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:
Jun. 22, 1999

Filed:

Jan. 21, 1998
Applicant:
Inventors:

Nicholas J Sisti, Boulder, CO (US);

Jan Zygmunt, Boulder, CO (US);

Herbert R Brinkman, Superior, CO (US);

Madhavi C Chander, Boulder, CO (US);

Xian Liang, Boulder, CO (US);

James D McChesney, Boulder, CO (US);

Assignee:

NaPro BioTherapeutics, Inc., Boulder, CO (US);

Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
C07D / ;
U.S. Cl.
CPC ...
549510 ; 549511 ;
Abstract

A method of acylating 10-deacetylbaccatin III at the C-10 position over the C-7 hydroxy position thereof to produce baccatin IIII is accomplished first by dissolving 10-deacetylbaccatin III in an acceptable ether solvent therefor, such as tetrahydrofuran. A lithium salt, preferably lithium chloride, is added. A trialkylamine base or pyridine is next added, followed by the addition of an acylating agent, such as acetyl chloride. The resulting solution may be quenched, for example with ammonium chloride, to eliminate excess of the acylating agent. The result is baccatin III in solution. This solution may then be diluted with ethyl acetate to form an organic phase and an aqueous phase, with the organic phase being washed and thereafter reduced. Recrystallization and column chromatography may be employed to purify the baccatin III.


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