2-Pyrazinecarboxylic acid → Methyl 2-(3-cyclohexyl-1,1,1-trifluoro-3-(pyrazine-2-carboxamido)propan-2-ylamino)-3,3-dimethylbutanoate

Participants

Reaction Steps

A mixture of the 6A1-isomer A of methyl 2-(3-cyclohexyl-1,1,1-trifluoro-3-aminopropan-2-ylamino)-3,3-dimethylbutanoate (389 mgm), pyrazinecarboxylic acid (65 mg), 1-ethyl-3-(3′-dimethylaminopropyl)-carbodimide ((331 mg), 1-hydroxy-benzotriazole (233 mg), and N-methylmorpholine (0.19 mL) in dichloromethane was stirred at room temperature for 24 hours. The reaction mixture was then diluted with ethyl acetate and washed successively with 1N hydrochloric acid, water, brine and then dried over anhydrous sodium sulfate. Evaporation to dryness under reduced pressure gave crude methyl 2-(3-cyclohexyl-1,1,1-trifluoro-3-(pyrazine-2-carboxamido)propan-2-ylamino)-3,3-dimethylbutanoate, an isomer of a compound of formula (7) designated as 7A1-isomer A.

Provenance & Evidence