METHOD OF PREPARING TAXANE DERIVATIVES.,申请号EP19930921984-传众专利搜索

METHOD OF PREPARING TAXANE DERIVATIVES.

申请公布号：EP0663908(A1)

申请号：EP19930921984

申请日期：1993.10.04

申请公布日期：1995.07.26

申请人：

RHONE-POULENC RORER S.A.

发明人：COMMERCON, ALAIN;DIDIER, ERIC;FOUQUE, ELIE

分类号：A61K31/335;A61K31/337;A61K31/42;A61K31/421;A61P35/00;C07D263/04;C07D263/06;C07D305/14;C07D413/12;(IPC1-7):C07D305/14

主分类号：A61K31/335

摘要：<p>PCT No. PCT/FR93/00969 Sec. 371 Date Apr. 5, 1995 Sec. 102(e) Date Apr. 5, 1995 PCT Filed Oct. 4, 1993 PCT Pub. No. WO94/07879 PCT Pub. Date Apr. 14, 1994This 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, R1 is a benzoyl radical or an R2-O-CO- radical in which R2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl, R3 is a trihalomethyl radical or phenyl substituted by a trihalomethyl radical, R4 is a hydrogen atom or is the same as R1. <IMAGE> (I) <IMAGE> (VII)</p>