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公开(公告)号：EP1335911B1
公开(公告)日：2004-05-06
申请号：EP01986686.2
申请日：2001-10-08
发明人： VILLANI, Flavio, Lab. Chimico InternationalS.p.A. , NARDI, Antonio, Lab. Chimico Internazional S.p.A. , SALVI, Annibale, Lab. Chimico Internazional S.p.A. , FALABELLA, G., Lab. Chimico Internazional S.p.A.
IPC分类号： C07D339/04
CPC分类号： C07D339/04
摘要： Process for the synthesis of R(+)α-lipoic acid comprising the following stages: a) Salifying of racemic 6,8-halo-octanoic acid with S(-)α-methylbenzylamine; b) separation by filtration of the crystallized diastereoisomeric salt of R(+)6,8-di-halo-octanoic acid-S(-)α-methylbenzylamine; c) purification by re-crystallization of the diastereoisomeric salt of R(+)6,8-di-halo-octanoic acid-S(-)α-methylbenzylamine; d) separation of the diastereoisomeric salt to obtain R(+)6,8-di-halo-octanoic acid by reation of said salt with strong mineral acids in an aqueous solution with a dilution between 2 and 10% by weight; e) esterification of R(+)6,8-di-halo-octanoic acid to obtain the corresponding alkyl ester; f) reaction of the alkyl ester of R(+)6,8-di-halo-octanoic acid in an organic solvent with an aqueous solution of alkali disulfide in presence of a compound for phase transfer catalysis; g) hydolysis of the ester of R(+)α-lipoic acid.
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公开(公告)号：EP1330450A2
公开(公告)日：2003-07-30
申请号：EP01986685.4
申请日：2001-10-08
发明人： VILLANI, FlavioLab.Chimico Internazionale S.P.A. , NARDI, AntonioLab.Chimico Internazionale S.P.A. , SALVI, AnnibaleLab.Chimico Internazionale S.P.A. , FALABELLA,GiovannaLab.Chimico Internazio.S.P.A.
IPC分类号： C07D339/04 , C07D319/06
CPC分类号： C07D339/04 , C07C319/06 , C07C323/60
摘要： Process for the synthesis of R(+)α-lipoic acid comprising the following stages: a) Salifying of racemic thioctic acid with R(+)α-methylbenzylamine; b) separation by filtration of the crystallized diastereoisomeric salt of R(+)α-lipoic acid-R(+)α-methylbenzylamine; c) purification by re-crystallization of the diastereoisomeric salt of R(+)α-lipoic acid-R(+)α-methylbenzylamine, in which the re-crystallization solvent consists of a mixture of non-polar/polar solvents; d) separation of the diastereoisomeric salt to obtain R(+)α-lipoic acid by reaction of said salt with acids selected from the group consisting of aliphatic hydroxy-carboxylic acids having 3 to 6 carbon atoms and aqueous phosphoric acid.
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公开(公告)号：EP0643694A1
公开(公告)日：1995-03-22
申请号：EP93912826.0
申请日：1993-05-28
CPC分类号： C07D487/04 , C07C233/25 , C07D209/34
摘要： A process for the preparation of 1,3-dimethyl-5-hydroxy-oxindole of formula (II) which comprises the reaction of 4-(N-methylamino)phenol with 2-halogen-propinol chloride and cyclization of the resulting compound in the presence of Lewis acids, and the conversion thereof to eserethole.
