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1. 发明申请

WO2007063523A1 INTERMEDIATES AND PROCESS FOR THE PREPARATION OF AROMATIC DERIVATIVES OF 1-ADAMANTANE 审中-公开
标题翻译：制备1-ADAMANTANE的芳族衍生物的中间体和方法
公开(公告)号：WO2007063523A1
公开(公告)日：2007-06-07
申请号：PCT/IB2006/054548
申请日：2006-12-01
申请人： FINORGA SAS , COMELY, Alexander Christian , MARFIL SÁNCHEZ, Marta , RAFECAS JANÉ, Llorenç , RIERA ESCALÉ, Antoni
发明人： COMELY, Alexander Christian , MARFIL SÁNCHEZ, Marta , RAFECAS JANÉ, Llorenç , RIERA ESCALÉ, Antoni
IPC分类号： C07C51/08 , C07C43/23 , C07C255/54 , C07C309/65
CPC分类号： C07C309/65 , C07C43/23 , C07C51/08 , C07C253/14 , C07C253/30 , C07C255/54 , C07C2603/74 , C07C65/26
摘要： Process for the preparation of aromatic derivatives of 1 -adamantane (tricyclo[3.3.1.1 (3,7)]decane), or an acceptable pharmaceutical salt thereof, based on a hydrolysis reaction of a precursor cyano compound. It also comprises different processes for obtaining the cyano compound. It is especially useful for obtaining Adapalene on an industrial scale in high yield and purity. It also comprises new intermediates useful in said preparation process.
摘要翻译：基于前体氰基化合物的水解反应制备1-金刚烷（三环[3.3.1.1（3,7）]癸烷）或其可接受的药物盐的芳族衍生物的方法。它还包括获得氰基化合物的不同方法。在工业规模上以高产率和纯度获得阿达帕林特别有用。它还包括在所述制备过程中有用的新中间体。

2. 发明申请

WO2006067216A2 INTERMEDIATE COMPOUNDS FOR THE PREPARATION OF AN ANGIOTENSIN II RECEPTOR ANTAGONIST 审中-公开
标题翻译：用于制备ANGIOTENSIN II受体拮抗剂的中间体化合物
公开(公告)号：WO2006067216A2
公开(公告)日：2006-06-29
申请号：PCT/EP2005/057104
申请日：2005-12-22
申请人： ENANTIA, S. L. , RAFECAS JANÉ, Llorenç , RIERA ESCALÉ, Antoni , ÉCIJA QUERALT, Marta , MOYANO BALDOIRE, Albert , COMELY, Alex , CASALPRIM CASTELLÀ, Irene
发明人： RAFECAS JANÉ, Llorenç , RIERA ESCALÉ, Antoni , ÉCIJA QUERALT, Marta , MOYANO BALDOIRE, Albert , COMELY, Alex , CASALPRIM CASTELLÀ, Irene
IPC分类号： C07D257/04 , C07F5/02
CPC分类号： C07D257/04 , C07F5/025
摘要： It comprises new substituted 4-valinylmethylphenyl boronic acids and their derivatives and also its preparation process. It also comprises a preparation process of Valsartan from such intermediates. The process comprises the reaction of the new 4-valinylmethylphenyl boronic compounds with a (halophenyl)tetrazole compound which proceeds with high yields. The process is particularly advantageous in its practical industrial realization because it avoids the use of azide derivatives and also the use of expensive biphenyl intermediates.
摘要翻译：它包含新的取代的4-缬氨基甲基苯基硼酸及其衍生物及其制备方法。它还包括从这样的中间体制备缬沙坦的制备方法。该方法包括新的4-缬烯基甲基苯基硼化合物与以高产率进行的（卤代苯基）四唑化合物的反应。该方法在其实际的工业实现中是特别有利的，因为它避免使用叠氮化物衍生物以及使用昂贵的联苯中间体。

