Tetrahydrofuran → HCID 57785922, compound

Participants

Reaction Steps

To a solution of 1-[9-chloro-1-(2,4-dichlorophenyl)-1,2,3,4-tetrahydropyrimido[1,2-a]benzimidazol-6-yl]propan-1-ol (50 mg, 0.123 mmol), cyclopropanecarboxylic acid (16 mg, 0.185 mmol), triethylamine (0.018 mL, 0.246 mmol) and 4-dimethylaminopyridine (23 mg, 0.185 mmol) in tetrahydrofuran (2 mL) was added 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (47 mg, 0.185 mmol) at room temperature. The mixture was stirred at room temperature for 18 hr. Saturated aqueous ammonium chloride was added to the reaction mixture and the mixture was extracted with ethyl acetate. The organic layer was washed with brine, dried over anhydrous magnesium sulfate and concentrated in vacuo. The residue was purified by flash chromatography on silica gel eluting with a 20-70% ethyl acetate/n-hexane gradient mixture and recrystallization from 2-propanol/n-hexane to give the title compound (25 mg, 0.0527 mmol, 43%) as colorless crystals.

Provenance & Evidence