反应详情

To a solution of 3-methyl-4-{[(3S)-3-methyl-1-piperazinyl]sulfonyl}benzonitrile (may be prepared as described in Description 9) (75 mg, 0.268 mmol), pyrazolo[1,5-a]pyrimidine-3-carboxylic acid (48.2 mg, 0.295 mmol) and DIPEA (0.070 ml, 0.403 mmol) in dry DMF (3 ml) at rt under argon was added HATU (122 mg, 0.322 mmol) and the resulting yellow solution stirred at rt for 1 hour. Concentration in vacuo gave a yellow oil, that was purified by MDAP; concentration of the desired fractions gave a clear film (80.2 mg). Flash chromatography (silica; Flash 12S; linear gradient (1-8%) [2M NH3 in MeOH] in DCM) gave the title compound as a clear film (44.9 mg), that became a white solid on standing in vacuo (1 mbar) for 1 h.

1. concentrationConcentration in vacuo
2. customgave a yellow oil, that
3. customwas purified by MDAP
4. customconcentration of the desired fractions gave a clear film (80.2 mg)