反应详情

2-Chloro-N-[6-[2-(4-cyano-phenyl)-2H-pyrazol-3-yl]-7-methyl-8-(3-trifluoromethyl-phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl]-acetamide (Int. 17, 150 mg, 0.28 mmol) was stirred in dry DMF (3 mL), then K2CO3 (83 mg, 0.60 mmol) and 1-methylpiperazine (56 mg, 0.56 mmol) were added. Stirring was continued for 2 hrs at RT then the reaction mixture was partitioned between EtOAc and water. The organic layer was washed with water followed by saturated brine, then dried (Na2SO4) and concentrated in vacuo. The resultant residue was purified by flash chromatography eluting with a gradient of 2-5% MeOH in DCM followed by 10% (2M NH3 in MeOH) in DCM to give the title compound as a white solid (128 mg).

1. customthe reaction mixture was partitioned between EtOAc and water
2. washThe organic layer was washed with water
3. dry with materialdried (Na2SO4)
4. concentrationconcentrated in vacuo
5. customThe resultant residue was purified by flash chromatography
6. washeluting with a gradient of 2-5% MeOH in DCM