4-Methylmorpholine → HCID 57887275, compound

Participants

Reaction Conditions

Reaction Steps

(2S,4S)-4-Amino-2-[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenylcarbamoyl]-pyrrolidine-1-carboxylic acid tert-butyl ester (90 mg) was dissolved in acetonitrile (0.75 ml). A solution of 5-chlorothiophene-2-carboxylic acid (53 mg), NMM (33 mg) and IBCF (44 mg) in acetonitrile (0.75 ml), which was stirred for 30 min at 25° C., was added to the first solution. The complete mixture was stirred for 72 h at 25° C., evaporated to dryness and purified by chromatography (silica gel; gradient: n-heptane->AcOEt) to yield (2S,4S)-4-[(5-chloro-thiophene-2-carbonyl)-amino]2-[2-fluoro-4-(2-oxo-2H-pyridin-1-yl)-phenylcarbamoyl]-pyrrolidine-1-carboxylic acid tert-butyl ester (46 mg) as colorless solid. MH+=561.3 (Cl-isotopes)

Provenance & Evidence