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Gold‐catalyzed C−H Functionalization of Phenothiazines with Aryldiazoacetates

Sripati Jana, Claire Empel, Chao Pei, Thành Vinh Nguyễn, René M. Koenigs

2020Advanced Synthesis & Catalysis26 citationsDOIOpen Access PDF

Abstract

Abstract Phenothiazine is an important structural motif in pharmaceuticals and advanced functional organic materials. However, the C−H functionalization reaction of N ‐protected phenothiazine is rather unexplored and often shadowed by its chemical reactivity on the heteroatomic centers, which limits the diversity of its potential applications. This report demonstrates a straightforward approach towards the site‐selective C−H functionalization of phenothiazine at the para ‐position of N atom via gold‐catalyzed carbene transfer reactions (37 examples, up to 83% yield). The mechanism behind the regionselectivity of the C−H functionalization reaction was also elucidated by a combination of computational and experimental studies. magnified image

Topics & Concepts

PhenothiazineChemistrySurface modificationCarbeneCatalysisCombinatorial chemistryReactivity (psychology)PhotochemistryNanotechnologyOrganic chemistryPhysical chemistryPathologyMaterials scienceMedicineAlternative medicinePharmacologyCyclopropane Reaction MechanismsCatalytic C–H Functionalization MethodsCatalytic Alkyne Reactions
Gold‐catalyzed C−H Functionalization of Phenothiazines with Aryldiazoacetates | Litcius