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公开(公告)号：EP0912536A1
公开(公告)日：1999-05-06
申请号：EP97931868.0
申请日：1997-07-04
发明人： DIDIER, Eric , PECQUET, Pascal
IPC分类号： C07D305
CPC分类号： C07D305/14
摘要： The invention discloses a method for the selective monoacylation of hydroxy taxanes using a methylene iminium salt.
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公开(公告)号：EP0691951A1
公开(公告)日：1996-01-17
申请号：EP94911225.0
申请日：1994-03-25
发明人： DIDIER, Eric , LEON, Patrick
CPC分类号： C07C269/04 , C07C231/02 , C07C231/18 , C07C233/87
摘要： Method for the preparation of β-phenylisoserine derivatives of general formula (I) involving the action of an anhydride and hydrogen with a product of general formula (II). The products of general formula (I) are especially useful in the preparation of taxoids having outstanding antitumour properties. In general formulae (I) and (II), Ar is an aryl radical, Ph is a phenyl radical or an optionally substituted α or β-naphtyl, R is a hydrogen atom or an alkyl radical optionally substituted by a phenyl radical and R1 is an optionally substituted phenyl radical or a R2-O radical wherein R2 is an alkyl, alkenyl, cycloalkyl, phenyl or heterocyclyl.
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公开(公告)号：EP0663907B1
公开(公告)日：1997-01-15
申请号：EP93921983.8
申请日：1993-10-04
发明人： COMMERCON, Alain , DIDIER, Eric , FOUQUE, Elie
IPC分类号： C07D305/14 , C07D263/04 , C07D413/12
CPC分类号： C07D263/04 , C07D305/14 , C07D413/10 , Y02P20/55
摘要： Method of preparing taxane derivatives of general formula (I) by esterification of protected baccatine III or 10-deacetylbaccatine III by means of an acid of general formula (VII), deprotection of the side chain and elimination of the hydroxy function protection groupings. In general formulae (I) and (VII): Ar stands for aryl, R is hydrogen or acetyl, R1 is benzoyl or R2-O-CO- in which R2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl, and R3 is hydrogen, alkoxy, optionally substituted aryl.
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公开(公告)号：EP0663908A1
公开(公告)日：1995-07-26
申请号：EP93921984.0
申请日：1993-10-04
发明人： COMMER ON, Alain , DIDIER, Eric , FOUQUE, Elie
CPC分类号： C07D263/04 , C07D305/14 , C07D413/10 , C07D413/12 , Y02P20/55
摘要： Method of preparing taxane derivatives of formula (I) by esterification of protected baccatine III or 10-deacetylbaccatine 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.
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5.发明授权PROCEDE DE PREPARATION DU TRIHYDRATE DU (2R,3S)-3-BENZOYLAMINO-2-HYDROXY-3-PHENYLPROPIONATE DE 4,10-DIACETOXY-2ALFA-BENZOYLOXY-BETA,20-EPOXY-BETA-DIHYDROXY-9-OXO-TAX-11-EN-BETA-YLE 失效METHOD FOR PRODUCING 4,10-二乙酰氧基2ALFA苯甲酰氧基5-β三水合物，20-环氧1,7BETA二羟基-9-氧代税-11-CN-13ALFA基酯（2R，35） -3-苯甲酰氨基-2-羟基-3-苯基丙酸
公开(公告)号：EP0805806B1
公开(公告)日：1999-12-15
申请号：EP96901832.4
申请日：1996-01-23
IPC分类号： C07D305/14 , A61K31/335
CPC分类号： C07D305/14
摘要： A method for preparing 4,10-diacetoxy-2α-benzoyloxy-5β,20-epoxy-1,7β-dihydroxy-9-oxo-tax-11-en-yl-13α (2R,3S)-3-benzoylamino-2-hydroxy-3-phenylpropionate trihydrate by crystallisation from a water/alcohol solution.
