反应详情

In a 10 mL round bottom flask, 6-{4-[3-((R)-2-methyl-pyrrolidin-1-yl)-propoxy]-phenyl}-4-pyridin-2-yl-4,5-dihydro-2H-pyridazin-3-one (120 mg, 0.31 mmol), and cesium carbonate (197 mg, 0.62 mmol), in dimethylsulfoxide (3 mL) was heated to 135° C. 3 h. The reaction was cooled and the slurry was partitioned between methylene chloride and water extracted three times, and then dried over MgSO4. Purification with silica gel chromatography eluting with methylene chloride/methanol (95:5), followed by HCl salt formation produced 120 mg (33%). Mp 157-161° C. MS m/z 391 (M+H).

1. custom3 h
2. temperatureThe reaction was cooled
3. customthe slurry was partitioned between methylene chloride and water
4. extractionextracted three times
5. dry with materialdried over MgSO4
6. customPurification with silica gel chromatography
7. washeluting with methylene chloride/methanol (95:5)
8. customproduced 120 mg (33%)