Title:
METHOD OF PREPARING AMINO ACID TAXANE DERIVATIVE AND POLYMER CONJUGATE CONTAINING THE SAME
Document Type and Number:
Japanese Patent JP2011093921
Kind Code:
A
Abstract:
To provide a method of preparing amino acid-substituted taxanes useful as intermediates in the production of polymer conjugated taxanes or as a part of pharmaceutically acceptable formulations.
The method for preparing the amino acid-substituted taxanes comprises coupling of a blocked amino acid to taxanes, and deprotection with about an equimolar amount of a secondary amine to substantially avoid base-catalyzed hydrolysis of amino acid from the taxane of formula (4).
Inventors:
ZHAO HONG
GREENWALD RICHARD B
GREENWALD RICHARD B
Application Number:
JP2010292710A
Publication Date:
May 12, 2011
Filing Date:
December 28, 2010
Export Citation:
Assignee:
ENZON PHARMACEUTICALS INC
International Classes:
C07D305/08; A61K47/48; C07D305/14; C07D409/12; A61K31/337
Domestic Patent References:
| JP2006508926A | 2006-03-16 |
Attorney, Agent or Firm:
Yusuke Hiraki
Satoshi Fujita
Eiichi Arai
Natsuo Tanaka
Satoshi Fujita
Eiichi Arai
Natsuo Tanaka