Cesium carbonate → 8-[(4-Methoxyphenyl)methyl]-12-(3-methyl-6-oxopyridazin-1-yl)-3,5,6,8,10-pentazatricyclo[7.4.0.02,6]trideca-1(9),2,4,10,12-pentaen-7-one

関与物質

反応条件

反応手順

9-Bromo-6-(4-methoxybenzyl)pyrido[3,2-e][1,2,4]triazolo[1,5-c]pyrimidin-5(6H)-one (Example 1, 75 mg, 0.19 mmol), 6-methylpyridazin-3(2H)-one (43 mg, 0.39 mmol), copper(I) iodide (44 mg, 0.23 mmol), dioxane (3 mL), trans-1,2-diaminocyclohexane (0.030 mL, 0.25 mmol) and Cs2CO3 (152 mg, 0.47 mmol) were combined and heated at 120° C. for 12 h in the microwave. The mixture was filtered, and purified (HPLC, 10-80% ACN-water) to afford the title compound (9 mg, 11%) as a white solid. 1H NMR (400 MHz, CDCl3) δ 2.44 (s, 3H), 3.76 (s, 3H), 5.77 (s, 2H), 6.81-6.83 (m, 2H), 7.03 (d, J=7.7 Hz, 1H), 7.60-7.61 (m, 2H), 8.36 (s, 1H), 8.99 (d, J=2.1 Hz, 1H), 9.25 (d, J=2.1 Hz, 1H). [M+H]=416.1.

情報源と証拠