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

Dedicated to Professor Alain Krief on the occasion of his 80^th birthday

Abstract

In 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 Introduction

2 Racemic Syntheses and Evaluation of Chiral Oxazinoindoles after Separation

3 Enantioselective Catalytic Syntheses of Oxazinoindoles

4 Conclusion

Key words

oxazinoindoles - bioactive molecules - chirality - chiral separation - asymmetric syntheses

Publication History

Received: 02 June 2022

Accepted after revision: 11 July 2022

Accepted Manuscript online:
11 July 2022

Article published online:
03 August 2022

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