反应详情

温度

0 °C

A stirred solution of 2-(7-methyl-1H-indazol-5-yl)-1-(1-neopentyl-1H-tetrazol-5-yl)ethanamine (20.0 mg, 0.06 mmol) in dimethylformamide (1.0 mL) at 0° C. was treated with carbonyl diimidazole (11.0 mg, 1.1 equiv). The reaction was stirred for 5 min at 0° C., warmed to room temperature, stirred for 10 min, and treated with 3-(piperidin-4-yl)-3,4-dihydroquinazolin-2(1H)-one (15.0 mg, 1.1 equiv). The mixture was stirred at room temperature overnight. The solvent was evaporated and the residue purified by column chromatography to afford 22.0 mg (64%). 1H-NMR (CD3OD, 500 MHz) δ 0.90 (s, 9H), 1.35-1.60 (m, 4H), 2.53 (s, 3H), 2.71-2.85 (m, 2H), 3.41-3.52 (m, 2H), 3.98-4.14 (m, 5H), 4.24 (d, J=14.3, 1H), 4.34 (m, 1H), 6.77 (d, J=7.9, 1H), 6.94 (dd, J=7.6, 7.3, 1H), 7.06-7.17 (m, 3H), 7.45 (s, 1H), 7.88 (s, 1H), 7.98 (s, 1H). Mass spec.: 571.28 (MH)+.

1. temperaturewarmed to room temperature
2. stirringstirred for 10 min
3. stirringThe mixture was stirred at room temperature overnight
4. customThe solvent was evaporated
5. customthe residue purified by column chromatography
6. customto afford 22.0 mg (64%)