反应详情

温度

100 °C

Degass a mixture of 2-(4-chloro-phenyl)-6H-thieno[2,3-c]pyridin-7-one (374 mg, 1.43 mmol), [(R)-1-(5-bromo-pyridin-2-yl)-pyrrolidin-3-yl]-cyclopropyl-amine (404 mg, 1.43 mmol) and cesium carbonate (932 mg, 2.86 mmol) in 1,4-dioxane (20 mL). Add copper (I) iodide (162 mg, 851 μmol) and sym-dimethylethylene diamine (150 mg, 1.70 mmol). Heat the mixture at 100° C. overnight. Dilute with concentrated NH4OH (5 mL) and water (50 mL) and CH2Cl2. Separate the organics and dry with Na2SO4, filter, and concentrate. Purify using chromatography (0 to 10% MeOH/CH2Cl2) to afford 0.384 g (64%) of 6-[6-((R)-3-amino-pyrrolidin-1-yl)-pyridin-3-yl]-2-(4-chloro-phenyl)-6H-thieno[2,3-c]pyridin-7-one.

1. customDegass
2. customSeparate the organics and
3. dry with materialdry with Na2SO4
4. filtrationfilter
5. concentrationconcentrate
6. customPurify