反应详情

To a solution of 1 g (5.18 mmol) of methyl 2-fluoro-4-methoxybenzoate in 20 ml of acetonitrile are respectively added 1.62 g (5.18 mmol) of tert-butyl 4-(4-formylphenyl)piperazine-1-carboxylate and 1.11 g (5.18 mmol) of tert-butyl 5-amino-1H-pyrazol-3-ylcarbamate. The reaction mixture is refluxed for 8 h. The solution is brought to room temperature, then the solid is filtered and rinsed several times with acetonitrile to yield 2.22 g (66%) of tert-butyl 4-(4-(3-(tert-butoxycarbonylamino)-5-cyano-6-(2-fluoro-4-methoxyphenyl)-4,7-dihydro-1H-pyrazolo[3,4-b]pyridine-4-yl)phenyl)piperazine-1-carboxylate in the form of a yellow solid.

1. temperatureThe reaction mixture is refluxed for 8 h
2. customis brought to room temperature
3. filtrationthe solid is filtered
4. washrinsed several times with acetonitrile