Catalyst-free and highly selective electrophilic mono-fluorination of acetoacetamides: facile and efficient preparation of 2-fluoroacetoacetamides in PEG-400

Abstract

Series of α-mono-fluorinated acetoacetamides were synthesized under mild condition with industrialized Selectfluor as the F⁺ source in PEG-400. The approach avoided the use of base or metal catalyst, and most of cases proceeded in nearly quantitative conversions regardless of the electronic nature of the diversity substituent.