Kanemoto Kazuya, Yoshida Suguru, Hosoya Takamitsu
Laboratory of Chemical Bioscience, Institute of Biomaterials and Bioengineering , Tokyo Medical and Dental University (TMDU) , 2-3-10 Kanda-Surugadai , Chiyoda-ku, Tokyo 101-0062 , Japan.
Org Lett. 2019 May 3;21(9):3172-3177. doi: 10.1021/acs.orglett.9b00875. Epub 2019 Apr 19.
A mild and odorless copper-catalyzed thiolation of terminal alkynes with thiosulfonates is described. The broad substrate scope provides convenient access to a wide variety of sulfur-containing heterocycles. In particular, divergent benzoheteroles are efficiently prepared in a simple manner by thiolation of ethynylbenzenes bearing ortho-nucleophilic functional groups followed by iodocyclization.
本文描述了一种温和且无臭的铜催化末端炔烃与硫代磺酸酯的硫醇化反应。广泛的底物范围为制备各种含硫杂环化合物提供了便利途径。特别地，通过对带有邻位亲核官能团的乙炔基苯进行硫醇化反应，然后进行碘环化反应，可以以简单的方式高效制备多种苯并杂环化合物。
