反应详情

To a solution of (3S)-3-methyl-1-({4-[(trifluoromethyl)oxy]phenyl}sulfonyl)piperazine (may be prepared as described in Description 13) (300 mg, 0.925 mmol), HOBt (142 mg, 0.925 mmol), HBTU (351 mg, 0.925 mmol) and pyrazolo[1,5-a]pyrimidine-3-carboxylic acid (151 mg, 0.925 mmol) in DMF (50 ml) was added DIPEA (0.485 ml, 2.78 mmol) and the resulting mixture stirred at room temperature overnight, then concentrated under vacuum. The residue was redissolved in EtOAc, washed with aqueous NaHCO3 and brine, then concentrated under vacuum. Flash chromatography (silica; EtOAc) and concentration of the desired fractions gave the title compound (157 mg).

1. concentrationconcentrated under vacuum
2. dissolutionThe residue was redissolved in EtOAc
3. washwashed with aqueous NaHCO3 and brine
4. concentrationconcentrated under vacuum