反应详情

温度

160 °C

Into a dry microwave vial under N2 was added 6-Bromo-4-[1-(3-phenyl-allyl)-piperidine-4-ylamino]-chromen-2-one (20 mg, 0.046 mmol), Pd(dppf)Cl2 (˜5 mol %), and CuI (˜6 mol %) in dry THF (0.5 mL) followed by n-butyl zinc bromide (0.273 mL, 0.138 mmol (0.5M in THF)) dropwise. The solution was heated in the microwave for 10 minutes at 160° C., filtered, and was purified by Prep HPLC to give 2.5 mg (10%) of the desired compound as the TFA salt. MS (ESI(+)Q1MS m/z 417 (M+H)+; 1H NMR (300 MHz, MeOH) δ ppm. 96 (t, 3H), 1.33-1.42 (m, 2H), 1.61-1.69 (m, 2H), 1.91-2.03 (m, 2H), 2.41 (br d, 2H), 2.72 (t, 2H), 3.24 (br t, 2H), 3.73 (br d, 2H), 3.96 (m, 3H), 5.42 (s, 1H), 6.30-6.40 (m, 1H), 6.95 (d, 1H), 7.23-7.54 (m, 8H), 7.86 (d, 1H).

1. filtrationfiltered
2. customwas purified by Prep HPLC