反应详情

Procedure EE: In a microwave reactor vessel, add (4-bromo-2-fluoro-phenyl)-(2-(S)-pyrrolidin-1-ylmethyl-pyrrolidin-yl)methanone (1.0 mmol), 4-methanesulfonylphenyl boronic acid (2.5 mmol), dichloropalladium di-triphenylphosphine (0.2 mmol), cesium fluoride (9.0 mmol) and acetonitrile (0.20M) and run in a CEM microwave reactor for 10 minutes at 120° C. with 75W power and cooling on. After this time, wash the reaction with water while extracting with 10% isopropanol/dichloromethane. Dry the organic layer with sodium sulfate, filter and concentrate in vacuo. Purify the title compound via radial chromatography eluting with 2M ammonia in methanol and dichloromethane. MS (m/e): 431.2 (M+1)

1. temperaturecooling on
2. washAfter this time, wash
3. customthe reaction with water
4. extractionwhile extracting with 10% isopropanol/dichloromethane
5. dry with materialDry the organic layer with sodium sulfate
6. filtrationfilter
7. concentrationconcentrate in vacuo
8. customPurify the title compound via radial chromatography
9. washeluting with 2M ammonia in methanol and dichloromethane