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1.发明公开ENZYMATIC RESOLUTION OF RACEMIC (2R,S)-2-(ACETYLAMINO)-3-METHOXY-N-(PHENYLMETHYL)PROPANAMIDE 审中-公开的外消旋酶拆分（2R，S）-2-（乙酰基氨基）-3-甲氧基-N-（苯基甲基）丙酰胺
公开(公告)号：EP2582833A1
公开(公告)日：2013-04-24
申请号：EP11736163.4
申请日：2011-06-15
申请人： Medichem, S.A.
IPC分类号： C12P13/02
CPC分类号： C12P41/006 , C12P13/02 , C12P41/007 , C12Y301/01003
摘要： The present invention is concerned with a process of preparing (R)-lacosamide. The process comprises providing an (R,S)-lacosamide precursor and contacting the same with at least an enzyme in the presence of a solvent. The enzyme either stereoselectively hydrolyzes or acetylates an (R)- or (S)-enantiomer of the (R,S)-lacosamide precursor. The process further comprises where appropriate also concurrently, or successively, employing one or more reagents capable of converting the hydrolysed or acetylated (R)- or (S)-enantiomer to (R)- lacosamide.
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公开(公告)号：EP2303829A2
公开(公告)日：2011-04-06
申请号：EP09750194.4
申请日：2009-05-21
申请人： Medichem, S.A.
IPC分类号： C07C209/86 , C07C209/84
CPC分类号： C07C209/84 , C07C209/86 , C07C2602/08 , C07C211/42
摘要： The invention relates to processes for preparing rasagiline mesylate that avoid the use of alcohol solvents, thereby producing rasagiline mesylate free of any alkyl mesylates, including isopropyl mesylate. The invention further relates to processes for purifying rasagiline mesylate to obtain a product free of alkyl mesylates, and to the thus obtained rasagiline mesylate.
摘要翻译： 本发明涉及制备甲磺酸雷沙吉兰的方法，其避免使用醇溶剂，从而生产不含任何甲磺酸烷基酯（包括甲磺酸异丙酯）的甲磺酸雷沙吉兰。 本发明进一步涉及纯化甲磺酸雷沙吉兰以获得不含甲磺酸烷基酯的产物的方法，并涉及由此获得的甲磺酸雷沙吉兰。
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3.发明授权
公开(公告)号：EP1885727B1
公开(公告)日：2010-03-03
申请号：EP06809025.7
申请日：2006-05-03
申请人： Medichem, S.A.
IPC分类号： C07D491/10
CPC分类号： C07D491/10
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4.发明授权
公开(公告)号：EP1971573B1
公开(公告)日：2009-10-14
申请号：EP06850451.3
申请日：2006-12-22
申请人： Medichem S.A.
IPC分类号： C07D205/08 , C07D263/24
CPC分类号： C07D205/08
摘要： The invention relates, in general, to an improved process for the preparation of the compounds (3R,4S)-4-(4-(benzyloxy)phenyl)-l-(4-fluorophenyl)-3-[3-(4-fluorophenyl)-3- oxopropyl]azetidin-2-one and (3R,4S)-l-(4-fluorophenyl)-3-[3-(4-fluorophenyl)-3-oxopropyl]- 4-(4-hydroxyphenyl)-azetidin-2-one, which are key intermediates for the synthesis of ezetimibe, as well as the use of these intermediates for the preparation of ezetimibe.
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5.发明授权
公开(公告)号：EP1426356B1
公开(公告)日：2008-04-16
申请号：EP01969812.5
申请日：2001-09-14
申请人： Medichem S.A.
发明人： BOSCH I LLADO, Jordi , CAMPS GARCIA, Pelayo , CONTRERAS LASCORZ, Juan , ONRUBIA MIGUEL, Ma Carmen
IPC分类号： C07C233/11 , C07C231/02 , C07D241/04
CPC分类号： C07C237/22 , C07D241/04
摘要： The invention relates to intermediate compounds that are used for the preparation of mirtazapine and the production methods thereof. The inventive method is used to produce (+/-)-3-phenyl-1-methylpiperazine which is an important intermediate for the production of mirtazapine. Said method consists in subjecting novel compounds having general formula (I), wherein Z is a leaving group that can undergo nucleophilic displacement, to a cyclization reaction in the presence of a reducing agent. The invention also relates to a method of producing novel compounds having formula (I).
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6.发明公开NEW PROCESS FOR THE PREPARATION OF A LEUKOTRIENE ANTAGONIST 审中-公开新方法用于生产EINESLEUKOTRIENANTAGONISTEN
公开(公告)号：EP1817289A1
公开(公告)日：2007-08-15
申请号：EP04798127.9
申请日：2004-11-30
申请人： Medichem, S.A.
IPC分类号： C07D215/18
CPC分类号： C07D215/18
摘要： The present invention relates to a novel process for the preparation of montelukast sodium, a compound of Formula (1b) and precursors thereof. The invention further concerns the free acid of this compound in crystalline form, obtainable for the first time by the new process.
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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。
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公开(公告)号：EP1162202B1
公开(公告)日：2002-10-23
申请号：EP00909370.9
申请日：2000-03-13
申请人： Medichem S.A.
IPC分类号： C07D405/12
CPC分类号： C07D405/12
摘要： The invention relates to a method for obtaining polymorph A from doxazosine mesylate, essentially consisting in reacting the basic doxazosine with methanesulphonic acid in a mixture of solvents containing an alcohol and a chlorinated solvent, subsequently eliminating the chlorinated solvent by distillation and precipitating the desired product in an alcohol after previously heating the resulting suspension to solvent reflux temperature.
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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.
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公开(公告)号：EP3717521A1
公开(公告)日：2020-10-07
申请号：EP18804644.5
申请日：2018-11-26
申请人： Medichem, S.A.
IPC分类号： C08B37/16
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