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1. 发明申请

WO2012085209A1 PREPARATION PROCESS OF AN ANTIVIRAL DRUG (ENTECAVIR) AND INTERMEDIATES THEREOF 审中-公开
标题翻译：抗病毒药物（ENTECAVIR）及其中间体的制备方法
公开(公告)号：WO2012085209A1
公开(公告)日：2012-06-28
申请号：PCT/EP2011/073800
申请日：2011-12-22
申请人： ESTEVE QUÍMICA, S.A. , BARTRA SANMARTÍ, Martí , BERENGUER MAIMÓ, Ramón , VELASCO TURBAU, Javier , ARIZA PIQUER, Javier , FARRÀS SOLER, Jaime , GARCÍA GÓMEZ, Jorge
发明人： BARTRA SANMARTÍ, Martí , BERENGUER MAIMÓ, Ramón , VELASCO TURBAU, Javier , ARIZA PIQUER, Javier , FARRÀS SOLER, Jaime , GARCÍA GÓMEZ, Jorge
IPC分类号： C07D473/18 , C07D303/14 , C07D303/16 , C07C13/11 , C07F7/08
CPC分类号： C07D473/18 , C07D303/14 , C07D303/16 , C07F7/0818 , C07F7/1852 , C07F7/1856 , C07F7/1868
摘要： It comprises a preparation process of entecavir comprising: submitting a (1S, 3R)-3-(tert-butyldimethylsilyloxy)-1 -(oxiran-2-yl)pent-4-yn-1-ol (VIII) to a double esterification and to a radicalary cyclization, yielding a compound of formula (V), where either a compound of formula (VIII) is submitted to a first esterification reaction, then to a catalytic radicalary cyclization using titanocene dichloride as catalyst in the presence of Mn/2,4,6-collidine HCI or Zn/2,4,6-collidine/trimethylsilyl chloride, and finally to a second esterification reaction or, alternatively, the compound of formula (VIII) is submitted first to a catalytic radicalary cyclization, and then to an esterification reaction. Entecavir can be obtained by submitting compound (V) to a desilylation reaction to remove the TBS group and then to a Mitsunobu coupling with 2- amino-6-chloroguanine, followed by hydrolysis. It also relates to some new intermediates of the process.
摘要翻译：其包括恩替卡韦的制备方法，其包括：将（1S，3R）-3-（叔丁基二甲基甲硅烷氧基）-1-（环氧乙烷-2-基）戊-4-炔-1-醇（VIII）和式（Ⅴ）化合物反应，其中式（Ⅷ）化合物进行第一次酯化反应，然后在二氯甲烷二氯化物作催化剂存在下，在Mn / 2存在下进行催化自由基环化，4,6-可力丁HCl或Zn / 2,4,6-可力丁/三甲基甲硅烷基氯，最后进行第二次酯化反应，或者，将式（Ⅷ）化合物首先进行催化活性环化，然后进行酯化反应。恩替卡韦可以通过将化合物（V）提交到脱甲硅烷基化反应中以除去TBS基团，然后与2-氨基-6-氯鸟嘌呤进行Mitsunobu偶联，然后水解。它也涉及到一些新的中间体的过程。

2. 发明申请

WO2012013755A1 PROCESS FOR THE PREPARATION OF 1-ARYL-PYRAZOL-3-ONE INTERMEDIATES USEFUL IN THE SYNTHESIS OF SIGMA RECEPTORS INHIBITORS 审中-公开
标题翻译：制备1-ARYL-PYRAZOL-3-ONE中间体在合成SIGMA受体抑制剂中有用的方法
公开(公告)号：WO2012013755A1
公开(公告)日：2012-02-02
申请号：PCT/EP2011/063020
申请日：2011-07-28
申请人： ESTEVE QUÍMICA, S.A. , BARTRA SANMARTÍ, Martí , BERENGUER MAIMÓ, Ramon , MEDRANO RUPÉREZ, Jorge , GARCÍA GÓMEZ, Jorge , ARIZA PIQUER, Javier
发明人： BARTRA SANMARTÍ, Martí , BERENGUER MAIMÓ, Ramon , MEDRANO RUPÉREZ, Jorge , GARCÍA GÓMEZ, Jorge , ARIZA PIQUER, Javier
IPC分类号： C07C59/125 , C07C69/96 , C07D231/20 , C07D317/30
CPC分类号： C07D207/36 , C07D231/20 , C07D317/30
摘要： The invention relates to a process for preparing 1-aryl-pyrazol-3-one intermediates, tautomers, and salts thereof, to novel intermediates, and to the use of the intermediates in the preparation of sigma receptor inhibitors.
摘要翻译：本发明涉及一种制备1-芳基 - 吡唑-3-酮中间体，互变异构体及其盐，新中间体以及中间体在制备σ受体抑制剂中的用途的方法。

