반응 #2396365

ord-cf10606eff4e4f6aaf979809a3c27649

반응 조건

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

후처리

  1. 1
    workup.STIRRINGAfter stirring for 1 hour
  2. 2
    온도to warm to ambient temperature
  3. 3
    workup.STIRRINGstirred for 17 hours
  4. 4
    기타After evaporation of methylene chloride
  5. 5
    workup.DISSOLUTIONthe residue was dissolved in water (50 ml)
  6. 6
    기타The precipitate was removed by filtration
  7. 7
    추출the filtrate was extracted with ethyl acetate (300 ml)
  8. 8
    세척The extract was washed with water
  9. 9
    건조dried over magnesium sulfate
  10. 10
    기타evaporated in vacuo
  11. 11
    기타The residue was chromatographed on silica gel (40 g)
  12. 12
    workup.ADDITIONThe fractions containing the desired compound
  13. 13
    농축concentrated under reduced pressure
  14. 14
    기타The residue was recrystallized from ethyl acetate

실험 절차

To a solution of trichloromethyl chloroformate (2.76 ml) in methylene chloride (200 ml) was added a solution of 3-aminopyridine (2.165 g) in methylene chloride (50 ml) and stirred for 2 hours at -50° C. The mixture was added to a mixture of N-amino-1,2,3,6-tetrahydropyridine hydrochloride (3.096 g) and triethylamine (2.327 g) in methylene chloride (100 ml) and the resultant mixture was stirred at the same temperature. After stirring for 1 hour, the reaction mixture was allowed to warm to ambient temperature and stirred for 17 hours. After evaporation of methylene chloride, the residue was dissolved in water (50 ml) and the resultant aqueous solution was adjusted to pH 8.0-8.5 with sodium bicarbonate. The precipitate was removed by filtration and the filtrate was extracted with ethyl acetate (300 ml). The extract was washed with water, dried over magnesium sulfate and evaporated in vacuo. The residue was chromatographed on silica gel (40 g) using chloroform. The fractions containing the desired compound were combined and concentrated under reduced pressure. The residue was recrystallized from ethyl acetate to give N-[(3-pyridylcarbamoyl)amino]-1,2,3,6-tetrahydropyridine (1.62 g).

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US04694004uspto-grants-1987_09