Diphosgene → (R)-cyclohexyl-(2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl)-acetic acid methyl ester

Participants

Reaction Conditions

Reaction Steps

To a solution of (R)-(2-amino-benzoylamino)-cyclohexyl-acetic acid methyl ester (1.08 g, 3.72 mmol) in THF (30 mL) is added trichloromethyl chloroformate (550 mg, 2.78 mmol). The mixture is stirred at 90° C. for 4 hours. The reaction mixture is allowed to cool to room temperature, diluted with EtOAc (100 mL) and washed with H2O (50 mL×3). The organic layer is dried over sodium sulfate and is concentrated to give the desired (R)-cyclohexyl-(2,4-dioxo-1,4-dihydro-2H-quinazolin-3-yl)-acetic acid methyl ester (1.17 g, 99%).

Provenance & Evidence