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PIDA-Mediated Rearrangement for the Synthesis of Enantiopure Triazolopyridinones

Zenghui Ye, Hong Zhang, Na Chen, Yanqi Wu and Fengzhi Zhang*

*College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310014, P.R. China, Email: zhangfengzhizjut.edu.cn

Z. Ye, H. Zhang, N. Chen, Y. Wu, F. Zhang, Org. Lett., 2020, 22, 6464-6467.

DOI: 10.1021/acs.orglett.0c02278


Abstract

A tandem oxidative cyclization/1,2-carbon migration of a broad scope of hydrazides enables the synthesis of otherwise inaccessible hindered or enantiopure triazolopyridinones with retention of configuration. This protocol can be easily scaled up by continuous flow synthesis under mild conditions.


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Key Words

fused N-heterocycles, PIDA


ID: J54-Y2020