Difluorocarbene as a C–F source for the construction of fluorinated benzothiazoles

Abstract

Difluorocarbene has served as a versatile intermediate for the incorporation of fluorinated groups into organic molecules. Extensive studies have shown that difluorocarbene can act as a CF₂ source and a nonfluorinated C₁ source. However, the use of difluorocarbene as a C–F source remains a challenging task. Herein we disclose that difluorocarbene can function as a C–F source for the cyclization of 2-aminobenzenethiols, allowing for the construction of fluorinated benzothiazoles, which may provide new possibilities for drug developments due to the magic effects of the fluorine element and the pharmacological properties of benzothiazoles.