反応 #1702032

ord-170cc3a8259f48feaeec895636c2ce05

反応方程式

CCc1c2c(nc3ccc(OC(=O)N4CCC(N5CCCCC5)CC4)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC.Cl.O.O.O
irinotecan hydrochloride trihydrate
[Na]
sodium
N[C@@H](CS(=O)(=O)O)C(=O)O
cysteic acid
CCc1c2c(nc3ccc(OC(=O)N4CCC(N5CCCCC5)CC4)cc13)-c1cc3c(c(=O)n1C2)COC(=O)[C@]3(O)CC
irinotecan

溶媒

反応条件

詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    その他evaporated in vacuo
  2. 2
    workup.ADDITION100 ml of water was added to the residue
  3. 3
    その他obtained
  4. 4
    その他after evaporation
  5. 5
    その他transparent (approx. 30 min)
  6. 6
    ろ過The obtained solution was filtered through 0.2 mm
  7. 7
    ろ過filter
  8. 8
    その他freeze dried
  9. 9
    ろ過The filtration

実験手順

Methanol stock-solutions of irinotecan hydrochloride trihydrate (100 ml, 1.15 mg/ml) and sodium salt of methyl ester of N-all-trans-retinoyl cysteic acid (27 ml, 15 mg/ml) were mixed in a 500 ml round-bottom flask and evaporated in vacuo. 100 ml of water was added to the residue obtained after evaporation and the mixture was stirred until it became clear and transparent (approx. 30 min). The concentration of irinotecan in the obtained solution was 1 mg/ml, corresponding to an irinotecan hydrochloride trihydrate concentration of 1.15 mg/ml. The obtained solution was filtered through 0.2 mm filter and freeze dried. The filtration did not result in reduction of irinotecan concentration.

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US08765173B2uspto-grants-2014_07