反应详情

To a solution of 4-[5-nitro-1H-indol-3-ylmethyl]-3-methoxy-benzoic acid methylester (0.50 grams, 1.47 mmol) and triethylamine (0.62 mL, 4.41 mmol) in methylene chloride (30 mL), at 0° C., was added a solution of phosgene in toluene (1.9 M in toluene, 1.5 mL, 2.9 mmol). The solution was warmed to room temperature and stirred for 1 hour. To this was added aminodiphenylmethane hydrochloride (0.65 grams, 2.94 mmol) and the resulting solution was stirred for 12 hours at room temperature. The solution was concentrated in vacuo and the crude triturated with methanol. The resulting pale yellow solid was collected via filtration to give 4-[1-(benzhydryl-carbamoyl)-5-nitro-1H-indol-3-ylmethyl]-3-methoxy-benzoic acid methylester (0.672 grams, 83% yield).

1. stirringthe resulting solution was stirred for 12 hours at room temperature
2. concentrationThe solution was concentrated in vacuo
3. customthe crude triturated with methanol
4. filtrationThe resulting pale yellow solid was collected via filtration