Triethylamine → MT-7716 free base

Participants

Reaction Steps

(R)-2-{3-[1-(Acenaphthen-1-yl)piperidin-4-yl]-2,3-dihydro-2-oxo-benzoimidazol-1-yl}acetic acid (1 g, 2.3 mmol) was dissolved in DMF (10 ml). Methylamine hydrochloride (0.17 g, 2.5 mmol), WSC•HCl (0.53 g, 2.7 mmol), HOBt (0.43 g, 2.8 mmol) and triethylamine (0.7 ml, 5 mmol) were added and the mixture was stirred at room temperature for 15 hr. The reaction mixture was poured into water, and the mixture was extracted with ethyl acetate. The extract was washed with water and saturated aqueous ammonium chloride solution, dried over magnesium sulfate, and concentrated. The obtained residue was purified by silica gel column chromatography (chloroform/methanol) to give the title compound (0.7 g) as pale-yellow crystals.

Provenance & Evidence