The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
May. 30, 2006

Filed:

Apr. 23, 2004
Applicants:

Alexander F. Zabudkin, Donetsk, UA;

Victor Matvienko, Donetsk, UA;

Alexey Matvyeyev, Donetsk, UA;

Aleksandr M. Itkin, San Diego, CA (US);

Inventors:

Alexander F. Zabudkin, Donetsk, UA;

Victor Matvienko, Donetsk, UA;

Alexey Matvyeyev, Donetsk, UA;

Aleksandr M. Itkin, San Diego, CA (US);

Assignee:

Solux Corporation, San Diego, CA (US);

Attorney:
Primary Examiner:
Assistant Examiner:
Int. Cl.
CPC ...
C07H 15/24 (2006.01);
U.S. Cl.
CPC ...
Abstract

A method of synthesizing 4-R-substituted anthracyclines and their corresponding salts from 4-demethyldaunorubicin includes the steps of treating 4-demethyldaunorubicin with a sulfonylating agent to form 4-demethyl-4-sulfonyl-R-daunorubicin. 4-Demethyl-4-R-sulfonyl-daunorubicin is then subject to a reducing agent in the presence of a transition metal catalyst in a temperature range of about 30° C. to about 100° C. in a polar aprotic solvent in an inert atmosphere. Protected 4-demethoxy-4-R-daunomycin then undergoes hydrolysis in a basic solution to form the 4-R-substituted anthracyclines. The novel method lacks the step of forming a stereospecific glycoside bond between aglycone and aminoglycoside. The method also increases the yield of the final product up to 30 to 40%.


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