반응 #68454

ord-851298e2ada047858e95d9b75aa367ec

반응 조건

온도
50°CELSIUS
상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    농축The reaction mixture was concentrated in vacuo
  2. 2
    기타The remaining oil was triturated with diethyl ether
  3. 3
    기타A gel-like solid formed which
  4. 4
    기타was collected on a glass frit
  5. 5
    세척washing with diethyl ether
  6. 6
    기타The solid was then triturated with ethyl acetate, and finally acetonitrile
  7. 7
    기타An amorphous solid formed which
  8. 8
    기타was collected on a glass frit
  9. 9
    세척washing with acetonitrile
  10. 10
    기타The solid was further dried under high vacuum
  11. 11
    농축In addition, the ethyl acetate filtrate was concentrated in vacuo
  12. 12
    기타The remaining oil was then triturated with acetonitrile
  13. 13
    기타An amorphous solid formed
  14. 14
    기타was collected on a glass frit
  15. 15
    세척washing with acetonitrile
  16. 16
    기타The solid was further dried under high vacuum

실험 절차

N′-(6-chloropyridazin-3-yl)-2-(7-methoxyquinolin-4-yloxy)acetohydrazide (2.53 g, 7.0 mmol) was suspended in tetrahydrofuran (50 mL) then added triphenylphosphine (2.8 g, 11 mmol) and trimethylsilyl azide (1.4 ml, 11 mmol). To this suspension, was added diethylazodicarboxylate (2.0 ml, 13 mmol) in rapid drops with a syringe. The mixture became clear and hot to the touch. The reaction mixture was heated at 50° C. for 30 minutes. The reaction mixture was concentrated in vacuo. The remaining oil was triturated with diethyl ether. A gel-like solid formed which was collected on a glass frit, washing with diethyl ether. The solid was then triturated with ethyl acetate, and finally acetonitrile. An amorphous solid formed which was collected on a glass frit, washing with acetonitrile. The solid was further dried under high vacuum. In addition, the ethyl acetate filtrate was concentrated in vacuo. The remaining oil was then triturated with acetonitrile. An amorphous solid formed and was collected on a glass frit, washing with acetonitrile. The solid was further dried under high vacuum affording 4-((6-chloro-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy)-7-methoxyquinoline as a tan solid. MS (ESI, pos. ion) m/z: 342.1 (M+1).

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US08524900B2uspto-grants-2013_09