3. 发明申请

WO2008046950A1 LIGANDOS QUIRALES BIDENTADOS DE TIPO P,S Y SU USO EN LA REACCIÓN DE PAUSON-KHAND 审中-公开
标题翻译： P，S型BIDENTATE CHIRAL LIGANDS及其在PAUSON-KHAND反应中的应用
公开(公告)号：WO2008046950A1
公开(公告)日：2008-04-24
申请号：PCT/ES2007/070174
申请日：2007-10-16
申请人： ENANTIA, S.L. , SOLÀ OLLER, Jordi , VERDAGUER ESPAULELLA, Xavier , RIERA ESCALÉ, Antoni
发明人： SOLÀ OLLER, Jordi , VERDAGUER ESPAULELLA, Xavier , RIERA ESCALÉ, Antoni
IPC分类号： C07F9/50 , C07F5/02 , C07F15/06 , C07C49/623 , C07C49/643 , C07C49/737 , C07B53/00
CPC分类号： C07F9/46 , C07B53/00 , C07F15/06 , C07F15/065
摘要： Se proporcionan nuevos ligandos quirales bidentados enantioméricamente enriquecidos de fórmula (I) o sus correspondientes enantiómeros de fórmula (I') que forman una coordinación tipo puente con complejos de dicobaltohexacarbonilo, en particular de manera diastereoselectiva cuando el alquino es monosustituido o disustituido con los dos sustituyentes diferentes. Se proporciona asimismo un procedimiento para la preparación de dichos ligandos quirales y un procedimiento para la preparación de los complejos de alquino-dicobaltotetracarbonilo. Los nuevos complejos de alquino-dicobaltotetracarbonilo formados permiten llevar a cabo la reacción de Pauson-Khand de manera enantioselectiva y con rendimientos elevados y, por tanto, son útiles en la síntesis de productos ciclopentánicos farmacéuticos y/o con actividad biológica.
摘要翻译：本发明涉及具有式（I）的对映体富集的双齿手性配体或其相应的对映异构体，具有式（I'），其与六钴基复合物形成桥键配位，特别是当炔被单取代或二取代时，以非对映选择性方式两个不同的取代基。本发明还涉及制备所述手性配体的方法以及制备炔烃 - 二羰基四羰基络合物的方法。所得到的新型炔 - 二钴四羰基络合物可用于以对映选择性方式和增加的产率进行Pauson-Khand反应，因此适用于合成生物活性和/或药物环戊烷产物。

4. 发明申请

WO2006067215A3 INTERMEDIATE COMPOUNDS FOR THE PREPARATION OF ANGIOTENSIN II RECEPTOR ANTAGONISTS 审中-公开
公开(公告)号：WO2006067215A3
公开(公告)日：2006-06-29
申请号：PCT/EP2005/057102
申请日：2005-12-22
申请人： ALGRY QUÍMICA, S. L. , DÍAZ MARTÍNEZ, Adolfo , RAFECAS JANÉ, Llorenç , RIERA ESCALÉ, Antoni , PASTÓ AGUILÀ, Mireia , ÉCIJA QUERALT, Marta
发明人： DÍAZ MARTÍNEZ, Adolfo , RAFECAS JANÉ, Llorenç , RIERA ESCALÉ, Antoni , PASTÓ AGUILÀ, Mireia , ÉCIJA QUERALT, Marta
IPC分类号： C07D233/22 , C07D233/32 , C07D235/02 , C07F5/02 , C07F5/05
摘要： It comprises new substituted heterocyclic methylphenyl boronic acids and their derivatives and also its preparation process. It also comprises a preparation process of Angiotensin II (A-II) receptor antagonists from such intermediates. The process includes the step of reacting the new substituted heterocyclic methylphenyl boronic compounds with a (halophenyl)tetrazole compound which proceeds with high yields. It allows to prepare the compounds of the present invention from a common intermediate compound, a N-protected- 5-(2-halogenphenyl)-1H-tetrazole, by a process which is particularly advantageous in its practical industrial realization because it avoids the use of azide derivatives and also the use of expensive biphenyl intermediates.

