Water → Convergence

Participants

Reaction Steps

To a solution of 1-{[4-(trifluoromethyl)phenyl]sulfonyl}piperazine (may be prepared as described in Description 1) (200 mg, 0.680 mmol) in DMF (5 ml) was added pyrazolo[1,5-a]pyrimidine-3-carboxylic acid (111 mg, 0.680 mmol), HOBT.H2O (104 mg, 0.680 mmol) and HBTU (258 mg, 0.680 mmol). Finally DIPEA (0.356 ml, 2.039 mmol) was added and the reaction mixture was stirred at rt for 20 hours. Solvent was removed by evaporation, the crude partitioned between DCM (50 ml) and saturated aq. sodium bicarbonate (50 ml), the DCM layer collected, dried (hydrophobic frit) and evaporated. MDAP purification yielded the title compound (317 mg) as an off-white solid.

Provenance & Evidence