反应详情

Add tributylvinyltin (0.059 mL, 0.19 mmol) to a solution of 4-[2-(6-chloro-pyridin-2-yl)-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazol-3-yl]-quinoline, EXAMPLE 101, (59 mg, 0.17 mmol) in toluene (0.7 mL) at RT. Bubble nitrogen into the reaction mixture for 5 min and add tetrakis-(triphenylphosphine) palladium (0) (10 mg, 0.0085 mmol). Bubble nitrogen into the solution for an additional 2 min and heat the reaction to 110° C. for 18 h. Concentrate the reaction in vacuo and purify by flash column chromatography (SiO2, 20-40% acetone/hexanes) to provide the title compound (35 mg, 62%) as a white solid.

1. waitBubble nitrogen into the solution for an additional 2 min
2. temperatureheat
3. customthe reaction to 110° C. for 18 h
4. concentrationConcentrate
5. customthe reaction in vacuo
6. custompurify by flash column chromatography (SiO2, 20-40% acetone/hexanes)