Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development and Shanghai Key Laboratory of Green Chemistry and Chemical Processes, East China Normal University, Shanghai 200062, P. R. China.
State Key Laboratory of Organometallic Chemistry, Shanghai Institute of Organic Chemistry, Shanghai 200032, P. R. China.
J Org Chem. 2021 Jul 2;86(13):9206-9217. doi: 10.1021/acs.joc.1c00754. Epub 2021 Jun 15.
An unprecedented catalyst-free reaction of benzo[]thiophene-2,3-diones with difluoroenoxysilanes has been developed using either MeOH or HO as the solvent, which constitutes a facile and efficient protocol for the solvent-controlled divergent synthesis of five- and seven-membered -heterocycles featuring a -difluoromethylene group. A gram-scale synthesis and the diversification of the product transformations to other difluorinated -heterocycles further highlight its utility.
一种前所未有的苯并噻吩-2,3-二酮与二氟烯氧硅烷的无催化剂反应已经被开发出来,使用甲醇或水作为溶剂,这构成了一种简便高效的方法,用于控制溶剂的发散合成具有 -二氟亚甲基基团的五元环和七元环 -杂环化合物。克级规模的合成以及产物转化为其他氟化 -杂环化合物的多样化进一步突出了其用途。