Invention Grant
- Patent Title: Process for the preparation of taxane derivatives
- Patent Title (中): 紫杉烷衍生物的制备方法
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Application No.: US411690Application Date: 1995-04-05
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Publication No.: US5621121APublication Date: 1997-04-15
- Inventor: Alain Commercon , Eric Didier , Elie Fouque
- Applicant: Alain Commercon , Eric Didier , Elie Fouque
- Applicant Address: FRX Antony
- Assignee: Rhone-Poulenc Rorer S.A.
- Current Assignee: Rhone-Poulenc Rorer S.A.
- Current Assignee Address: FRX Antony
- Priority: FRX9211743 19921005
- Main IPC: A61K31/335
- IPC: A61K31/335 ; A61K31/337 ; A61K31/42 ; A61K31/421 ; A61P35/00 ; C07D263/04 ; C07D263/06 ; C07D305/14 ; C07D413/12
Abstract:
This invention relates to a method of preparing taxane derivatives of formula (I) by esterification of protected baccatin III or 10-deacetylbaccatin III by means of an acid of formula (VII), elimination of protection groupings and acylation of the amine function of the side chain. The products of formula (I) have remarkable antitumor and antileukemia properties. In formulae (I) and (VII): Ar stands for aryl, R is hydrogen or acetyl, R.sub.1 is a benzoyl radical or an R.sub.2 --O--CO-- radical in which R.sub.2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl, R.sub.3 is a trihalomethyl radical or phenyl substituted by a trihalomethyl radical, R.sub.4 is a hydrogen atom or is the same as R.sub.1. ##STR1##
Public/Granted literature
- US4968273A Water-borne vessel Public/Granted day:1990-11-06
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