反应详情

温度

0 °C

Intermediate 5 (250 mg, 0.55 mmol) and benzyl hydrazine hydrochloride (120 mg, 0.61 mmol) were suspended in CH3CN (10 mL) at 0° C., and Et3N (85 μl, 0.61 mmol) was added. The reaction mixture was stirred at 0° C. for 30 mins and then allowed to reach RT and stirred for a further 1 hour. The reaction mixture was filtered and the filtrate was concentrated in vacuo. The resulting residue was purified by silica gel chromatography eluting with a gradient of 0-100% to yield the title compound as a yellow solid (100 mg).

1. customto reach RT
2. stirringstirred for a further 1 hour
3. filtrationThe reaction mixture was filtered
4. concentrationthe filtrate was concentrated in vacuo
5. customThe resulting residue was purified by silica gel chromatography
6. washeluting with a gradient of 0-100%