反应详情

In a similar manner to Step 2 of Example 6, 4-chloro-7-[1-(tert-butoxycarbonyl)-5-formylindol-2-yl]isoindolinone (57.5 mg, 0.140 mmol) was dissolved in acetonitrile (3 mL), and the solution was treated with aniline (0.051 mL, 0.56 mmol), acetic acid (0.160 mL, 2.80 mmol) and sodium triacetoxyborohydride (89 mg, 0.42 mmol). The reaction mixture was added with 1 mol/L hydrochloric acid and extracted with ethyl acetate. The organic layer was washed with saturated aqueous sodium hydrogencarbonate solution and saturated brine, and dried over anhydrous sodium sulfate. The solvent was evaporated under reduced pressure to obtain 4-chloro-7-(1-(tert-butoxycarbonyl)-5-(phenylaminomethyl)indol-2-yl)isoindolinone (63.0 mg, yield 92%).

1. extractionextracted with ethyl acetate
2. washThe organic layer was washed with saturated aqueous sodium hydrogencarbonate solution and saturated brine
3. dry with materialdried over anhydrous sodium sulfate
4. customThe solvent was evaporated under reduced pressure