反应详情

温度

50 °C

1.45 g 7-formyl-1-methyl-1H-indole-2-carboxylic acid (salt with N-methyl-morpholine) are dissolved in 8 ml N,N-dimethylformamide and combined with 2.72 g O-(7-azabenzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium-hexafluorophosphate (HATU), 2.45 ml N,N-diisopropyl-ethylamine (DIEA) as well as 324 mg 1-hydroxy-7-azabenzotriazole (HOAT). The mixture is left for 15 minutes at ambient temperature with stirring and then 1.47 g N-(3-amino-5-tert-butyl-2-methoxy-phenyl)-methanesulphonamide hydrochloride are added. The reaction is heated to 50° C. for 12 hours and then divided between water and ethyl acetate. The organic phase is washed successively with 1 N hydrochloric acid, water and saturated aqueous sodium chloride solution and dried on magnesium sulphate. After elimination of the solvents in vacuo the residue is chromatographed on silica gel with cyclohexane/ethyl acetate (70:30 to 20:80).

1. washThe organic phase is washed successively with 1 N hydrochloric acid, water and saturated aqueous sodium chloride solution
2. customdried on magnesium sulphate
3. customAfter elimination of the solvents in vacuo the residue is chromatographed on silica gel with cyclohexane/ethyl acetate (70:30 to 20:80)