| 摘要 |
Sulfonated 2 min -acryloyltaxol and sulfonated 2 min -O-acyl acid taxol derivatives are synthesized which have improved water solubility and stability while maintaining bio-activity. In particular, 2 min -[(3-sulfo-1-oxopropyl)oxy] taxol sodium salt is synthesized by reacting taxol with acrylic acid, and subsequently reacting the 2 min -acryloyltaxol with bisulfite in a Michael reaction. 2 min -{[(4-((2-sulfoethyl)amino)-1,4-dioxobutyl)oxy}taxol sodium salt and 2 min -{[4-((3-sulfopropyl)amino)-1,4-dioxobutyl]oxy} taxol sodium salt are synthesized by reacting 2 min -succinyltaxol with the tetrabutylammonium salts of taurine and 3-amino-propyl sulfonic acid, respectively, and subsequently exchanging the ammonium with sodium. Glycol derivatives of 2 min -O-acyl acid taxols with improved water solubility are synthesized by reaction of a glycol with 2 min -O-acyl acid taxol. <IMAGE> |
