[NH:1]1[CH2:4][CH:3]([O:5][C:6]2[C:11]([Br:12])=[CH:10][N:9]=[C:8]([NH:13][C@H:14]3[CH2:19][CH2:18][C@@H:17]([CH3:20])[CH2:16][CH2:15]3)[N:7]=2)[CH2:2]1.CCN(CC)CC.[CH3:28][S:29](Cl)(=[O:31])=[O:30]>C(Cl)Cl>[Br:12][C:11]1[C:6]([O:5][CH:3]2[CH2:2][N:1]([S:29]([CH3:28])(=[O:31])=[O:30])[CH2:4]2)=[N:7][C:8]([NH:13][C@H:14]2[CH2:19][CH2:18][C@@H:17]([CH3:20])[CH2:16][CH2:15]2)=[N:9][CH:10]=1To a solution of 4-(azetidin-3-yloxy)-5-bromo-N-(cis-4-methylcyclohexyl)-pyrimidin-2-amine (1.24 g, 3.64 mmol) and Et3N (0.6 mL, 3.64 mmol) in DCM (20 mL) at 0° C. was added methanesulfonyl chloride (417 mg, 3.64 mmol). The mixture was stirred at 0° C. for 5 h, diluted by DCM, washed with saturated aqueous sodium carbonate solution and water, dried over sodium sulfate, filtered, and concentrated. The residue was purified by flash chromatography (silica gel, eluted by 1% methanol in DCM) to give the title compound as a white solid (1.3 g, 85% yield). MS (ESI) m/z: Calc. 418.1 (M+). Found: 420.1 (M++2).
Wird geladen…
