反应详情

To a suspension of ethyl 1-(4-bromophenyl)-1,4-dihydropyrrolo[2,3-d]imidazole-5-carboxylate (EXAMPLE 1) (95 mg) in ethanol (3 mL) was added 1 mL of 3N NaOH and the mixture heated at reflux for 6 h, after which time mixture was cooled to rt and acidified with 3N HCl to pH=3. The resulting off-white solid was collected by filtration to yield 1-(4-bromophenyl)-1,4-dihydropyrrolo[2,3-d]imidazole-5-carboxylic acid. LC-MS (ES+): m/z 306/308 (1/1) [MH+]. 1H NMR (DMSO-d6, 400 MHz): δ=7.18 (d, J=1.0 Hz, 1H), 7.86 (d, J=9.0 Hz, 2H), 7.92 (d, J=9.0 Hz, 2H), 8.69 (s, 1H), 12.15 (s, 1H, NH).

1. temperaturethe mixture heated
2. temperatureat reflux for 6 h
3. filtrationThe resulting off-white solid was collected by filtration