反应详情

To a solution of (3S)-3-methyl-1-{[4-(trifluoromethyl)phenyl]sulfonyl}piperazine (may be prepared as described in Description 2) (80.0 mg, 0.259 mmol) in DMF (5 ml) was added pyrazolo[1,5-a]pyrimidine-3-carboxylic acid (42.3 mg, 0.259 mmol), HOBT.H2O (39.7 mg, 0.259 mmol) and HBTU (98.0 mg, 0.259 mmol). Finally DIPEA (0.136 ml, 0.778 mmol) was added and the reaction mixture was stirred at room temperature for 3 hours. DMF was evaporated in vacuo then 5 ml of DCM added and washed with saturated aq. NaHCO3 solution (5 ml), dried on a phase separation cartridge and evaporated in vacuo. The crude material was dissolved in MeCN/DMSO 1:1 and purified by MDAP. The desired fractions were collected and concentrated in vacuo to give the title compound as a white solid (105 mg).

1. customDMF was evaporated in vacuo
2. addition5 ml of DCM added
3. washwashed with saturated aq. NaHCO3 solution (5 ml)
4. customdried on a phase separation cartridge
5. customevaporated in vacuo
6. dissolutionThe crude material was dissolved in MeCN/DMSO 1:1
7. custompurified by MDAP
8. customThe desired fractions were collected
9. concentrationconcentrated in vacuo