反应详情

To a stirred solution of 3-methoxy-4-[N′-(2-methylphenyl)ureido]phenylacetic acid (456 mg, 1.45 mmol) and ethyl 4-(3-methylamino-1-propyl)benzoate (220 mg, 1.45 mmol) were added EDC.HCl (417 mg, 2.16 mmol), HOBt (cat.), and DMAP (catalytic amount) in DMF (10 mL), and the resulting mixture was stirred overnight. The mixture was diluted with EtOAc (300 mL), washed with brine, dried over MgSO4, and evaporated. The residue was chromatographed on silica-gel with CHCl3—EtOH (10:1) to give 503 mg (71%) ethyl 4-[3-[3-methoxy-4-[N′-(2-methylphenyl)ureido]phenylacetyl-N-methylamino]-1-propyl]benzoate as a yellow oil. MS (FAB) m/z 518(M+H)+.

1. washwashed with brine
2. dry with materialdried over MgSO4
3. customevaporated
4. customThe residue was chromatographed on silica-gel with CHCl3—EtOH (10:1)