(1-(2-ethoxyethyl)-1H-benzimidazol-2-yl)(piperidin-4-yl)amine → 1-(3,4,5-trimethoxybenzoyl)-3-(2-(4-(1-(2-ethoxyethyl)-1H-benzimidazol-2-yl-amino)piperidin-1-yl)ethyl)-3-(4-fluorophenyl)pyrrolidine

Participants

Reaction Steps

Prepare by the method of Example 16.7 using 1-(3,4,5-trimethoxybenzoyl)-3-(4-fluorophenyl)-3-(2-methanesulfonyloxyethyl)pyrrolidine (1.0 g, 3.5 mmol) and (1-(2-ethoxyethyl)-1H-benzimidazol-2-yl)(piperidin-4-yl)amine (1.6 g, 1.6 mmol). Purify by chromatography on silica gel eluting with 2% triethylamine/10% methanol/ethyl acetate to give the title compound: mp; 217-220° C. Rf=0.38 (silica gel, 2% triethylamine/5% methanol/ethyl acetate).

Provenance & Evidence