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

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...

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Veröffentlicht in:Organic & biomolecular chemistry 2022-12, Vol.20 (48), p.9722-9733
Hauptverfasser: Jin-Wei, Yuan, Mei-Yue, Zhang, Liu, Yan, Wen-Yu, Hu, Liang-Ru, Yang, Yong-Mei, Xiao, Xiao-Qiong Diao, Shou-Ren, Zhang, Mao, Jian
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Sprache:eng
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Zusammenfassung: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.
ISSN:1477-0520
1477-0539
DOI:10.1039/d2ob01904c