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Transition-metal-free radical difluorobenzylation/cyclization of unactivated alkenes: access to ArCF 2 -substituted ring-fused quinazolinones.

Jin-Wei YuanMei-Yue ZhangYan LiuWen-Yu HuLiang-Ru YangYong-Mei XiaoXiao-Qiong DiaoShou-Ren ZhangJian Mao
Published in: Organic & biomolecular chemistry (2022)
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 ArCF 2 -containing polycyclic quinazolinones.
Keyphrases
  • transition metal
  • molecular docking
  • structure activity relationship
  • structural basis