2,4-Dimethoxybenzylamine → 4-{4-[4-(2,4-Dimethoxy-benzylcarbamoyl)-oxazol-5-yl]-phenyl}-2,2-dimethyl-piperazine-1-carboxylic acid tert-butyl ester

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Reaction Steps

4-[4-(4-Carboxy-oxazol-5-yl)-phenyl]-2,2-dimethyl-piperazine-1-carboxylic acid tert-butyl ester was dissolved in 30 mL DMF. To the solution was added 2,4-dimethoxybenzylamine (1.26 g, 7.6 mmol), HATU (2.8 g, 7.4 mmol) and TEA (1 g, 10 mmol). The mixture was stirred at room temperature overnight and the solvent was removed in vacuo. The residue was purified by silica gel column chromatography (PE:EtOAc=5:1 to DCM:MeOH=200:1) to afford the title compound (1.6 g, 3 mmol, yield: 54% over two steps).

Provenance & Evidence