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 (30.0 mg, 0.0730 mmol) was dissolved in acetonitrile (2 mL), and the solution was treated with glycine ethylester hydrochloride (41.0 mg, 0.294 mmol), triethylamine (0.081 mL, 0.58 mmol), acetic acid (0.084 mL, 1.5 mmol) and sodium triacetoxyborohydride (77.0 mg, 0.360 mmol). The reaction mixture was added with water and sodium hydrogen carbonate, followed by extracting with ethyl acetate. The organic layer was washed with saturated brine and dried over anhydrous sodium sulfate. The solvent was evaporated under reduced pressure to obtain 4-chloro-7-[1-(tert-butoxycarbonyl)-5-(ethoxycarbonylmethylaminomethyl)indol-2-yl]isoindolinone (39.2 mg).

1. extractionby extracting with ethyl acetate
2. washThe organic layer was washed with saturated brine
3. dry with materialdried over anhydrous sodium sulfate
4. customThe solvent was evaporated under reduced pressure