Strain-release trifluoromethoxylation and pentafluorosulfanoxylation of [1.1.0]bicyclobutanes: expanded access to fluorinated cyclobutane hybrid bioisosteres.

Abstract

Methods for formal bromo-trifluoromethoxylation and bromo-pentafluorosulfanoxylation of [1.1.0]bicyclobutanes using AgOCF₃ or AgOSF₅ and 1,3-dibromo-5,5-dimethylhydantoin are disclosed. These represent complementary strategies to the syntheses of SF₅- and CF₃SF₄-containing cyclobutanes previously reported from our laboratory, ultimately enabling comparative structural studies and in vitro ADME profiling for various fluorinated cyclobutanes.