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6.发明公开DIHYDRATE DU (2R,3S)-3-TERT-BUTOXYCARBONYLAMINO-2-HYDROXY-3-PHENYLPROPIONATE DE 4,10$g(b)-DIACETOXY-2$g(a)-BENZOYLOXY-5$g(b),20-EPOXY-1-HYDROXY-9-OXO-19-NOR-CYCLOPROPA G]TAX-11-ENE-13$g(a)-YLE, ET SON PROCEDE DE PREPARATION 失效二水合物（2R，3S）-3-叔丁氧羰基-2-羟基-3-苯基丙酸BETA-4,10-二乙酰氧基2ALFA苯甲酰氧基5beta，20-环氧基-1-羟基-9-氧代 - 19酯 -NOR环丙G] TAX-11-CN-13ALFA基及其制造方法
公开(公告)号：EP0876361A1
公开(公告)日：1998-11-11
申请号：EP96941720.0
申请日：1996-12-09
CPC分类号： C07D305/14
摘要： A 4,10β-diacetoxy-2α-benzoyloxy-5β,20-epoxy-1-hydroxy-9-oxo-19-nor-cyclopropa[g]tax-11-ene-13α-yl (2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate dihydrate, and the preparation thereof by crystallisation from a water-alcohol or water-ketone solution, are disclosed.
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公开(公告)号：EP0663908B1
公开(公告)日：1997-02-12
申请号：EP93921984.6
申请日：1993-10-04
发明人： COMMERCON, Alain , DIDIER, Eric , FOUQUE, Elie
IPC分类号： C07D305/14 , C07D263/04 , C07D413/12
CPC分类号： C07D263/04 , C07D305/14 , C07D413/10 , C07D413/12 , Y02P20/55
摘要： Method of preparing taxane derivatives of formula (I) by esterification of protected baccatine III or 10-deacetylbaccatine 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.
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公开(公告)号：EP0691951B1
公开(公告)日：1998-06-10
申请号：EP94911225.4
申请日：1994-03-25
发明人： DIDIER, Eric , LEON, Patrick
IPC分类号： C07C269/04 , C07C231/02 , C07D305/14
CPC分类号： C07C269/04 , C07C231/02 , C07C231/18 , C07C233/87
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9.发明公开PROCEDE DE PREPARATION DU TRIHYDRATE DU (2R,3S)-3-BENZOYLAMINO-2-HYDROXY-3-PHENYLPROPIONATE DE 4,10-DIACETOXY-2ALFA-BENZOYLOXY-BETA,20-EPOXY-BETA-DIHYDROXY-9-OXO-TAX-11-EN-BETA-YLE 失效METHOD FOR PRODUCING 4,10-二乙酰氧基2ALFA苯甲酰氧基5-β三水合物，20-环氧1,7BETA二羟基-9-氧代税-11-CN-13ALFA基酯（2R，35） -3-苯甲酰氨基-2-羟基-3-苯基丙酸
公开(公告)号：EP0805806A1
公开(公告)日：1997-11-12
申请号：EP96901832.0
申请日：1996-01-23
CPC分类号： C07D305/14
摘要： A method for preparing 4,10-diacetoxy-2α-benzoyloxy-5β,20-epoxy-1,7β-dihydroxy-9-oxo-tax-11-en-yl-13α (2R,3S)-3-benzoylamino-2-hydroxy-3-phenylpropionate trihydrate by crystallisation from a water/alcohol solution.
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公开(公告)号：EP0663907A1
公开(公告)日：1995-07-26
申请号：EP93921983.0
申请日：1993-10-04
发明人： COMMER ON, Alain , DIDIER, Eric , FOUQUE, Elie
CPC分类号： C07D263/04 , C07D305/14 , C07D413/10 , Y02P20/55
摘要： Method of preparing taxane derivatives of general formula (I) by esterification of protected baccatine III or 10-deacetylbaccatine III by means of an acid of general formula (VII), deprotection of the side chain and elimination of the hydroxy function protection groupings. In general formulae (I) and (VII): Ar stands for aryl, R is hydrogen or acetyl, R1 is benzoyl or R2-O-CO- in which R2 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl, and R3 is hydrogen, alkoxy, optionally substituted aryl.
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