4H-pyrazolo[1,5-[alpha]]benzimidazole compound analogue as PARP inhibitor
A compound, CH3 technology, applied in anti-inflammatory agents, organic chemistry, drug combination, etc., can solve problems such as unrealized treatment
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Embodiment 1
[0264] 6-Fluoro-3-(piperidin-4-yl)-4H-benzo[4,5]imidazo[1,2-b]pyrazole-8-carboxamide
[0265]
Embodiment 1A
[0267] tert-butyl 4-(p-toluenesulfonyloxymethyl)piperidine-1-carboxylate
[0268]
[0269] Under nitrogen protection at 0°C, tert-butyl 4-(hydroxymethyl)piperidine-1-carboxylate (10 g, 46.5 mmol), triethylamine (5.64 g, 55.8 mmol) and DMAP (1.13 g, 9.3 mmol) in dichloromethane (100 ml) was added in portions to TosCl (9.73 g, 51.2 mmol), stirred at 17 °C for 2 hours, quenched by adding water (100 ml), and the aqueous layer was washed with dichloromethane (100 mL × 2) extraction, the combined organic layers were dried over sodium sulfate, filtered and evaporated, and the residue was purified by column chromatography to obtain the title compound (white solid, 17 g, 99% yield). LCMS(ESI)m / z:370(M+1).
Embodiment 1B
[0271] tert-Butyl 4-(cyanomethyl)piperidine-1-carboxylate
[0272]
[0273] Example 1A (19 g, 55.7 mmol), a mixture of sodium cyanide (8.19 g, 167 mmol) in dimethyl sulfoxide (100 ml) was reacted at 100°C for 16 hours. After cooling to room temperature, dilute with water (200 mL), extract the aqueous layer with ethyl acetate (100 mL × 3), wash the combined organic layer with water (50 mL), brine (50 mL), dry over sodium sulfate, filter and evaporate , provided the title compound (11 g) which was used directly in the next step without further purification. LCMS(ESI)m / z:225(M+1)
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