Water → 3-[((2R)-2-Methyl-4-{[4-(trifluoromethyl)phenyl]sulfonyl}-1-piperazinyl)carbonyl]pyrazolo[1,5-a]pyrimidine

To a solution of (3R)-3-methyl-1-{[4-(trifluoromethyl)phenyl]sulfonyl}piperazine (may be prepared as described in Description 10) (80.0 mg, 0.259 mmol) in DMF (4 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), HBTU (98 mg, 0.259 mmol) and DIPEA (0.136 ml, 0.778 mmol) and the reaction mixture was stirred at rt for 1.5 hours. The DMF was evaporated in vacuo then DCM (5 ml) was added and the whole 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 to give the title compound (100 mg).

1. customThe DMF was evaporated in vacuo
2. additionDCM (5 ml) was added
3. washthe whole washed 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

ORD 기록

ord-3ae772d66956482295c6ee92b36f41cf

출처 데이터셋

uspto-grants-2012_01

DOI

10.6084/m9.figshare.5104873.v1

특허 번호

US08093249B2