Issue 21, 2021

Palladium-catalyzed carbonylative synthesis of 5-trifluoromethyl-1,2,4-triazoles from trifluoroacetimidohydrazides and aryl iodides

Abstract

A palladium-catalyzed three-component carbonylative reaction of trifluoroacetimidohydrazides and aryl iodides for the synthesis of pharmaceutically valuable 5-trifluoromethyl-1,2,4-triazoles has been achieved. The reaction is characterized by a low catalyst loading amount, a broad substrate scope, high efficiency, no participation of CO gas and good application prospects. The protocol has been successfully applied to prepare the bioactive molecule GlyT1 inhibitor.

Graphical abstract: Palladium-catalyzed carbonylative synthesis of 5-trifluoromethyl-1,2,4-triazoles from trifluoroacetimidohydrazides and aryl iodides

Supplementary files

Article information

Article type
Research Article
Submitted
19 Jul 2021
Accepted
04 Sep 2021
First published
06 Sep 2021

Org. Chem. Front., 2021,8, 6089-6094

Palladium-catalyzed carbonylative synthesis of 5-trifluoromethyl-1,2,4-triazoles from trifluoroacetimidohydrazides and aryl iodides

J. Tang, J. Zhang, Y. Zhang, Z. Chen and X. Wu, Org. Chem. Front., 2021, 8, 6089 DOI: 10.1039/D1QO01064F

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