反应 #1702031

ord-b59c5040c4d74c4eba154504c0cb4c58

反应方程式

CC[C@@]1(O)C(=O)OCc2c1cc1n(c2=O)Cc2cc3c(CN(C)C)c(O)ccc3nc2-1.Cl
topotecan hydrochloride
[Na]
sodium
N[C@@H](CS(=O)(=O)O)C(=O)O
cysteic acid
CC[C@@]1(O)C(=O)OCc2c1cc1n(c2=O)Cc2cc3c(CN(C)C)c(O)ccc3nc2-1
topotecan

溶剂

反应条件

详细条件
See reaction.notes.procedure_details.

后处理

  1. 1
    其他evaporated in vacuo
  2. 2
    workup.ADDITION120 ml sodium chloride solution (9 mg/ml) was added to the residue
  3. 3
    其他obtained
  4. 4
    其他after evaporation
  5. 5
    其他transparent (approx. 20 min)
  6. 6
    其他The solution obtained
  7. 7
    过滤was filtered through 0.2 mm
  8. 8
    过滤filter
  9. 9
    过滤The filtration

实验过程

Methanol stock-solutions of topotecan hydrochloride (120 ml, 1.09 mg/ml) and sodium salt of methyl ester of N-all-trans-retinoyl cysteic acid (32 ml, 15 mg/ml) were mixed in a 500 ml round-bottom flask and evaporated in vacuo. 120 ml sodium chloride solution (9 mg/ml) was added to the residue obtained after evaporation, and the mixture was stirred until it became clear and transparent (approx. 20 min). The concentration of topotecan in the obtained solution was 1 mg/ml, corresponding to a topotecan hydrochloride concentration of 1.09 mg/ml. The solution obtained was filtered through 0.2 mm filter. The filtration did not result in reduction of topotecan concentration.

来源

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