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. 2021 Mar 19;23(6):2347-2352. doi: 10.1021/acs.orglett.1c00515. Epub 2021 Mar 5.
An efficient synthetic method of -arylphenothiazines from -sulfanylanilines under transition-metal-free conditions is disclosed. An - and -arylation sequence of -sulfanylanilines enabled us to synthesize a wide variety of -arylphenothiazines. In particular, one-pot synthesis of -arylphenothiazines was accomplished from easily available modules through preparation of -sulfanylanilines by thioamination of aryne intermediates and following - and -arylation sequence.
本文公开了一种在无过渡金属条件下由 -硫代苯胺合成 -芳基吩噻嗪的有效方法。-硫代苯胺的 -和 -芳基化反应序列使我们能够合成各种 -芳基吩噻嗪。特别是,通过芳基炔中间体的硫氨化制备 -硫代苯胺,并随后进行 -和 -芳基化反应序列,可从易得的模块一步合成 -芳基吩噻嗪。