Synthesis of Chiral Tertiary Allylic- and Propargylic Fluorides from Nonaflates of Chiral α-Fluorinated β-Keto Dicarbonyl Compounds

J Org Chem. 2023 Aug 18;88(16):11895-11904. doi: 10.1021/acs.joc.3c01184. Epub 2023 Jul 31.

Abstract

The acetyl group of chiral α-fluorinated dicarbonyl compounds was transformed to nonaflates through a reaction with perfluorobutanesulfonyl fluoride in the presence of DBU in 82-95% yield. These nonaflates were used in Suzuki and Sonogashira coupling reactions to afford chiral tertiary allylic fluorides bearing gem-disubstituted terminal alkenes with excellent optical purities (45-91%, ≥94% ee). In addition, chiral tertiary propargylic fluorides were obtained from the reaction of nonaflates with DBU (73-86%, ≥94% ee).