公开(公告)号：EP2581375A2

公开(公告)日：2013-04-17

申请号：EP11791980.3

申请日：2011-06-13

申请人： Medichem, S.A.

发明人： SOLDEVILLA MADRID, Nuria ,  VÁZQUEZ MARTÍNEZ, Manel

IPC分类号： C07D471/08

CPC分类号： A61K31/504 ,  C07D471/08

摘要： The present invention provides an improved method for preparing a compound of formula (IIIA), which is a varenicline synthesis intermediate. Furthermore, the present invention provides an improved method for preparing varenicline, or a salt or a solvate thereof. Moreover, the present invention provides a process for decolouring varenicline, or a salt or a solvate thereof. Moreover, the present invention provides a process for preparing varenicline L-tartrate, with an improved yield. Moreover, the present invention relates to the use of a compound of formula (V), or a salt or a solvate thereof, as reference marker and reference standard for evaluating the purity of varenicline, or a salt or a solvate thereof.

摘要翻译： 本发明提供了制备式（IIIA）化合物的改进方法，其为伐伦尼克合成中间体。 此外，本发明提供了制备伐伦尼克或其盐或溶剂合物的改进方法。 此外，本发明提供一种脱色伐伦碱或其盐或溶剂合物的方法。 此外，本发明提供了一种以提高的产率制备L-酒石酸伐伦碱的方法。 此外，本发明涉及式（V）化合物或其盐或溶剂合物作为评价伐伦尼克或其盐或溶剂化物的纯度的参考标准和参考标准的用途。

公开(公告)号：EP1213279B1

公开(公告)日：2004-09-15

申请号：EP00945958.7

申请日：2000-07-17

申请人： Medichem S.A.

发明人： ARNALOT I AGUILAR, Carmen ,  BOSCH I LLADO, Jordi ,  CAMPS GARCIA, Pelayo ,  ONRUBIA MIGUEL, Maria del Carmen ,  SOLDEVILLA MADRID, Nuria

IPC分类号： C07C213/08 ,  C07C217/74

CPC分类号： C07C213/08 ,  C07C217/74 ,  C07C2601/14

摘要： Process for producing venlafaxine and/or physiologically acceptable addition salts thereof, consisting in reacting a compound having the general formula (II) wherein R is a C1-C10 alkyl group, aryl group, aralkyl group or cycloalkyl group having from 3 to 6 carbon atoms, with an organomagnesian compound having the general formula (III) wherein X is a halogen atom and, if desired, a salt of venlafaxine can be obtained by reaction with a physiologically acceptable acid.

摘要翻译： 一种制备文拉法辛和/或其生理上可接受的加成盐的方法，其通过使通式（II）的化合物反应，其中R是3至6个碳原子的C 1 -C 10烷基，芳基，芳烷基或环烷基 与通式（III）的有机镁化合物，其中X是卤素原子，如果需要，通过与生理上可接受的酸反应形成所得文拉法新的盐。

公开(公告)号：EP1213279A1

公开(公告)日：2002-06-12

申请号：EP00945958.7

申请日：2000-07-17

申请人： Medichem S.A.

发明人： ARNALOT I AGUILAR, Carmen ,  BOSCH I LLADO, Jordi ,  CAMPS GARCIA, Pelayo ,  ONRUBIA MIGUEL, Maria del Carmen ,  SOLDEVILLA MADRID, Nuria

IPC分类号： C07C213/08 ,  C07C217/74

CPC分类号： C07C213/08 ,  C07C217/74 ,  C07C2601/14

摘要： A process for the preparation of venlafaxin and/or the physiologically acceptable addition salts thereof that consists of reacting a compound of general formula (II) where R is a C 1 -C 10 alkyl, aryl, aralkyl or cycloalkyl group of 3 to 6 atoms of carbon, with a organomagnesium compound of general formula (III) where X is an atom of halogen and, if desired, a salt of the thus obtained venlafaxin is formed by reaction thereof with a physiologically acceptable acid.

公开(公告)号：EP2160372A1

公开(公告)日：2010-03-10

申请号：EP08762874.9

申请日：2008-06-13

申请人： Medichem, S.A.

发明人： SOLDEVILLA MADRID, Nuria ,  BOSCH I LLADO, Jordi

IPC分类号： C07B57/00 ,  B01D15/38 ,  G01N30/68

CPC分类号： G01N30/88 ,  B01D15/3833 ,  G01N30/02 ,  G01N2030/884 ,  G01N2030/8877

摘要： The present invention relates to a method for differentiating and quantifying the enantiomers, thereby determining the enantiomeric purity, of darifenacin and its intermediate compounds and salts thereof. In addition, the invention relates to a method for differentiating and quantifying the enantiomers, thereby determining the enantiomeric purity of compounds of formula (I): wherein Y is hydrogen or a substituent of the formula (II): including the differentiation and quantification of compounds of formula (I) of varying enantiomeric purity from their corresponding enantiomers. The invention further relates to a process for preparing enantiomerically pure darifenacin using enantiomerically pure starting compounds which have been previously differentiated and quantified according to the method of the invention.

公开(公告)号：EP1960357A2

公开(公告)日：2008-08-27

申请号：EP06850474.5

申请日：2006-11-14

申请人： Medichem S.A.

发明人： SOLDEVILLA MADRID, Nuria

IPC分类号： C07D211/32

CPC分类号： C07D211/32

摘要： The invention relates to a process for preparing 2- (l-benzylpiperidin-4- ylmethyliden) -5, 6-dimethoxyindan-l-one (a key intermediate in the synthesis of donepezil hydrochloride), crystalline polymorph forms of this key intermediate and their use thereof for producing donepezil hydrochloride. In particular, the invention provides a method for producing the intermediate 2-(l -benzylpiperidin-4-ylmethyliden) -5, 6- dimethoxyindan-1-one. The process includes reacting 5, 6-dimethoxyindan-l-one with l-benzylpiperidine-4-carbaldehyde using potassium hydroxide in an aqueous solvent. The aqueous solvent can be a mixture of an organic solvent and water. Where the organic solvent is not miscible with water, the reaction may be performed in the presence of a phase transfer catalyst.

公开(公告)号：EP1896455A2

公开(公告)日：2008-03-12

申请号：EP06848846.9

申请日：2006-06-06

申请人： Medichem, S.A.

发明人： SOLDEVILLA MADRID, Nuria

IPC分类号： C07D403/10 ,  A61K31/4184 ,  A61P9/00

CPC分类号： C07D403/10 ,  Y02P20/55

摘要： The invention provides a method for preparing candesartan cilexetil and related tetrazolyl compounds. More particularly, the invention relates to the preparation of candesartan cilexetil and related tetrazolyl compounds and includes a method of removing a protective group (e.g., triphenylmethane (trityl) protecting group) from an N-protected tetrazolyl compound using a Lewis acid in an inert solvent and in the presence of an alcohol (e.g., reacting an N-protected tetrazolyl compound with ZnCl2 in the presence of an alcohol).