反应详情

A suspension of 1-methyl-7-nitroindole-2-carboxylic acid (220 mg, 1 mmol) in 5 mL of SO2Cl was heated at reflux for 3 h to give a yellow solution. The excess SO2Cl was removed by distillation and the resulting yellow solid was dissolved in 5 mL of dry THF. Et3N (0.21 mL, 1.5 mmol) and N-(3-amino-5-tert-butyl-2-methoxy-phenyl)-methanesulfonamide (327 mg, 1.2 mmol) were added successively and the mixture was stirred 12 h. The reaction mixture was extracted with EtOAc to give 410 mg (87%) of 1-methyl-7-nitroindole-2-carboxylic acid (5-tert-butyl-3-methanesulfonylamino-2-methoxy-phenyl)-amide.

1. temperaturewas heated
2. temperatureat reflux for 3 h
3. customto give a yellow solution
4. customThe excess SO2Cl was removed by distillation
5. dissolutionthe resulting yellow solid was dissolved in 5 mL of dry THF
6. extractionThe reaction mixture was extracted with EtOAc