反应详情

温度

90 °C

(S)-ethyl 2-(2,6-difluoro-5-iodonicotinoyl)-3-((1-ethylpyrrolidin-2-yl)methylamino)acrylate (Intermediate 38, 0.360 g, 0.73 mmol) was taken up in DMF (5 mL), K2CO3 (0.303 g, 2.19 mmol) was added and reaction mixture was heated to 90° C. for 15 min. The reaction mixture cooled to room temperature and N1,N1-dimethylethane-1,2-diamine (0.080 mL, 0.73 mmol) was added and stirred for 15 min. The reaction mixture was quenched with water and extracted with EtOAc 3 times. The combined organics were washed with brine two times, dried over Mg2SO4, and the solvent removed. Crude product was carried on without purification.

1. customreaction mixture
2. temperatureThe reaction mixture cooled to room temperature
3. customThe reaction mixture was quenched with water
4. extractionextracted with EtOAc 3 times
5. washThe combined organics were washed with brine two times
6. dry with materialdried over Mg2SO4
7. customthe solvent removed
8. customCrude product was carried on without purification