Transition-Metal-Free Synthesis of N-Arylphenothiazines through an N- and S-Arylation Sequence
Transition-Metal-Free Synthesis of N-Arylphenothiazines through an N- and S-Arylation Sequence
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DOI：
10.1021/acs.orglett.1c00515
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发表时间：
2021-03-05
期刊：
影响因子：
5.2
通讯作者：
Yoshida, Suguru
中科院分区：
文献类型：
--
作者：
Matsuzawa, Tsubasa;Hosoya, Takamitsu;Yoshida, Suguru
公开了一种在无过渡金属条件下由邻磺酰基苯胺高效合成N-芳基吩噻嗪的方法。邻磺酰苯胺的 N- 和 S- 芳基化序列使我们能够合成多种 N-芳基吩噻嗪。特别是，N-芳基吩噻嗪的一锅合成是通过芳基中间体的硫胺化制备邻磺酰基苯胺并遵循N-和S-芳基化序列，从容易获得的模块完成的。
An efficient synthetic method of N-arylphenothiazines from o-sulfanylanilines under transition-metal-free conditions is disclosed. An N- and S-arylation sequence of o-sulfanylanilines enabled us to synthesize a wide variety of N-arylphenothiazines. In particular, one-pot synthesis of N-arylphenothiazines was accomplished from easily available modules through preparation of o-sulfanylanilines by thioamination of aryne intermediates and following N- and S-arylation sequence.