1-Hydroxybenzotriazole → HCID 86625485, compound

Participants

Reaction Steps

A solution of 1-(5-{4-[(1,2-benzisoxazol-3-ylamino)carbonyl]piperazin-1-yl}-1,2,4-thiadiazol-3-yl)piperidine-4-carboxylic acid (100 mg, 0.219 mmol), 1-hydroxybenzotriazole (29.6 mg, 0.219 mmol), 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (84.0 mg, 0.438 mmol) and tert-butyl N-(2-aminoethyl)carbamate (35.0 mg, 0.219 mmol) in N,N-dimethylformamide (2 ml) was stirred at room temperature for 12 hours. The reaction mixture was poured to water, and a solid was separated by filtration, which was recrystallized from a mixed solvent of tetrahydrofuran, ethyl acetate and hexane to give 111 mg (84.7%) of the desired product as a solid.

Provenance & Evidence