反应详情

E5 (66.8 mg, 0.11 mmol), 4-cyanophenyl boronic acid (20 mg, 0.13 mmol), and Pd(dppf)2Cl2 (9 mg, 0.01 mmol) was added into a 10 mL CEM microwave tube, followed by THF (1.1 mL) and sodium carbonate (0.55 mL, 2M). The mixture was reacted by microwave at 150° C. for 10 min and then partitioned between water and ethyl acetate. Column chromatography with gradient dichloromethane:ethyl acetate (4:1 to 3:1 to 2:1) afforded 38 mg 7.01 as a yellow foamy solid in a racemic mixture. Additional amounts of 7.01 were prepared and combined.

1. customThe mixture was reacted by microwave at 150° C. for 10 min
2. custompartitioned between water and ethyl acetate