反应详情

To a solution of 6-bromopyrazolo[1,5-a]pyrimidine-3-carboxylic acid (may be prepared as described in Description 17) (471 mg, 1.946 mmol) in N,N-Dimethylformamide (10 mL) under a flush of argon was added HATU (740 mg, 1.946 mmol) and the reaction stirred for 10 minutes. (3S)-3-methyl-1-{[4-(trifluoromethyl)phenyl]sulfonyl}piperazine (may be prepared as described in Description 2) (600 mg, 1.946 mmol) was then added followed by N,N-diisopropylethylamine (0.680 mL, 3.89 mmol) and the reaction stirred for 18 h. The reaction mixture was partitioned between ethyl acetate (60 mL) and water (40 mL). The organic layer was washed with further water (20 mL) and brine (20 mL) before it was dried (MgSO4), filtered and the solvent removed in vacuo. The crude material was purified by silica chromatography, 40 M cartridge, eluting 0-75% EtOAC in isohexane and the solvent evaporated to give the title compound (587 mg) as a white solid.

1. stirringthe reaction stirred for 18 h
2. customThe reaction mixture was partitioned between ethyl acetate (60 mL) and water (40 mL)
3. washThe organic layer was washed with further water (20 mL) and brine (20 mL) before it
4. dry with materialwas dried (MgSO4)
5. filtrationfiltered
6. customthe solvent removed in vacuo
7. customThe crude material was purified by silica chromatography, 40 M cartridge
8. washeluting 0-75% EtOAC in isohexane
9. customthe solvent evaporated