反应详情

To a DCM (2 mL) solution of 6-(2-(3-fluorophenyl)piperidin-1-yl)imidazo[1,2-b]pyridazin-3-amine (45 mg, 0.14 mmol) was added CDI (35 mg, 0.22 mmol) at ambient temperature in one portion. After stirring for five hours, azetidin-3-ol hydrochloride (54 mg, 0.33 mmol) was added in one portion, followed by DIEA (0.05 mL, 0.29 mmol), and the reaction was stirred at ambient temperature overnight. The reaction was diluted with DCM, washed with water, dried over Na2SO4 and concentrated. The crude product was purified by reversed phase column, eluting with 0 to 55% CH3CN/water to obtain the desired product as a solid (30 mg, 51% yield). MS (apci) m/z=411.2 (M+H).

1. stirringthe reaction was stirred at ambient temperature overnight
2. washwashed with water
3. dry with materialdried over Na2SO4
4. concentrationconcentrated
5. customThe crude product was purified by reversed phase column
6. washeluting with 0 to 55% CH3CN/water