反应详情

温度

150 °C

A solution of tert-butyl 4-[6-(6-chloropyrazolo[4,3-c]pyridin-1-yl)-2-pyridyl]piperazine-1-carboxylate (120 mg, 0.290 mmol) and palladium(0)tetrakis(triphenylphosphine) (34 mg, 0.0290 mmol) in N,N-dimethylacetamide 1.0 mL was added tributyl-(3-methylisothiazol-5-yl)stannane (224 mg, 0.579 mmol). The reaction mixture heated at 150° C. for 45 min in a microwave (Biotage Inc.). The reaction mixture was filtered through celite and concentrated. The crude product was diluted with EtOAc then washed with water. The organic layers was dried with sodium sulfate, filtered, and concentrated in vacuum. The crude product was purified by flash chromatography (EtOAc/Heptane eluted at 20% EtOAc) to give tert-butyl 4-[6-[6-(3-methylisothiazol-5-yl)pyrazolo[4,3-c]pyridin-1-yl]-2-pyridyl]piperazine-1-carboxylate (65 mg) 47% yield:

1. filtrationThe reaction mixture was filtered through celite and
2. concentrationconcentrated
3. additionThe crude product was diluted with EtOAc
4. washthen washed with water
5. dry with materialThe organic layers was dried with sodium sulfate
6. filtrationfiltered
7. concentrationconcentrated in vacuum
8. customThe crude product was purified by flash chromatography (EtOAc/Heptane eluted at 20% EtOAc)