Reaktion #166619

ord-ceca31226c3d4a3fa1ef72d7b200bc92

Reaktionsbedingungen

Temperatur
60°CELSIUS
Detaillierte Bedingungen
See reaction.notes.procedure_details.

Aufarbeitung

  1. 1
    Temperaturto cool the solvent
  2. 2
    Sonstigewas removed under vacuum
  3. 3
    Sonstigeto give a brown solid
  4. 4
    workup.DISSOLUTIONto dissolve
  5. 5
    SonstigeThe phases were separated
  6. 6
    Extraktionthe bicarbonate solution was extracted further with ethyl acetate (50 mL)
  7. 7
    TrocknenThe combined ethyl acetate extracts were dried over sodium sulfate
  8. 8
    Filtrationfiltered
  9. 9
    Einengenconcentrated under vacuum
  10. 10
    Sonstigeto give a solid
  11. 11
    Wascheneluting with ethyl acetate
  12. 12
    workup.ADDITIONFractions containing the product
  13. 13
    Einengenwere concentrated

Vorschrift

4-((2,2-Dimethyl-1,3-dioxolan-4-yl)methoxy)pyridin-2-amine (5.6 g, 0.025 mol) was mixed with ethanol (60 mL) in a reaction flask, under an atmosphere of dry nitrogen. A solution of ethyl 2-chloro-3-oxopropanoate (5% in benzene; 93 mL; Commercial solution from Toronto Research Chemicals Inc.) was added. The mixture was heated to 60° C. under nitrogen for 2 hours. After allowing the mixture to cool the solvent was removed under vacuum to give a brown solid. The solid was mixed with ethyl acetate (200 mL) and sodium bicarbonate solution (100 mL) and stirred to dissolve. The phases were separated and the bicarbonate solution was extracted further with ethyl acetate (50 mL). The combined ethyl acetate extracts were dried over sodium sulfate, filtered and concentrated under vacuum to give a solid. The crude material was dissolved in ethyl acetate and passed through a short column of silica, eluting with ethyl acetate. Fractions containing the product were concentrated to give ethyl 7-((2,2-dimethyl-1,3-dioxolan-4-yl)methoxy)imidazo[1,2-a]pyridine-3-carboxylate as a pale yellow solid (5.76 g).

Quelle

DOI: 10.6084/m9.figshare.5104873.v1Patent: US08841455B2uspto-grants-2014_09