반응 #48011

ord-2fbe8299d8a94d909354b35d447df8ca

반응 조건

상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    온도The reaction is heated
  2. 2
    온도to reflux for 5 hours
  3. 3
    여과filtered
  4. 4
    기타The filtrate is evaporated
  5. 5
    추출extracted with ethyl acetate
  6. 6
    세척The combined organic phases are washed with brine
  7. 7
    건조dried (MgSO4)
  8. 8
    기타evaporated
  9. 9
    기타The crude product is purified by flash column chromatography (3:1-2:1 isohexanes-EtOAc gradient)

실험 절차

Sodium metal (0.345 g, 15.0 mmol) is dissolved in ethanol (20 ml) and diethyl malonate (0.713 g, 4.70 mmol) is added, followed by a suspension of 2,3-bis(chloromethyl)pyridine hydrochloride (Org. Process Res. Dev., 2002, 6, 938; 1.0 g, 4.70 mmol) in ethanol (15 ml) over 5 minutes. The reaction is heated to reflux for 5 hours, cooled to ambient temperature and filtered. The filtrate is evaporated, taken into water and extracted with ethyl acetate. The combined organic phases are washed with brine, dried (MgSO4) and evaporated. The crude product is purified by flash column chromatography (3:1-2:1 isohexanes-EtOAc gradient) to afford 5,7-dihydro-[1]pyrindine-6,6-dicarboxylic acid diethyl ester, MH+264.

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US07745462B2uspto-grants-2010_06