[Br:1][C:2]1[C:3](Cl)=[N:4][C:5]([Cl:8])=[N:6][CH:7]=1.[CH2:10]([NH:12][CH2:13][CH2:14][C:15]([NH:17][CH3:18])=[O:16])[CH3:11].C(N(CC)CC)C>C(#N)C>[Br:1][C:2]1[C:3]([N:12]([CH2:10][CH3:11])[CH2:13][CH2:14][C:15]([NH:17][CH3:18])=[O:16])=[N:4][C:5]([Cl:8])=[N:6][CH:7]=15-Bromo-2,4-dichloropyrimidine (Aldrich; 1.14 g, 5.00 mmol), 3-ethylamino-N-methyl-propanamide (Intermediate 83; 0.642 g, 5.00 mmol) and triethylamine (0.71 mL, 5.10 mmol) were combined in acetonitrile (25 mL) and heated to 100° C. for 4 hrs. The solvent was removed under reduced pressure and the residue taken up in Ethyl Acetate, washed with water and purified by flash silica chromatography (companion, 40 g, 0-10% Methanol/DCM) to give the title compound as a white solid (1.06 g, 3.3 mmol, 66%).
Loading…
