Semi-synthetic conversion of paclitaxel to docetaxel

US20070027332A1Inactive Publication Date: 2007-02-01INNOVATIONAL HLDG LLC

Patent Information

Authority / Receiving Office
US · United States
Patent Type
Applications(United States)
Current Assignee / Owner
INNOVATIONAL HLDG LLC
Publication Date
2007-02-01
Estimated Expiration
Not applicable · inactive patent

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Abstract

A process is provided for the semi-synthesis of taxane derivatives useful in the preparation of docetaxel, in particular, the semi-synthesis of protected taxane derivatives in a one pot reaction of protecting the C-2′, C-7 and C-10 and introducing a t-Boc group at the nitrogen of the amide group at the C-3′ position in paclitaxel and subsequently conversion to docetaxel, and derivatives used therein.
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Description

CROSS-REFERENCE TO RELATED APPLICATION

[0001] This application is a continuation of U.S. patent application Ser. No. 10 / 881,711 filed Jun. 29, 2004, now pending, which application is incorporated herein by reference in its entirety.BACKGROUND OF THE INVENTION

[0002] 1. Field of the Invention

[0003] The present invention relates to a semi-synthesis of taxane derivatives useful in the preparation of docetaxel, from pure or crude paclitaxel or related taxane starting material, in particular, the semi-synthesis of protected taxane derivatives in a one pot reaction and its conversion to docetaxel.

[0004] 2. Description of the Related Art

[0005] The taxane family of terpenes has received much attention in the scientific and medical community because the members of this family have demonstrated broad spectrum anti-leukemic and tumor-inhibitory activity. Docetaxel (1, Taxotere), a semi-synthetic analog, and paclitaxel (2, Taxol), a complex diterpene isolated from the bark of the Pacific yew...

Claims

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