1-Hydroxybenzotriazole → HCID 57901820, compound

Participants

Reaction Steps

To a mixture of 2-(tritylthio)ethylamine hydrochloride (0.32 g), triethylamine (0.126 mL) and N,N-dimethylformamide (10 mL) were added 5-methoxy-7-[(2-thienylsulfonyl)amino]-1H-indole-2-carboxylic acid (265 mg), 1H-1,2,3-benzotriazol-1-ol (0.15 g) and N-[3-(dimethylamino)propyl]-N′-ethylcarbodiimide hydrochloride (188 mg) under ice-cooling, and the mixture was stirred at room temperature for 15 hr. The reaction mixture was diluted with ethyl acetate, washed with aqueous citric acid solution, aqueous sodium hydrogencarbonate solution and saturated brine, dried over anhydrous magnesium sulfate, and concentrated under reduced pressure. The obtained oil was crystallized from dichloromethane-hexane to give the title compound (465 mg, yield 95%) as pale-yellow crystals. melting point 128-129° C.

Provenance & Evidence