反应详情

温度

150 °C

1-(8-bromo-9-methyl-9H-purin-6-yl)-4-phenylpiperidine-4-carbonitrile (400 mg, 1.0 mmol), 1-Methylpyrazole-4-boronic acid pinacol ester (419 mg, 2.0 mmol), and potassium phosphate (427 mg, 2.0 mmol) were suspended in dioxane (5 mL). To that mixture was added Pd(dppf)Cl2 (82 mg, 0.10 mmol) and water. This suspension was heated to 150° C. in the microwave for 30 minutes. Upon cooling, the resulting mixture was filtered through Celite and a PL-thiol SPE cartridge. The filtrate was then purified by prep HPLC to afford 2 mg of the desired product. 1H NMR (400 MHz, DMSO-d6): δ 8.42 (s, 1H), 8.26 (s, 1H), 8.03 (s, 1H), 7.59-7.51 (m, 2H), 7.42 (m, 2H), 7.35 (m, 1H), 5.62 (s, 2H), 3.93 (s, 3H), 3.84 (s, 3H), 3.34 (m, 4H), 2.27 (m, 2H), 2.08 (m, 2H). EI (MS) for C22H22N8: 399.29 (MH+).

1. temperatureUpon cooling
2. filtrationthe resulting mixture was filtered through Celite
3. customThe filtrate was then purified by prep HPLC