3. 发明申请

WO2009092716A1 CRYSTALLINE FORM OF ABACAVIR THAT IS ESSENTIALLY FREE OF SOLVENT 审中-公开
标题翻译： ABACAVIR的结晶形式基本不含溶剂
公开(公告)号：WO2009092716A1
公开(公告)日：2009-07-30
申请号：PCT/EP2009/050613
申请日：2009-01-21
申请人： ESTEVE QUÍMICA, S.A. , BARTRA SANMARTÍ, Martí , BERENGUER MAIMÓ, Ramón , BENET-BUCHHOLZ, Jordi , SOLÀ I CARANDELL, Lluís
发明人： BARTRA SANMARTÍ, Martí , BERENGUER MAIMÓ, Ramón , BENET-BUCHHOLZ, Jordi , SOLÀ I CARANDELL, Lluís
IPC分类号： C07D473/16 , A61K31/52 , A61P31/00
CPC分类号： C07D473/16
摘要： Crystalline form of abacavir that is essentially free of solvent of formula (I), in particular crystalline Form I, and its preparation process which comprises the following steps: a) crystallizing abacavir from a solution of said compound in a (C 1 -C 4 )-alcohol, dichloromethane, acetonitrile/water, or mixtures thereof; b) isolating the crystalline form of abacavir that appears in the prior step; and c) removing the solvent from the crystalline form of abacavir thus obtained. Crystalline Form I can also be obtained by dispersion of abacavir in acetonitrile. The crystalline form of abacavir that is essentially free of solvent is useful for the preparation of pharmaceutical compositions for use in the treatment and/or prophylaxis of HIV infections.
摘要翻译：结晶形式的阿巴卡韦，基本上不含式（I）的溶剂，特别是结晶形式I及其制备方法，其包括以下步骤：a）将所述化合物在（C1-C4） - 醇，二氯甲烷，乙腈/水或其混合物; b）分离出现在先前步骤中的阿巴卡韦的结晶形式; 和c）从由此获得的阿巴卡韦的结晶形式除去溶剂。结晶形式I也可以通过将阿巴卡韦分散在乙腈中获得。基本上不含溶剂的阿巴卡韦的结晶形式可用于制备用于治疗和/或预防HIV感染的药物组合物。

4. 发明申请

WO2011098553A1 PREPARATION PROCESS OF THE SODIUM SALT OF ESOMEPRAZOLE 审中-公开
标题翻译：异辛醚钠盐的制备方法
公开(公告)号：WO2011098553A1
公开(公告)日：2011-08-18
申请号：PCT/EP2011/052026
申请日：2011-02-11
申请人： ESTEVE QUÍMICA, S.A. , BARTRA SANMARTÍ, Martí , BERENGUER MAIMÓ, Ramón , SOLSONA ROCABERT, Joan Gabriel
发明人： BARTRA SANMARTÍ, Martí , BERENGUER MAIMÓ, Ramón , SOLSONA ROCABERT, Joan Gabriel
IPC分类号： C07D401/12 , A61K31/4439
CPC分类号： C07D401/12
摘要： Preparation process of the sodium salt of a 2-(2-pyridylmethylsulfinyl)- benzimidazole derivative compound It comprises a preparation process of esomeprazole sodium substantially free of sulfone impurity comprising the steps of: a) combining either esomeprazole with a (C 3 -C 8 )-ketone or a mixture thereof, a sodium alkoxide, and a (C 1 -C 5 )-alcohol, or esomeprazole sodium with a (C 3 -C 8 )-ketone or a mixture thereof and a (C 1 -C 5 )-alcohol; and b) recovering the esomeprazole sodium formed from the reaction media by filtration.
摘要翻译： 2-（2-吡啶基甲基亚磺酰基） - 苯并咪唑衍生物化合物的钠盐的制备方法其包括基本上不含砜杂质的艾美拉唑钠的制备方法，包括以下步骤：a）将埃索美拉唑与（C3-C8） - 酮或其混合物，醇钠和（C1-C5） - 醇或与（C3-C8） - 酮或其混合物和（C1-C5） - 醇的艾美拉唑钠; 和b）通过过滤回收由反应介质形成的埃索美拉唑钠。

