Ethylmorpholine → HCID 178476723, compound

Participants

Reaction Conditions

Reaction Steps

At 4° C. TOTU (48 mg, 0.14 mmol) was added to a solution of [3-(4-carbamimidoyl-phenyl)-2-(R,S)-cyclohexyl-propionylamino]-(S)-cyclohexyl-acetic acid hydrochloric acid salt (60 mg, 0.14 mmol), (S)-2-amino-5-guanidino-pentanoic acid phenethyl-amide dihydrochloride (51 mg, 0.14 mmol) and N-ethylmorpholine (56 μl, 0.42 mmol) in dimethylformamide (10 ml). The mixture was stirred at 22° C. for 15 hours. The solvent was evaporated and the residue was purified by column chromatography (Sephadex LH20, n-butanol/acetic acid/water 17:1:2) to give two stereoisomeric product mixtures. more polar diastereomeric mixture: 41 mg MS m/z 673.6 (M+H)+. less polar diastereomeric mixture: 21 mg MS m/z 673.6 (M+H)+. Total yield: 57%.

Provenance & Evidence