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Elemental‐Sulfur‐Promoted C(sp 3 )−H Activation of Methyl Heteroarenes Leading to Thioamides
Author(s) -
Liu Jianming,
Zhao Shanshan,
Yan Xuyang,
Zhang Yanyan,
Zhao Shufang,
Zhuo Kelei,
Yue Yuanyuan
Publication year - 2017
Publication title -
asian journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.846
H-Index - 44
eISSN - 2193-5815
pISSN - 2193-5807
DOI - 10.1002/ajoc.201700532
Subject(s) - chemistry , thioamide , sulfur , dimethylamine , elemental analysis , medicinal chemistry , organic chemistry
An approach to access bioactive thioamides was developed based on elemental‐sulfur‐promoted C(sp 3 )−H activation of methyl heteroarenes. This transformation could successfully furnish a series of heterocyclic thioamides with excellent yields and it could be conducted on gram scale with good reaction efficiency. Mechanistic studies showed that methyl heteroarenes reacted with dimethylamine released from DMF to form the desired thioamide through elemental‐sulfur‐promoted C−H activation.