反应详情

3-iodopyridin-4-amine (2.2 g, 10 mmol), (5-chloro-2-methoxyphenyl)boronic acid (1.86 g, 10 mmol) and, and K2CO3 (4.2 g, 30 mmol) were mixed in 50 mL of toluene, 5 mL of deionized water and 5 mL of ethanol. To the solution was bubbled with nitrogen for 15 min. Pd(PPh3)4 (0.23 g, 0.2 mmol) was then added. The mixture was refluxed overnight under nitrogen. After cooling, the aqueous layer was removed and the organic layer was then concentrated. The residue was then purified by column chromatography using ethyl acetate as the eluent. 2.0 g (85%) of product was collected as the product.

1. customTo the solution was bubbled with nitrogen for 15 min
2. temperatureThe mixture was refluxed overnight under nitrogen
3. temperatureAfter cooling
4. customthe aqueous layer was removed
5. concentrationthe organic layer was then concentrated
6. customThe residue was then purified by column chromatography
7. custom2.0 g (85%) of product was collected as the product