反应详情

In a similar manner to Example 5, (E)-4-(tert-butoxycarbonylamino)acetyl-1-{4-[2-(1H-indazol-3-yl)vinyl]benzoyl}piperazine was obtained using dihydrochloride of Compound 18 (800 mg, 2.18 mmol), N-(tert-butoxycarbonyl)glycine (314 mg, 1.79 mmol), 1-hydroxybenzotriazole monohydrate (315 mg, 2.56 mmol), 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (482 mg, 2.51 mmol) and N-methylmorpholine (0.80 mL, 7.28 mmol). In a similar manner to Example 18, (E)-4-(tert-butoxycarbonylamino)acetyl-1-{4-[2-(1H-indazol-3-yl)vinyl]benzoyl}piperazine was treated with 10% hydrogen chloride-methanol solution to obtain Compound 61 (448 mg, 64%).