral oxazinoindoles for their bioactive properties. 1. Introduction 2. Racemic syntheses and evaluation of chiral oxazinoindoles after separation 3. Enantioselective catalytic syntheses of oxazinoindoles 4. Conclusion