1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → 1-[(R)-3-(2-{4-[1-(2-Ethoxy-ethyl)-1H-benzoimidazol-2-yl]-[1,4]diazepan-1-yl}-ethyl)-3-phenyl-pyrrolidin-1-yl]-1-[5-(3-methanesulfonyl-[1,2,4]triazol-4-yl)-2-methoxy-phenyl]-methanone

Participants

Reaction Steps

Condense 5-(3-methanesulfonyl-[1,2,4]triazol-4-yl)-2-methoxy-benzoic acid (0.125 g, 0.42 mmol) and 1-(2-ethoxy-ethyl)-2-{4-[2-((S)-3-phenyl-pyrrolidin-3-yl)-ethyl]-[1,4]diazepan-1-yl}-1H-benzoimidazole dihydrochloride (0.23 g, 0.42 mmol) in the presence of 1-hydroxybenzotriazole hydrate (0.062 g, 0.51 mmol), 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide (0.97 g, 0.51 mmol), diisopropylethylamine (0.22 mL, 1.26 mmol), and dichloromethane (15 mL) as described for the preparation of Example 124 to afford 0.065 g of the title compound, Rf=0.28 (silica gel, 10% methanol in dichloromethane). The compound may be converted to the dihydrochloride salt by methods well known in the art.

Provenance & Evidence