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 (about 5 mol %), and CuI (about 6 mol %) in dry THF (0.5 mL) followed by cyclopentyl 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 4.4 mg (18%) of the desired compound as the TFA salt. MS (ESI(+)Q1MS m/z 429 (M+H)+; 1H NMR (300 MHz, MeOH) δ ppm. 1.62-2.13 (m, 10H), 2.40 (br d, 2H), 3.06-3.12 (m, 1H), 3.24(br t, 2H), 3.72 (br d, 2H), 3.96 (m, 3H), 5.42 (s, 1H), 6.31-6.40 (m, 1H), 6.96 (d, 1H), 7.23-7.54 (m. 8H), 7.90 (d, 1H).

1. filtrationfiltered
2. customwas purified by Prep HPLC