5-[1-tert-Butyl-2-(2-1,2,4-triazol-1-yl-phenyl)-1H-benzimidazol-5-yl]-4-methoxy-pyrimidin-2-ylamine → 2-Amino-5-[1-tert-butyl-2-(2-1,2,4-triazol-1-yl-phenyl)-1H-benzimidazol-5-yl]-3H-pyrimidin-4-one

Participants

Reaction Conditions

Reaction Steps

To a vial are added 5-[1-tert-butyl-2-(2-1,2,4-triazol-1-yl-phenyl)-1H-benzimidazol-5-yl]-4-methoxy-pyrimidin-2-ylamine (Example 44) (47 mg, 0.107 mmol) in THF (2 mL) and HBr (1 mL). The reaction mixture is stirred at 70° C. for 12 hours. The solvent is concentrated. The residue is purified by prep HPLC, with 5-95% acetonitrile/water as gradient to afford the title compound (31 mg, 68%) as a white-gray glass solid. LCMS (ESMS): m/z 427.72 (M++1)

Provenance & Evidence