Key Laboratory of Organo-Pharmaceutical Chemistry of Jiangxi Province, Gannan Normal University, Ganzhou 341000, China.
J Org Chem. 2023 Feb 17;88(4):2190-2206. doi: 10.1021/acs.joc.2c02610. Epub 2023 Feb 1.
A copper-promoted aerobic oxidative [3+2] cycloaddition reaction for the synthesis of various substituted pyrazoles from N,N-disubstituted hydrazines with alkynoates in the presence of bases is developed. This work involves a direct C(sp)-H functionalization and the formation of new C-C/C-N bonds. In this strategy, inexpensive and easily available CuO serves as the promoter and air acts as the green oxidant. The reaction exhibits the advantages of high atom and step economy, high regioselectivity, and easy operation.
发展了一种铜促进的有氧氧化[3+2]环加成反应，用于在碱的存在下，从 N,N-二取代腙与炔酸酯合成各种取代的吡唑。这项工作涉及直接 C(sp)-H 官能化和新的 C-C/C-N 键的形成。在该策略中，廉价且易得的 CuO 用作促进剂，空气作为绿色氧化剂。该反应具有原子经济性和步骤经济性高、区域选择性高、操作简便等优点。