5. 发明申请

WO2010146119A1 PREPARATION PROCESS OF AN ANTIVIRALLY HETEROCYCLIC AZAHEXANE DERIVATIVE 审中-公开
标题翻译：抗病毒性偶氮染料衍生物的制备方法
公开(公告)号：WO2010146119A1
公开(公告)日：2010-12-23
申请号：PCT/EP2010/058545
申请日：2010-06-17
申请人： ESTEVE QUÍMICA, S.A. , BARTRA SANMARTÍ, Martí , BERENGUER MAIMÓ, Ramón , ORTIZ GIL, Jordi , ISERN SÁNCHEZ, Olga
发明人： BARTRA SANMARTÍ, Martí , BERENGUER MAIMÓ, Ramón , ORTIZ GIL, Jordi , ISERN SÁNCHEZ, Olga
IPC分类号： C07D213/42
CPC分类号： C07D213/42
摘要： A process for the preparation of atazanavir or its pharmaceutically salts, or its solvates, which comprises condensing N-(methoxycarbonyl)-L-tert-leucine and 1-[4-(piridyn-2-yl)phenyl-4(S)-hydroxy]-5-(S)-2,5-diamino-6-phenyl-2-azahexane or a salt thereof using N,N-diisopropylcarbodiimide or N,N-dicyclohexylcarbodiimide and a tertiary organic amine, being the condensation carried out in the absence of 1-hydroxy-benzotriazole.
摘要翻译：一种制备阿扎那韦或其药用盐或其溶剂合物的方法，其包括将N-（甲氧基羰基）-L-叔亮氨酸和1- [4-（吡啶-2-基）苯基-4（S） - 羟基] -5-（S）-2,5-二氨基-6-苯基-2-氮杂己烷或其盐使用N，N-二异丙基碳二亚胺或N，N-二环己基碳二亚胺和叔有机胺，其是在不存在1-羟基 - 苯并三唑。

6. 发明申请

WO2010097420A1 PROCESS FOR THE PREPARATION OF A CHIRAL BETA AMINOACID DERIVATIVE AND INTERMEDIATES THEREOF 审中-公开
标题翻译：制备丙氨酸氨基酸衍生物及其中间体的方法
公开(公告)号：WO2010097420A1
公开(公告)日：2010-09-02
申请号：PCT/EP2010/052359
申请日：2010-02-24
申请人： ESTEVE QUÍMICA, S.A. , BARTRA SANMARTÍ, Martí , RUSTULLET OLIVER, Albert , FERNÁNDEZ HERNÁNDEZ, Sara , MONSALVATJE LLAGOSTERA, Montserrat
发明人： BARTRA SANMARTÍ, Martí , RUSTULLET OLIVER, Albert , FERNÁNDEZ HERNÁNDEZ, Sara , MONSALVATJE LLAGOSTERA, Montserrat
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , Y02P20/55
摘要： It comprises a process for the preparation of sitagliptin, or its pharmaceutically acceptable salts, or its solvates, including hydrates, comprising: a) coupling an halo-2,4,5-trifluorobenzene with a compound of formula (IV) to give N-protected sitagliptin; the coupling being carried out via the formation of an organocupric compound of the halo-2,4,5-trifluorobenzene or, alternatively, via the formation of a organozinc compound of a compound of formula (IV); where R 1 is hydrogen or an amino protective group; R 2 is an amino protective group; or alternatively R 1 and R 2 taken together form a phtalimido group; X is Br or I; and Y is Br, I or R 3 SO 3 - wherein R 3 is (C 1 -C 4 )- alkyl, phenyl, or phenyl mono- or disubstituted by a (C 1 -C 4 )-alkyl radical; b) submitting the N-protected sitagliptin to a deprotection reaction; and c) optionally its conversion into a pharmaceutically acceptable salt. It also comprises new intermediate compounds useful in such preparation process.
摘要翻译：其包括制备西格列汀或其药学上可接受的盐或其溶剂化物，包括水合物的方法，包括：a）将卤代-2,4,5-三氟苯与式（IV）的化合物偶联，得到N- 保护西他列汀; 通过形成卤代-2,4,5-三氟苯的有机配位化合物或者通过形成式（IV）化合物的有机锌化合物来进行偶合。其中R1是氢或氨基保护基; R2是氨基保护基; 或者R1和R2一起形成邻苯二甲酰亚胺基; X是Br或I; 并且Y是Br，I或R3SO3-，其中R3是（C1-C4） - 烷基，苯基或被（C1-C4） - 烷基单或二取代的苯基; b）将N-保护的西他列汀提交至去保护反应; 和c）任选地将其转化成药学上可接受的盐。它还包括在这种制备过程中有用的新的中间体化合物。

