반응 #49290

ord-84af0d98ff3348a18b8bc49b462fc0fb

반응 조건

상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    추출by extracting with ethyl acetate
  2. 2
    세척The organic layer was washed with saturated brine
  3. 3
    건조dried over anhydrous sodium sulfate
  4. 4
    기타The solvent was evaporated under reduced pressure

실험 절차

In a similar manner to Step 2 of Example 6, 4-chloro-7-[1-(tert-butoxycarbonyl)-5-formylindol-2-yl]isoindolinone (20.7 mg, 0.0504 mmol) was dissolved in acetonitrile (1 mL), and the solution was treated with 1-(2-hydroxyethyl)piperazine (28 mg, 0.22 mmol), acetic acid (0.232 mL, 4.05 mmol) and sodium triacetoxyborohydride (116 mg, 0.547 mmol). The reaction mixture was added with water and sodium 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-[4-(2-hydroxyethyl)piperazin-1-ylmethyl]indol-2-yl)isoindolinone (29.6 mg).

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US07745641B2uspto-grants-2010_06