反应详情

温度

80 °C

A mixture of 1-(4-Bromo-2,6-dichloro-benzyl)-3-(4-methoxy-cyclohexyl)-pyrrolidin-2-one (0.4 g, 0.92 mmol) and 4-fluorophenylboronic acid (0.19 g, 1.38 mmol) in THF (15 mL) and water (5 mL) and sodium carbonate (0.29, 0.75 g) is purged with N2. Treat the reaction with Pd(PPh3)4 (0.05 g, 0.046 mmol) and heat to 80° C. for 2 hour under N2. Cool the reaction, dilute with ethyl acetate, and wash with HCl (1N) and water. Dry the organic layer (Na2SO4), remove the solvent in vacuo to afford crude product, and purify with a 35% ethyl acetate in hexanes to afford 0.45 g of the titled product. MS (m/z): 451 (M+).

1. customis purged with N2
2. additionTreat
3. temperatureCool
4. customthe reaction
5. washwash with HCl (1N) and water
6. dry with materialDry the organic layer (Na2SO4)
7. customremove the solvent in vacuo
8. customto afford crude product
9. custompurify with a 35% ethyl acetate in hexanes