反应详情

To a solution of (S)-N-{2-[5-[2-(7-aza-bicyclo[2.2.1]hept-7-yl)-1,1-dimethyl-2-oxo-ethyl]-2-(3,5-dimethylphenyl)-1H-indol-3-yl]-propyl}-N-(2-morpholin-4-yl-ethyl)-2,4-dinitrobenzenesulfonamide (61.3 mg in 1.4 mL dry methylene chloride) was added 0.130 mL of n-propylamine and the mixture stirred at room temperature. After 60 minutes the reaction was quenched by the addition of water, extracted with ethyl acetate and the combined organics washed with saturated aqueous sodium bicarbonate. The organic portion was then dried over sodium sulfate and concentrated in vacuo. Purification of the residue by flash chromatography on silica gel (methylene chloride:methanol, 92:8; then methylene chloride:methanol:ammonium hydroxide, 90:7:1) gave the title compound (39 mg).

1. customAfter 60 minutes the reaction was quenched by the addition of water
2. extractionextracted with ethyl acetate
3. washthe combined organics washed with saturated aqueous sodium bicarbonate
4. dry with materialThe organic portion was then dried over sodium sulfate
5. concentrationconcentrated in vacuo
6. customPurification of the residue by flash chromatography on silica gel (methylene chloride