反应详情

In a similar manner to Step 2 of Example 6, 4,5-dichloro-7-[1-(tert-butoxycarbonyl)-5-formylindol-2-yl]isoindolinone (115 mg, 0.258 mmol) was dissolved in acetonitrile (8.1 mL), and the solution was treated with 1-(2-hydroxyethyl)piperazine (134 mg, 1.03 mmol), acetic acid (0.295 mL, 5.16 mmol) and sodium triacetoxyborohydride (191 mg, 0.903 mmol). The reaction mixture was added with 1 mol/L hydrochloric acid and extracted with ethyl acetate. The organic layer was washed with sodium carbonate and saturated brine and dried over anhydrous sodium sulfate. The solvent was evaporated under reduced pressure to obtain 4,5-dichloro-7-{1-(tert-butoxycarbonyl)-5-[4-(2-hydroxyethyl)pyperazin-1-ylmethyl]indol-2-yl}isoindolinone (136 mg, yield 94%).

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