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

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. Described herein is the use of difluorocarbene as a C-F source for the cyclization of 2-aminobenzenethiols to provide fluorinated benzothiazoles. A one-step process installs a fluorine atom and constructs a heterocycle.

Automated summary

Difluorocarbene has been used as a versatile intermediate for incorporating fluorinated groups into organic molecules. In this study, it was revealed that difluorocarbene can function as a C-F source for the synthesis of fluorinated benzothiazoles, which may have potential applications in drug development.