1-((3,5-Difluorophenyl)sulfonyl)bicyclo[1.1.0]butane

CAS 1862202-13-8, Cat. No EN300-6495224
Reagent for installation of bicyclobutane and further remote diversification

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1-((3,5-Difluorophenyl)sulfonyl)bicyclo[1.1.0]butane is a versatile reagent used for installing bicyclobutane onto amines and thiols, enabling remote diversification of molecules¹. The reagent is a white solid, stable under ambient conditions, and recommended for long-term storage in a freezer. It exhibits high chemoselectivity for thiols over other functional groups and is used for late-stage functionalization of pharmaceuticals. A key feature of this reagent is the ability to remove the sulfone to reveal the parent bicyclobutane or use it as a handle for further remote diversification. Reported diversification reactions include deuterium labeling, allylation, fluorination, and olefination via a Julia reaction².

Synonyms: None