Title:
NEW ALKOXY SUBSTITUTED TAXANE AND MEDICINE COMPOSITION CONTAINING THE SAME
Document Type and Number:
Japanese Patent JP3217155
Kind Code:
B2
Abstract:
PURPOSE: To obtain a new compound useful as antileucemia, antitumor agent.
CONSTITUTION: The compound expressed by formula I [R1 is phenyl; R3 is CH3O-, CH3 CH2O-; Z is -OT1, -COT2 (T1 is H, a hydroxyl protecting group; T2 is H, a 1-6C alkyl, 1-6C alkenyl, 1-6C alkynyl, etc.; Ac is acetyl; E1 and E2 are each H, a hydroxyl protecting group, functional group], for example, N-dibenzoyl-N-methoxycarbonyltaxol, is obtained by allowing a β-lactam expressed by formula II (R2 is a hydroxy protecting group) to react with a metal alkoxide having a taxaneteracyclic nucleus and a C-13 metal oxide substituent expressed by formula III (T3 is H, a hydroxyl protecting group; M is Li, Mg, Na, etc.) to form the compound having a β-amide ester substituent in C-13. Dosage is 1 to 2 mg/kg with root in vein.
Inventors:
Robert a holton
Ronald J. Bydigger
Ronald J. Bydigger
Application Number:
JP27676392A
Publication Date:
October 09, 2001
Filing Date:
September 22, 1992
Export Citation:
Assignee:
Florida State University
International Classes:
A61K31/335; A61K31/337; A61P35/00; C07D305/14; C07D407/12; C07D409/12; C07F7/00; C07F7/18; C08G67/00; (IPC1-7): C07D305/14; A61K31/335; A61P35/00
Domestic Patent References:
| JP5239055A | ||||
| JP6330479A |
Other References:
【文献】国際公開91/13066(WO,A1)
Attorney, Agent or Firm:
Motohiro Kurauchi (1 outside)