Iodine-catalyzed oxidative annulation: facile synthesis of pyrazolooxepinopyrazolones via methyl azaarene sp3 C-H functionalization

作者：Zhang, Xin-Ke; Miao, Xiao-Yu; Zhou, Yu; Wang, Yu-Mei; Song, Ying-Chun; Liu, Hang; Xiong, Yi-Lu; Li, Ling-Yu; Wu, An-Xin; Zhu, Yan-Ping^*

来源：Organic and Biomolecular Chemistry, 2022, 20(6): 1236-1242.

DOI：10.1039/d1ob02436a

• C-SP3-H FUNCTIONALIZATION
• ALLENES
• CYCLIZATION
• INHIBITORS
• ACID

An iodine-catalyzed methyl azaarene sp(3) C-H functionalization has been developed for the synthesis of a seven-membered O-heterocyclic architecture containing three different heterocyclic aromatic hydrocarbons. This method can be applied to a wide range of substituted methyl azaarenes and diverse 2,4-dihydro-3H-pyrazol-3-ones, and brings about the efficient preparation of 2,9-dihydrooxepino[2,3-c:6,5-c ']dipyrazol-3(7H)-ones in high yields with the merits of low catalyst loading, good functional group tolerance and metal-free conditions.

• 单位
  烟台大学