5. 发明申请

WO2011098160A1 ENANTIOMERICALLY ENRICHED AMINODIPHOSPHINES AS LIGANDS FOR THE PREPARATION OF CATALYSTS FOR ASYMMETRIC SYNTHESIS 审中-公开
标题翻译：作为制备不对称合成催化剂的配方的强化氨基磷酸酯
公开(公告)号：WO2011098160A1
公开(公告)日：2011-08-18
申请号：PCT/EP2010/065366
申请日：2010-10-13
申请人： ENANTIA, S.L. , ALONSO XALMA, Mónica , VERDAGUER ESPAULELLA, Xavier , REVÉS VILAPLANA, Marc , RIERA ESCALÉ, Antoni
发明人： ALONSO XALMA, Mónica , VERDAGUER ESPAULELLA, Xavier , REVÉS VILAPLANA, Marc , RIERA ESCALÉ, Antoni
IPC分类号： C07F9/46 , C07F15/00 , C07B53/00
CPC分类号： C07F9/46 , C07B53/00 , C07F15/0073
摘要： The present invention relates to enantiomerically enriched aminodiphosphine ligands where the chirality is located in the phosphorus atom and their preparation process, to catalysts containing them and their preparation process, as well as their use in asymmetric synthesis.
摘要翻译：本发明涉及手性浓缩的氨基二膦配体，其中手性位于磷原子及其制备方法中，含有它们的催化剂及其制备方法以及它们在不对称合成中的应用。

6. 发明申请

WO2011039290A1 A PROCESS FOR THE PREPARATION OF TRANS-(2R)-4-SUBSTITUTED-PIPECOLIC ACIDS AND ESTERS THEREOF, AND INTERMEDIATE COMPOUNDS USED THEREIN 审中-公开
标题翻译：一种制备转（2R）-4-取代的邻苯二甲酸及其酯的方法及其使用的中间体化合物
公开(公告)号：WO2011039290A1
公开(公告)日：2011-04-07
申请号：PCT/EP2010/064513
申请日：2010-09-30
申请人： ENANTIA, S.L. , RIERA ESCALÉ, Antoni , COMELY, Alexander Christian , GINESTA BUCH, Xavier
发明人： RIERA ESCALÉ, Antoni , COMELY, Alexander Christian , GINESTA BUCH, Xavier
IPC分类号： C07D211/48 , C07D401/12
CPC分类号： C07D211/48 , C07D401/12
摘要： Process for the preparation of a compound of formula (III) wherein R 1 is a (C 1 - C 10 )-alkyl radical or a radical of one of the known ring systems with 1 -3 rings, the rings being aromatic and being isolated or partially/totally fused and having 5-6 members, being each member independently selected from C, CH, N, NH, O, S; and the ring system being optionally substituted by one or more radicals independently selected from (C 1 -C 6 )-alkyl, (C 1 -C 6 )-alkoxy, and halogen; the process comprising: a) reacting a (C 1 -C 10 )-alkyl lithium, or a lithium salt of the ring system as defined above with a copper salt to obtain an organocuprate compound, and b) reacting the organocuprate compound obtained in step a) with di( tert -butyl) (2R)-3,6-dihydro-6-oxo-1,2(2H)- pyridinedicarboxylatejn an inert solvent system in the presence of a Lewis acid. Intermediate IV is new and is useful as an intermediate for the preparation of pharmaceutically active ingredients such as Argatroban.
摘要翻译：制备式（III）化合物的方法，其中R 1是（C 1 -C 10） - 烷基或具有1〜3个环的已知环体系之一的基团，所述环是芳族的并被隔离或部分/ 完全融合并具有5-6个成员，各自独立地选自C，CH，N，NH，O，S; 并且所述环系统任选地被一个或多个独立地选自（C 1 -C 6） - 烷基，（C 1 -C 6） - 烷氧基和卤素的基团取代; 所述方法包括：a）使（C1-C10） - 烷基锂或如上定义的环系的锂盐与铜盐反应，得到有机起始化合物，和b）使步骤a）中得到的有机铜化合物，与二（叔丁基）（2R）-3,6-二氢-6-氧代-1,2（2H） - 吡啶二羧酸二乙酯在惰性溶剂体系中在路易斯酸存在下反应。中间体IV是新的，并且可用作制备药学活性成分如阿加曲班的中间体。

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