期刊
JOURNAL OF ORGANIC CHEMISTRY
卷 86, 期 9, 页码 6622-6632出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.1c00403
关键词
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资金
- National Science Foundation of China [81573304, 81703342]
- Natural Science Foundation of Jiangsu [BK20161050]
- Natural Science Foundation of Nanjing University of Chinese Medicine [NZY81703342]
- Postgraduate Research & Practice Innovation Program of Jiangsu Province [KYCX19_1261]
This reaction method is simple and efficient, allowing for the preparation of phenothiazine products from readily available starting materials, with high atom economy and broad substrate scope.
A one-pot and step economic reaction involving Rh(III)-catalyzed C-H thiolation and relay Cu(II)-catalyzed C-N amination of acetanilide and 2-bromothiophenol is reported here, with several valuable phenothiazine products obtained. This synthesis protocol proceeds from easily starting materials, demonstrating high atom economy, broad substrate scope, and good yield. Furthermore, the directing group can be easily eliminated, and chlorpromazine is provided in a large scale; thus this synthesis protocol could be utilized to construct phenothiazine scaffolds.
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