Hydroxide → Ethyl trifluoroacetate

Participants

Reaction Steps

Synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one can be accomplished through the use of commercially available 4-chloroaniline. After reaction with pivaloyl chloride in the presence of hydroxide to afford the corresponding amide, treatment with an alkyl lithium and ethyl triflouroacetate is followed by acidification with a mineral acid to provide the salt of the triflouroketone (Scheme 1).

Provenance & Evidence