N-Aminomorpholine → HCID 86659722, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of 2-(4-bromophenyl)-5-chloro-7-morpholin-4-yl-pyrazolo[1,5-a]-pyrimidine (100 mg, 0.25 mM) in toluene (7.0 mL), there were, in order, added sodium tert-butoxide (49 mg, 0.51 mM), tris(dibenzylidene-acetone) dipalladium (12 mg, 0.013 mM), tri-tert-butyl-phosphine (25 μL, 0.10 mM) and N-amino-morpholine (39 mg, 0.38 mM) and the mixture was stirred at 90° C. for 4 hours. After cooling the mixture to room temperature, water was added thereto and the mixture was extracted with ethyl acetate. The organic phase thus obtained was washed with a saturated aqueous common salt solution, dried over anhydrous magnesium sulfate and then concentrated under reduced pressure. The resulting residue was washed with methanol to thus give the title compound (62 mg, yield: 60%).

Provenance & Evidence