Water → HCID 53238990, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of dimethlyamine hydrochloride (20 mg, 0.3 mmol) in dry toluene (8 mL) is added AlMe3 (0.22 mL, 0.45 mmol) at room temperature. The solution is stirred at the same temperature for 15 minutes. 3-[5-(2-Amino-pyrimidin-5-yl)-1-tert-butyl-1H-benzoimidazol-2-yl]-4-[1,2,4]triazol-1-yl-benzoic acid methyl ester (example 7) (70 mg, 0.15 mmol) is added to the solution and it is heated to 90° C. for 12 hours. The mixture is cooled down to room temperature and water (10 mL) is added. The mixture is extracted with EtOAc (3×10 mL) and the combined organic layer is dried by Mg2SO4 (300 mg) and is filtered. The filtrate is concentrated and the residue is purified by silica gel flash column chromatography with 10% MeOH in CH2Cl2 as the eluent to afford the title compound (17 mg, 25%). LCMS (ESMS): m/z 468.20 (M++1)

Provenance & Evidence