College of Pharmaceutical Sciences, Soochow University, Suzhou 215123, China.
J Org Chem. 2021 Sep 3;86(17):12148-12157. doi: 10.1021/acs.joc.1c01480. Epub 2021 Aug 16.
The nickel-catalyzed aminomethylation of mercaptans has been disclosed that offers efficient and expedient access to synthesize α-aminosulfides. The intramolecular fragment coupling shows excellent chemoselectivity. This transformation shows good functional-group compatibility, tolerates a wide range of electron-withdrawing, electron-neutral, and electron-donating substituents in this process, and can serve as a powerful synthetic tool for the synthesis of α-aminosulfides at a gram scale. Thus, the newly developed methodology enables a facile route for C-S bond formation in a straightforward fashion.
镍催化的硫醇的氨甲基化反应已经被揭示，它为合成α-氨基硫化物提供了高效、便捷的途径。分子内片段偶联显示出优异的化学选择性。这种转化对功能基团具有很好的兼容性，在这个过程中可以容忍广泛的吸电子、电子中性和供电子取代基，并且可以作为在克级规模上合成α-氨基硫化物的有力合成工具。因此，新开发的方法为 C-S 键的形成提供了一种直接的简便途径。
