Dimethylformamide → HCID 131723236, compound

Participants

Reaction Steps

To a solution of [3-(4-carbamimidoyl-phenyl)-2-(R,S)-dimethylcarbamoyl-propionylamino]-(S)-cyclohexyl-acetic acid (100 mg, 0.248 mmol, example 1 h) and 4-aminomethyl-benzonitrile hydrochloride (37 mg, 0.22 mmol) in dimethylformamide (10 ml) TOTU (79 mg, 0.24 mmol) and N-ethylmorpholine (50 mg, 0.44 mmol) were added at −15° C. The mixture was stirred for 1 hour and then allowed to warm to room temperature. After evaporation the residue was purified by chromatography on Sephadex LH20 employing n-butanol (17): glacial acetic acid (1): water (2) as eluent. Pure fractions were combined. The solvent was evaporated, the residue was taken up in water and the aqueous solution was lyophilized to yield 83 mg (65%) of the desired product. MS m/z: 517.4 (M+H)+.

Provenance & Evidence