We have developed an efficient method to achieve N-gem-difluorocyclopropylation of N-heterocycles with the use of gem-difluorocyclopropyl tosylate as a building block under mild conditions, gem- Difluorocyclopropyl tosylates could be easily prepared on a large scale and exhibit great stability.
The copper-mediated trifluoromethylation of terminal alkynes with S-(trifluoromethyl)diarylsulfonium salt has been carefully investigated. The reactions proceeded smoothly to afford trifluoromethylated acetylenes in moderate to good yields. This approach is a convenient method to synthesize a variety of functional trifluoromethylated acetylenes.