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 (42.6 mg, 0.104 mmol) was dissolved in acetonitrile (2 mL), and the solution was treated with 2-piperadinone (42 mg, 0.42 mmol), acetic acid (0.120 mL, 2.10 mmol) and sodium triacetoxyborohydride (46 mg, 0.22 mmol). The reaction mixture was added with water and sodium carbonate to adjust the pH to 9. The mixture was extracted 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-(3-oxopiperazin-1-ylmethyl)indol-2-yl]isoindolinone (55.6 mg).

1. extractionThe mixture was extracted 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