反应详情

To a solution of 4-((1,3-dimethyl-1H-pyrazol-5-yl)methylamino)-2-methyl-6-(((1S,2S)-2-(5-methylpyridin-2-yl)cyclopropyl)methoxy)pyridazin-3(2H)-one (10 mg, 0.025 mmol) in 1,2-Dichloroethane (2.0 mL) was added NCS (4.0 mg, 0.030 mmol). After stirred for 1 h at rt, the reaction mixture was concentrated. The residue was purified by reverse phase chromatography (X bridge Prep C18OBD, 40-60% acetonitrile in water with 10 mmol NH4HCO3 modifier) to obtain product. 1H NMR (400 MHz, MeOD) δ 8.21 (s, 1H), 7.53 (d, 1H), 7.14 (d, 1H), 5.91 (s, 1H), 4.42 (s, 2H), 4.21-4.16 (m, 1H), 4.11-4.06 (m, 1H), 3.79 (s, 3H), 3.63 (s, 3H), 2.31 (s, 3H), 2.19 (s, 3H), 2.12-2.06 (m, 1H), 1.82-1.79 (m, 1H), 1.25-1.20 (m, 1H), 1.10-1.05 (m, 1H); LRMS m/z (M+H) 429.1 found, 429.17 required.

1. concentrationthe reaction mixture was concentrated
2. customto obtain product