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34.发明公开A process for the preparation of 1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydro-pyrrole/2,3-b/indol-5(3aS,8aR)-heptylcarbamate 失效制备1,3a，8-三甲基-1,2,3,3a，8,8a-六氢 - 吡咯/ 2,3-b /吲哚-5（3aS，8aR） - 庚基氨基甲酸酯
公开(公告)号：EP0499179A1
公开(公告)日：1992-08-19
申请号：EP92102199.4
申请日：1992-02-10
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： A process for the preparation of 1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydro-pyrrole[2,3-b]indol-5(3aS,8aR)heptylcarbamate, of formula (I)
by reacting eseroline with heptylisocyanate in the presence of a metal cyanate and of a quaternary ammonium salt, in polar aprotic solvents.摘要翻译： （I）的1,3a，8-三甲基-1,2,3,3a，8,8a-六氢 - 吡咯[2,3-b]吲哚-5（3aS，8aR）庚基氨基甲酸酯的制备方法， ）通过在金属氰酸盐和季铵盐存在下在极性非质子传递溶剂中使eseroline与庚基异氰酸酯反应来制备。
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公开(公告)号：EP3122362A1
公开(公告)日：2017-02-01
申请号：EP15732035.9
申请日：2015-03-24
CPC分类号： A61K31/55 , A61K9/146 , A61K9/1611 , A61K9/1635 , A61K9/1641 , A61K9/1652
摘要： The subject-matter of the present invention is a novel, non-salified ivabradine solid form, in particular an ivabradine form adsorbed on an inert carrier. The subject-matter of the invention is also a process for preparing said solid form, its use in therapy and pharmaceutical compositions comprising it.
摘要翻译： 本发明的主题是一种新型的非盐化的伊伐布拉定固体形式，特别是吸附在惰性载体上的伊伐布雷定形式。 本发明的主题也是制备所述固体形式，其在治疗中的用途和包含其的药物组合物的方法。
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公开(公告)号：EP2739605B1
公开(公告)日：2016-04-27
申请号：EP11770507.9
申请日：2011-08-03
IPC分类号： C07C231/00 , C07C233/18
CPC分类号： C07C233/25 , C07B2200/13 , C07C231/22 , C07C233/18
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37.发明授权PROCESS FOR THE PREPARATION OF (R)-(-)-3-(CARBAMOYLMETHYL)-5-METHYLHEXANOIC ACID AND OF PREGABALIN AND SYNTHESIS INTERMEDIATES 有权用于生产（R） - （ - ） - 3-（氨基甲酰基甲基）-5-甲基己和普瑞巴林与合成中间体
公开(公告)号：EP2035368B1
公开(公告)日：2015-05-27
申请号：EP07766518.0
申请日：2007-06-06
IPC分类号： C07C211/27 , C07C215/28 , C07C227/32 , C07C229/08 , C07C231/20 , C07C233/05
CPC分类号： C07C231/20 , C07C211/27 , C07C215/28 , C07C227/32 , C07C233/05 , C07C229/08
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38.发明公开PROCESS FOR PRODUCING CHIRAL 1 - SUBSTITUTED 2 - PIPERIDINOLS EMPLOYING OXIDOREDUCTASES 有权生产手性1-取代2-哌啶醇使用氧化剂的方法
公开(公告)号：EP2861750A1
公开(公告)日：2015-04-22
申请号：EP12735330.8
申请日：2012-06-18
发明人： BERTOLINI, Giorgio , MAGRI', Paolo
IPC分类号： C12P13/00 , C12N9/02 , C07D211/00 , C12P17/12
CPC分类号： C12P17/12 , C07D211/42 , C12N9/0008 , Y02P20/52
摘要： The present invention relates to an enantioselective enzymatic process for the preparation of an optically active 3-hydroxypiperidinecarboxylic acid derivative.
摘要翻译： 本发明涉及用于制备光学活性3-羟基哌啶羧酸衍生物的对映体选择性酶促方法。
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公开(公告)号：EP2539331B1
公开(公告)日：2014-10-08
申请号：EP11709460.7
申请日：2011-01-26
发明人： SADA, Mara , NARDI, Antonio , MAIORANA, Stefano
IPC分类号： C07D307/82
CPC分类号： C07D307/82
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40.发明公开
公开(公告)号：EP2739610A1
公开(公告)日：2014-06-11
申请号：EP12772396.3
申请日：2012-07-31
发明人： NARDI, Antonio , DE ANGELIS, Bruno , CEREA, Paolangelo , RAFECAS, Jane, Llorenc , TESSON, Nicolas
IPC分类号： C07D223/16 , C07C213/10
CPC分类号： C07D223/16 , C07C53/134 , C07C57/30 , C07C209/46 , C07C211/04 , C07C213/10 , C07C215/50 , C07C2602/06 , Y02P20/582
摘要： The invention concerns a new process for the resolution of ivabradine and of intermediates of synthesis thereof.
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