反应详情

温度

40 °C

HCl (4N in dioxane, 5 mL) was added to 3-{3,5-dichloro-4-[4-(6-methylpyrimidin-4-ylamino)thiazolo[5,4-c]pyridin-2-yl]-phenyl}-azetidine-1-carboxylic acid tert-butyl ester (0.062 g, 0.114 mmol). The suspension was heated at 40° C. for 1 hour and then cooled to room temperature. The volatiles were removed under reduced pressure and the resultant residue was triturated with a mixture of EtOAc/DCM and then purified by column chromatography on silica gel eluting with 0-5% 2N NH3/MeOH in DCM to afford the title compound as an off-white solid (20 mg, 40% yield). 1H NMR (400 MHz, CDCl3): δ 8.65 (d, J=1.2 Hz, 1H), 8.46 (d, J=5.6 Hz, 1H), 7.84 (d, J=5.6 Hz, 1H), 7.75 (s, 2H), 7.63 (s, 1H), 3.99-3.90 (m, 1H), 3.85 (t, J=7.6 Hz, 2H), 3.61 (t, J=6.9 Hz, 2H), 2.41 (s, 3H). LCMS (Method C): RT=2.21 min, m/z: 443 [M+H+].

1. temperaturecooled to room temperature
2. customThe volatiles were removed under reduced pressure
3. customthe resultant residue was triturated with a mixture of EtOAc/DCM
4. custompurified by column chromatography on silica gel eluting with 0-5% 2N NH3/MeOH in DCM