7. 发明申请

WO2011076813A1 PREPARATION PROCESS OF ERLOTINIB 审中-公开
标题翻译： ERLOTINIB的制备方法
公开(公告)号：WO2011076813A1
公开(公告)日：2011-06-30
申请号：PCT/EP2010/070424
申请日：2010-12-21
申请人： ESTEVE QUÍMICA, S.A. , BARTRA SANMARTÍ, Martí , LUPON ROSES, María del Pilar , COMELY, Alexander, Christian , GEORGES, Yohan, Philippe
发明人： BARTRA SANMARTÍ, Martí , LUPON ROSES, María del Pilar , COMELY, Alexander, Christian , GEORGES, Yohan, Philippe
IPC分类号： C07D239/94
CPC分类号： C07D239/94
摘要： Preparation process of erlotinib or its salts comprising: reacting 6,7-bis(2-methoxyethoxy)-4-methoxyquinazoline with 3-ethynylaniline or a salt thereof in the presence of a base and a reaction-inert solvent, and optionally, treating the compound obtained with a pharmaceutically acceptable acid to form the corresponding pharmaceutically acceptable salt. The compound 6,7-bis(2-methoxyethoxy)-4-methoxyquinazoline can be prepared either from 4-methoxyquinazoline-6,7-diol or 6,7-bis(2-methoxyethoxy)quinazolinone. The compounds 6,7-bis(2-methoxyethoxy)-4-methoxyquinazoline and 4-methoxyquinazoline-6,7-diol are new intermediates useful for the preparation of erlotinib or its salts.
摘要翻译：厄洛替尼或其盐的制备方法包括：在碱和反应惰性溶剂的存在下使6,7-双（2-甲氧基乙氧基）-4-甲氧基喹唑啉与3-乙炔基苯胺或其盐反应，任选地，用药学上可接受的酸获得的化合物形成相应的药学上可接受的盐。化合物6,7-双（2-甲氧基乙氧基）-4-甲氧基喹唑啉可以由4-甲氧基喹唑啉-6,7-二醇或6,7-双（2-甲氧基乙氧基）喹唑啉酮制备。化合物6,7-双（2-甲氧基乙氧基）-4-甲氧基喹唑啉和4-甲氧基喹唑啉-6,7-二醇是可用于制备厄洛替尼或其盐的新中间体。

