反应详情

Suspend 2-methoxy-4-[2-(4-methoxy-phenyl)-7-oxo-4,7-dihydro-5H-thieno[2,3-c]pyridin-6-yl]-benzoic acid (0.1451 g, 0.35 mmol) in DMF (5 mL) and add 2-pyrrolidin-1-yl-ethylamine (45 mg, 0.39 mmol), EDCI (81 mg, 0.42 mmol), HOBt (57 mg, 0.42 mmol) and Et3N (0.15 mL, 1.06 mmol). Stir the reaction at RT overnight. Dilute with EtOAc (100 mL), wash with water (2×30 mL), and dry over Na2SO4. Purify the crude material by silica gel chromatography, eluting with 2% NH3—H2O, 50% CH3OH/EtOAc to give 9 mg (5%) of the title compound. LC-MS/ES m/z 506.2 [M+H]+.

1. customthe reaction at RT overnight
2. washwash with water (2×30 mL)
3. dry with materialdry over Na2SO4
4. customPurify the crude material by silica gel chromatography
5. washeluting with 2% NH3—H2O, 50% CH3OH/EtOAc