THREE-STEP CONVERSION OF PROTECTED TAXANE ESTER TO PACLITAXEL

Title:

THREE-STEP CONVERSION OF PROTECTED TAXANE ESTER TO PACLITAXEL

Document Type and Number:

WIPO Patent Application WO2002085879

Kind Code:

B1

Abstract:

The present invention relates to a method of producing paclitaxel from a protected coupled ester compound having a formula: wherein P>1< is a hydrogenatable protecting group, comprising deprotecting the 7-O-position and 3'-N-position of the protected coupled ester compound to form a first intermediate compound, benzoylating the first intermediate compound at the 3?1>-N-position thereby to form a second intermediate compound, and deprotecting the second intermediate compound by replacing P1 with hydrogen in the presence of an acid. The present invention also provides chemical compounds useful in the production of paclitaxel.

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Inventors:

ZYGMUNT JAN
MCCHESNEY JAMES D

Application Number:

PCT/US2002/013288

Publication Date:

April 03, 2003

Filing Date:

April 25, 2002

Export Citation:

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Assignee:

NAPRO BIOTHERAPEUTICS INC (US)

International Classes:

A61K31/337; A61P35/00; B01J23/44; C07B61/00; C07D305/14; (IPC1-7): C07D305/14

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