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Title:
2-DEBENZOYL-2-ACYLTAXOL DERIVATIVE AND ITS PRODUCTION
Document Type and Number:
Japanese Patent JPH06329650
Kind Code:
A
Abstract:

PURPOSE: To provide a compound exhibiting antitumor activity and useful in the treatment of cancer.

CONSTITUTION: A compound of formula I (wherein R1 represents substituted alkyl; R2 represents H, OH, oxy-protecting group or acyl; R3 represents H, OH or acyl; R4 represents H or OH; R5 represents H or acyl, but except for C(O)C6H5 and C(O)-3-hydroxyphenyl) is obtained by hydrolysis of 2'-7-trialkylsilyl- protected derivative of formula II (wherein R6 represents OH, oxy-protecting group or acyloxy; R7 represents substituted alkyl) under the phase transition conditions which allows its benzolyoxy substituent to be substituted with hydroxyl group in a mixture containing an aqueous sodium hydroxide, an organic solvent and a phase transition catalyst, whereby the taxol derivative may be derived to a analog containing modified substituent which has an aqueous solubility superior to taxol.


Inventors:
DEBITSUDO JII KEI KINGUSUTON
ASHIYOTSUKU GOPARU CHIYAUDOHAR
MIRINDO MORESUWAA GARUPUA
JIYON MACHIYUU RIMORUDEI
EI EI RESURII GANATERIKA
Application Number:
JP7625994A
Publication Date:
November 29, 1994
Filing Date:
March 10, 1994
Export Citation:
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Assignee:
VIRGINIA TECH INTELL PROP
International Classes:
A61K31/337; A61P35/00; A61K31/335; C07D305/14; C07D405/12; C07D409/12; C07F7/18; (IPC1-7): C07D305/14; A61K31/335
Attorney, Agent or Firm:
Takehiko Saito