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Elemental‐Sulfur‐Promoted C(sp3)−H Activation of Methyl Heteroarenes Leading to Thioamides

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A novel approach to access bioactive thioamides is developed based on elemental sulfur promoted C(sp3)-H activation of methyl heteroarenes. This transformation could successfully furnish a series of heterocyclic thioamides with… Click to show full abstract

A novel approach to access bioactive thioamides is developed based on elemental sulfur promoted C(sp3)-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 a good reaction efficiency. Mechanistic studies show that methyl heteroarenes proceeded with dimethylamine released from DMF to form the desired thioamide through element sulfur promoted C(sp3)-H activation.

Keywords: methyl heteroarenes; sp3 activation; sulfur promoted; promoted sp3

Journal Title: Asian Journal of Organic Chemistry
Year Published: 2017

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