Reaktion #11301

ord-578df404b51c42d4ba39c716919cc8b2

Lösungsmittel

Reaktionsbedingungen

Detaillierte Bedingungen
See reaction.notes.procedure_details.

Aufarbeitung

  1. 1
    TemperaturThe mixture was heated
  2. 2
    Temperaturto reflux
  3. 3
    Temperaturthen cooled
  4. 4
    Filtrationfiltered
  5. 5
    EinengenThe filtrate was concentrated under reduced pressure
  6. 6
    WaschenElution of the column with 9:1 dichloromethane/methanol

Vorschrift

To a mixture of adefovir (1.36 g, 5 mmol) and 3-hexadecyloxy-1-propanol (1.8 g, 6 mmol) in dry pyridine was added DCC (2.06 g, 10 mmol). The mixture was heated to reflux and stirred 18 h then cooled and filtered. The filtrate was concentrated under reduced pressure and the residue was applied to a short column of silica gel. Elution of the column with 9:1 dichloromethane/methanol yielded hexadecyloxypropyl-adefovir (HDP-ADV) as a white powder.

Quelle

DOI: 10.6084/m9.figshare.5104873.v1Patent: US07098197B2uspto-grants-2006_08