Reaktion #3766

ord-46ef6b3fdcb74f75b3a22e357525e9cd

Reaktionsgleichung

CC(=O)O
acetic acid
CCN(CC)CC
triethylamine
O=P(Cl)(Oc1ccccc1)Oc1ccccc1
diphenyl chlorophosphate
O=C1CCC(=O)N1O
N-hydroxysuccinimide
CC(=O)ON1C(=O)CCC1=O
acetic acid succinimidyl ester
Ausbeute 70.0%

Reaktionsbedingungen

Detaillierte Bedingungen
See reaction.notes.procedure_details.

Aufarbeitung

  1. 1
    Sonstigerising to 41° C
  2. 2
    SonstigeA thick, white suspension resulted
  3. 3
    Temperaturheated at 45°-55° C. for 16 hours
  4. 4
    SonstigeAfter ending of the reaction
  5. 5
    Filtrationthe solid was filtered off
  6. 6
    Waschenwashed with 2×3 ml of ethyl acetate
  7. 7
    SonstigeThe combined filtrates were evaporated in vacuo
  8. 8
    Waschenthe semicrystalline residue which remained was washed
  9. 9
    SonstigeThe white solid thus obtained
  10. 10
    Filtrationwas filtered off
  11. 11
    Waschenwashed with 2×3 ml of ethanol
  12. 12
    Sonstigesucked dry
  13. 13
    Waschenwashed
  14. 14
    workup.STIRRINGby stirring with 10 ml of isopropanol
  15. 15
    FiltrationAfter filtering off
  16. 16
    Waschenwashing with 2×2 ml of isopropanol
  17. 17
    Sonstigedrying in vacuo

Vorschrift

1.27 g (0.011 mol) of N-hydroxysuccinimide were initially introduced into 10 ml of ethyl acetate, a solution of 3.22 g (0.012 mol) of diphenyl chlorophosphate in 10 ml of ethyl acetate was added and then a solution of 2.53 g (0.025 mol) of triethylamine in 10 ml of ethyl acetate was added dropwise in the course of 10 minutes, the temperature rising to 41° C. A thick, white suspension resulted, which was treated with a solution of 0.6 g (0.01 mol) of acetic acid in 10 ml of ethyl acetate and heated at 45°-55° C. for 16 hours. After ending of the reaction, the solid was filtered off and washed with 2×3 ml of ethyl acetate. The combined filtrates were evaporated in vacuo and the semicrystalline residue which remained was washed by stirring with 20 ml of ethanol for 30 minutes. The white solid thus obtained was filtered off, washed with 2×3 ml of ethanol, sucked dry and then washed by stirring with 10 ml of isopropanol. After filtering off, washing with 2×2 ml of isopropanol and drying in vacuo, 1.1 g (70%) of white acetic acid succinimidyl ester were obtained.

Quelle

DOI: 10.6084/m9.figshare.5104873.v1Patent: US05734064uspto-grants-1998_03