A mild protocol for Ni-catalyzed trifluoromethylthiolation of aryl chlorides and bromides is described herein. The method utilizes AgSCF as an easily accessible nucleophilic trifluoromethylthiolating reagent and does not require any ligands or additives. Ortho-selectivity is achieved using a variety of directing groups such as imines, pyridines, and oxazolines for 24 examples in up to 95% yield.
Multi-drug resistant tuberculosis is a worldwide problem where despite treatment; mortality can range up to 18%. An N-aryl 2-aminothiazole-4-carboxamide derivative was identified as a lead compound in a Tuberculosis Coordinating Antimicrobial Acquisition Facility (TCAAF) screen. Synthesis and biological evaluation of additional analogs led to structure-activity relationships for activity against TB.
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