Issue 11, 2024

Synthesis of pyrazino[1,2-b]indazoles via cascade cyclization of indazole aldehydes with propargylic amines

Abstract

An efficient intermolecular annulation of indazole aldehydes with propargylic amines has been developed for the synthesis of pyrazinoindazoles under catalyst- and additive-free conditions. This straightforward methodology was found to feature a wide substrate scope, high atom economy and environmental advantages. The bioactivity results of these new pyrazino[1,2-b]indazoles showed that some of them exhibited significant antifungal activity.

Graphical abstract: Synthesis of pyrazino[1,2-b]indazoles via cascade cyclization of indazole aldehydes with propargylic amines

Supplementary files

Article information

Article type
Paper
Submitted
10 Jan 2024
Accepted
07 Feb 2024
First published
07 Feb 2024

Org. Biomol. Chem., 2024,22, 2226-2230

Synthesis of pyrazino[1,2-b]indazoles via cascade cyclization of indazole aldehydes with propargylic amines

Z. Wu, H. Qu, B. Han, J. Yang, X. Chang and C. Feng, Org. Biomol. Chem., 2024, 22, 2226 DOI: 10.1039/D4OB00051J

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