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Abstract
A late-stage C-H functionalization of 1,4-benzodiazepines for direct C-H amidation has been developed via Ru-catalyzed C-H activation. This method efficiently generates medicinally relevant functionalized products using Ru-metal. Tosyl azide serves as a bench-stable amidating reagent. The amidated product is further converted to an aminated product through chemoselective hydrolysis of the sulfonamide bond. In mechanistic studies, ruthenacycle has been synthesized and charac-terized by NMR spectroscopy.
Supplementary materials
Title
Late-Stage C-H Amidation of Benzodiazepine Scaffold
Description
A late-stage C-H functionalization of 1,4-benzodiazepines for direct C-H amidation has been developed via Ru-catalyzed C-H activation. This method efficiently generates medicinally relevant functionalized products using Ru-metal. Tosyl azide serves as a bench-stable amidating reagent. The amidated product is further converted to an aminated product through chemoselective hydrolysis of the sulfonamide bond. In mechanistic studies, ruthenacycle has been synthesized and charac-terized by NMR spectroscopy.
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