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Radical-Polar Crossover Enabled Triple Cleavage of CF<sub>2</sub>Br<sub>2</sub>: A Multicomponent Tandem Cyclization to 3-Fluoropyrazoles

Wanqing Zuo, Lingling Zuo, Xiao Geng, Zhifang Li, Lei Wang

2023Organic Letters85 citationsDOI

Abstract

The elaboration of step-economy and catalytic approaches for accessing diverse fluorinated heterocyclics is highly desirable. Described herein is a radical-polar crossover enabled three-component cyclization to polysubstituted fluoropyrazoles by using CF 2 Br 2 as a novel C1F1 synthon. Mechanistic experiments revealed that the in situ generation of the reactive intermediate gem -difluorovinylimine ion is the key to this transformation. This protocol unlocks the novel reactivity of CF 2 Br 2 and adds significant synthetic values to fluorine chemistry.

Topics & Concepts

SynthonChemistryTandemPolarReactivity (psychology)Cleavage (geology)Combinatorial chemistryCatalysisBond cleavageStereochemistryOrganic chemistryMedicineAstronomyFracture (geology)PhysicsGeotechnical engineeringEngineeringAlternative medicinePathologyMaterials scienceComposite materialFluorine in Organic ChemistryRadical Photochemical Reactions