反应详情

A solution of 7-chloro-3-(carboxy)pyrazolo[3,4-c][1]-benzazepine-4,10(1H,9H)-dione (300 mg, 1.03 mmol) (compound of Example 9) and 1,1′-carbonyldiimidazole (251 mg, 1.55 mmol) in N,N-dimethylformamide (12 mL) was stirred for 1 hour. In one portion N-isopropylhydroxylamine hydrochloride (345 mg, 3.09 mmol) was added and the solution was stirred for 55 minutes at room temperature. To the resulting solution was added water (40 mL) giving a precipitate which was separated by filtration. This Crude product was purified by flash chromatography eluting with chloroform:2-propanol (98:2-96.5:3.5) to give the title compound (167 mg, 47% yield, m.p. 224° C.).

1. customgiving a precipitate which
2. customwas separated by filtration
3. customThis Crude product was purified by flash chromatography
4. washeluting with chloroform:2-propanol (98:2-96.5:3.5)