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Title:
METHOD OF PRODUCING 4-DEMETHOXYDAUNORUBICIN
Document Type and Number:
Japanese Patent JP2012232971
Kind Code:
A
Abstract:

To provide methods for the chemical synthesis of anthracycline compounds, more particularly, a method for the production of 4-demethoxydaunorubicin (idarubicin).

The present invention relates to a method for the synthesis of 4-demethoxydaunorubicin (idarubicin) having the chemical structure of formula (I), which involves the demethylation of 3'-Prot-daunorubicin in the presence of a soft Lewis acid. The method does not comprise cleavage of the glycosidic linkage at carbon C7, thus resulting in a faster synthesis cycle and an improved yield of the final product.


Inventors:
ZABUDKIN ALEXANDER
MATVIENKO VICTOR
MATVYEYEV ALEXEY
Application Number:
JP2012063036A
Publication Date:
November 29, 2012
Filing Date:
March 21, 2012
Export Citation:
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Assignee:
SYNBIAS PHARMA LTD
International Classes:
C07H15/252; A61K31/704; A61P35/02; C07B61/00
Domestic Patent References:
JPH021423A1990-01-05
JP2002255888A2002-09-11
JP2010526845A2010-08-05
JPH021423A1990-01-05
Foreign References:
US4188377A1980-02-12
US20040236086A12004-11-25
US20070135624A12007-06-14
US4188377A1980-02-12
Attorney, Agent or Firm:
Hatsushi Shimizu
Masao Haruna
Hirotaka Yamaguchi
Toshi Gobe
Ryuichi Inoue
Toshimitsu Sato
Koichi Niimi
Tomohiko Kobayashi
Shinichi Watanabe
Masato Ozeki
Yoshihiro Igarashi
Kazuya Kawamoto