ArticleOrganic letters2026
Ru(II)-Catalyzed C-H Sulfonamidation of the Medicinally Relevant Benzodiazepine Scaffolds.
Article in Organic letters, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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8 authors.
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Abstract
A late-stage, efficient C-H functionalization of medicinally relevant 1,4-benzodiazepines for direct C-H sulfonamidation has been developed via Ru-catalyzed C-H activation. Tosyl azide (TsN3) serves as a bench-stable sulfonamidating reagent. The sulfonamidated product is further converted to an aminated product through chemoselective hydrolysis of the sulfonamide bond. In mechanistic studies, a ruthenacycle (BDZ-Ru-Cl) has been synthesized and characterized by NMR spectroscopy and SC-XRD. Additionally, a novel intermediate, Int-C (a six-membered N-SO2Ar-inserted species), was synthesized from BDZ-Ru-Cl, providing further support for the proposed mechanistic pathway. Density functional theory (DFT) studies were also conducted to gain deeper mechanistic insight and to validate the developed protocol.
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