Department of Chemistry, Tianjin Key Laboratory of Molecular Optoelectronic Sciences, Frontiers Science Center for Synthetic Biology (Ministry of Education), and Tianjin Collaborative Innovation Centre of Chemical Science & Engineering, Tianjin University, Tianjin 300072, People's Republic of China.
Joint School of National University of Singapore and Tianjin University, International Campus of Tianjin University, Binhai New City, Fuzhou 350207, People's Republic of China.
J Org Chem. 2021 Feb 19;86(4):3574-3582. doi: 10.1021/acs.joc.0c02957. Epub 2021 Jan 28.
A EtN-triggered regioselective [3 + 2] cycloaddition reaction of 3-alkynoates with Seyferth-Gilbert reagent has been developed to furnish a series of trisubstituted pyrazole-3-phosphonates. A one-pot cycloaddition/alkylation sequence further offered access to the corresponding fully substituted pyrazoles.
已开发出一种 EtN 触发的炔丙酸盐与 Seyferth-Gilbert 试剂的区域选择性 [3 + 2] 环加成反应，以提供一系列三取代吡唑-3-膦酸酯。一锅加成/烷基化序列进一步提供了相应的完全取代吡唑。
