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.
               
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