反应详情

Using methods described in Example 6, and starting with (R)-tert-butyl 3-methyl-4-(5-phenylpyrido[3,2-d]pyridazin-8-yl)piperazine-1-carboxylate 74 (325 mg, 801 μmol) and trifluoroacetic acid (3.09 ml, 40.1 mmol), yielded (R)-8-(2-methylpiperazin-1-yl)-5-phenylpyrido[3,2-d]pyridazine 75 (240 mg, 98.1% yield). 1H-NMR (400 MHz, CDCl3): δ 9.07 (dd, J=4.3, 2.0 Hz, 1H), 8.31 (dd, J=8.6, 2.0 Hz, 1H), 7.72 (m, 2H), 7.64 (dd, J=8.6, 4.3 Hz, 1H), 7.52 (m, 3H), 5.38 (m, 1H), 4.60 (dt, J=13.3, 2.3 Hz, 1H), 3.64 (ddd, J=13.7, 10.6, 4.7 Hz, 1H), 3.31 (dd, J=12.5, 3.9 Hz, 1H), 3.15 (m, 2H), 2.95 (dd, J=12.5, 1.6 Hz, 1H), 1.43 (d, J=7.0 Hz, 1H). MS 305.2 306.1 (M+H, found).