Transition-metal-free radical difluorobenzylation/cyclization of unactivated alkenes: access to ArCF2-substituted ring-fused quinazolinones

Abstract

A mild and efficient transition-metal-free radical difluorobenzylation/cyclization of unactivated alkenes toward the synthesis of difluorobenzylated polycyclic quinazolinone derivatives with easily accessible α,α-difluoroarylacetic acids has been developed. This transformation has the advantages of wide functional group compatibility, a broad substrate scope, and operational simplicity. This methodology provided a highly attractive access to pharmaceutically valuable ArCF2-containing polycyclic quinazolinones.

Graphical abstract: Transition-metal-free radical difluorobenzylation/cyclization of unactivated alkenes: access to ArCF2-substituted ring-fused quinazolinones

Supplementary files

Article information

Article type
Paper
Submitted
18 Oct 2022
Accepted
22 Nov 2022
First published
23 Nov 2022

Org. Biomol. Chem., 2022, Advance Article

Transition-metal-free radical difluorobenzylation/cyclization of unactivated alkenes: access to ArCF2-substituted ring-fused quinazolinones

J. Yuan, M. Zhang, Y. Liu, W. Hu, L. Yang, Y. Xiao, X. Diao, S. Zhang and J. Mao, Org. Biomol. Chem., 2022, Advance Article , DOI: 10.1039/D2OB01904C

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