MODIFIED TAXOLS .6. PREPARATION OF WATER-SOLUBLE PRODRUGS OF TAXOL

被引：68
作者：
ZHAO, ZY
KINGSTON, DGI
CROSSWELL, AR
机构：
[1] VIRGINIA POLYTECH INST & STATE UNIV,DEPT CHEM,BLACKSBURG,VA 24061
[2] BRISTOL MYERS SQUIBB,WALLINGFORD,CT 06492
来源：
JOURNAL OF NATURAL PRODUCTS | 1991年 / 54卷 / 06期
关键词：
D O I：
10.1021/np50078a018
中图分类号：
Q94 [植物学];
学科分类号：
071001 ;
摘要：
Three H2O-soluble prodrugs of taxol have been prepared using a sulfonate group as the H2O-solubilizing group. The first two contain taurine or 3-amino-1-sulfopropionic acid linked to the 2'-position of taxol through a succinate group, and a novel method of preparing these derivatives is described. The third derivative is prepared by the Michael addition of bisulfite to 2'-acryloyltaxol. A 2'-(gamma-aminobutyryl)taxol salt was too unstable to be isolable.
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页码：1607 / 1611
页数：5
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