반응 #1753219

ord-02f55ea4b9014151b06c6b99a89e175b

반응 조건

온도
5°CELSIUS
상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    기타was adjusted to 35° C
  2. 2
    workup.ADDITIONwas added dropwise over 2 hours
  3. 3
    기타The reaction mixture was further reacted for 4.5 hours
  4. 4
    기타to obtain a reaction solution
  5. 5
    workup.ADDITIONwas added
  6. 6
    추출was then extracted with ethyl acetate
  7. 7
    세척The organic layer was washed with saturated saline
  8. 8
    농축concentrated
  9. 9
    기타to obtain residues
  10. 10
    기타The residues were subjected to recrystallization from 60 ml of 28% ammonia water and 1350 ml of 2-propanol

실험 절차

73.8 g (352 mmol) of indol-3-pyruvic acid was added to and dissolved in 917 g of 1.6 wt % aqueous sodium hydroxide. The temperature of the reaction solution was adjusted to 35° C. While the pH of the solution was kept at 11.1 with 30% aqueous sodium hydroxide, 310.2 g (1761 mmol) of 50% aqueous pyruvic acid was added dropwise over 2 hours. The reaction mixture was further reacted for 4.5 hours to obtain a reaction solution containing 4-hydroxy-4-(3-indolylmethyl)-2-ketoglutaric acid. While the pH of this reaction solution was kept at 7 with 30% aqueous sodium hydroxide, 367.2 g (2114 mmol) of 40% aqueous hydroxylamine hydrochloride was added thereto, and the mixture was stirred at 5° C. for 17.5 hours. The pH value of the reaction solution was adjusted to 2 with concentrated hydrochloric acid, and its organic matter was then extracted with ethyl acetate. The organic layer was washed with saturated saline and then concentrated to obtain residues. The residues were subjected to recrystallization from 60 ml of 28% ammonia water and 1350 ml of 2-propanol to obtain 43.4 g of 4-hydroxy-4-(3-indolylmethyl)-2-hydroxyiminoglutarate diammonium salt (142 mmol: yield 40% relative to indol-3-pyruvic acid) as crystals.

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US08043836B2uspto-grants-2011_10