1-Pyrrolidinamine → HCID 46929148, compound

Participants

Reaction Steps

Hydroxybenzotriazole hydrate (64.7 mg; 0.41 mmol), N-ethyldiisopropylamine (181 μL, 1.04 mmol) and N-(3-dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride (81 mg, 0.41 mmol) were added to a mixture of 6-[3-(3,4-difluoro-phenyl)-5-hydroxymethyl-isoxazol-4-ylmethoxy]-nicotinic acid (150 mg, 0.41 mmol) and 1-aminopyrrolidine (51.8 mg, 0.41 mmol) in THF (15 mL) at room temperature. After stirring overnight the solvent was removed by distillation and the residue was purified by chromatography (silica, dichloromethane:methanol=98:2 to 95:5) afforded the title compound (150 mg, 84%) as a white solid. MS: m/e=429.1 [M−H]−.

Provenance & Evidence