8. 发明申请

WO2008119793A1 PROCESS FOR THE PREPARATION OF ENTACAPONE AND INTERMEDIATES THEREOF 审中-公开
标题翻译：制备ENTACAPONE及其中间体的方法
公开(公告)号：WO2008119793A1
公开(公告)日：2008-10-09
申请号：PCT/EP2008/053843
申请日：2008-03-31
申请人： ESTEVE QUÍMICA, S.A. , BARTRA SANMARTÍ, Martí , SOLSONA ROCABERT, Joan Gabriel , PALOMO NICOLAU, Francisco Eugenio , MOLINA PONCE, Andrés
发明人： BARTRA SANMARTÍ, Martí , SOLSONA ROCABERT, Joan Gabriel , PALOMO NICOLAU, Francisco Eugenio , MOLINA PONCE, Andrés
IPC分类号： C07C255/51 , C07C253/30
CPC分类号： C07C255/41 , C07C253/30
摘要： New preparation process for the preparation of entacapone which comprises converting the 3,4-dimethoxy-5-nitrobenzoic acid into an activated derivative which is reacted with 2-cyano-N,N-diethylacetamide in the presence of a base to give 2-cyano-3-(3,4-dimethoxy-5-nitrophenyl)- N,N -diethyl-3- hydroxyacrylamide; reacting the resulting compound with MHB(OCOR) 3 where R is (C 1 -C 4 )-alkyl, phenyl, or CF 3 ; and M is a sodium, potassium or ((C 1 -C 4 )-alkyl) 4 N, in the presence of an appropriate solvent to give E-2 -cyano- 3-3,4-dimethoxy-5-nitrophenyl)- N,N -diethylacrylamide; and finally submitting the compound obtained to a demethylation reaction to yield entacapone. Both 2-cyano-3-(3,4-dimethoxy-5-nitrophenyl)- N,N -diethyl-3-hydroxyacrylamide and E-2 -cyano-3-3,4-dimethoxy-5-nitrophenyl)- N,N -diethylacrylamide are new. Entacapone has industrial applicability as antiparkinson's agent.
摘要翻译：用于制备恩他卡朋的新制备方法，其包括将3,4-二甲氧基-5-硝基苯甲酸转化成活化的衍生物，其在碱的存在下与2-氰基-N，N-二乙基乙酰胺反应，得到2-氰基 -3-（3,4-二甲氧基-5-硝基苯基）-N，N-二乙基-3-羟基丙烯酰胺; 使所得化合物与MHB（OCOR）3，其中R是（C 1 -C 4 -C 4 - ） - 烷基，苯基或CF _{3 ; 并且M是在适当的溶剂存在下的钠，钾或（（C 1 -C 4 -C 4 - ）烷基）N 4 N 得到E-2-氰基-3-3,4-二甲氧基-5-硝基苯基）-N，N-二乙基丙烯酰胺; 最后将得到的化合物进行去甲基化反应，得到恩他卡朋。 2-氰基-3-（3,4-二甲氧基-5-硝基苯基）-N，N-二乙基-3-羟基丙烯酰胺和E-2-氰基-3-3,4-二甲氧基-5-硝基苯基）-N， N-二乙基丙烯酰胺是新的。恩他卡朋具有工业适用性，作为抗帕金森氏剂。}

9. 发明申请

WO2007051828A2 PROCESS FOR THE PREPARATION OF A LEUKOTRIENE ANTAGONIST AND INTERMEDIATES THEREOF 审中-公开
标题翻译：制备白藜芦醇拮抗剂及其中间体的方法
公开(公告)号：WO2007051828A2
公开(公告)日：2007-05-10
申请号：PCT/EP2006/068052
申请日：2006-11-03
申请人： ESTEVE QUÍMICA, S. A. , COPPI, Laura , BARTRA SANMARTÍ, Martí , GASANZ GUILLÉN, Yolanda , MONSALVATJE LLAGOSTERA, Montserrat , TALAVERA ESCASANY, Pedro
发明人： COPPI, Laura , BARTRA SANMARTÍ, Martí , GASANZ GUILLÉN, Yolanda , MONSALVATJE LLAGOSTERA, Montserrat , TALAVERA ESCASANY, Pedro
CPC分类号： C07D215/18
摘要： It comprises a preparation process of Montelukast from a new intermediate compound of formula (VI), which is previously prepared by reaction of the corresponding sulfonate with 1-(mercaptomethyl)cyclopropyl)methanol. Compound (VI) is reacted with a Grignard reactant to convert the ester group into a tertiary alcohol, followed by conversion of the primary alcohol into a sulfonate, substitution of the sulfonate group by a cyano group, and finally transforming the cyano compound to the carboxilic acid compound by a hydrolysis reaction to afford Montelukast. Montelukast can also be prepared by a hydrolysis reaction of the corresponding amide. It also comprises new intermediate compounds useful in such preparation process.
摘要翻译：它包括由新的式（VI）中间体化合物的Montelukast的制备方法，其通过相应的磺酸酯与1-（巯基甲基）环丙基）甲醇的反应预先制备。使化合物（VI）与格氏反应物反应，将酯基转化成叔醇，然后将伯醇转化成磺酸盐，用磺酰基取代氰基，最后将氰基化合物转化为羧酸酸化合物通过水解反应得到蒙特鲁卡斯特。孟鲁司特也可以通过相应酰胺的水解反应制备。它还包括在这种制备过程中有用的新的中间体化合物。

10. 发明申请

WO2014177517A1 PREPARATION PROCESS OF AN AGONIST OF THE THROMBOPOIETIN RECEPTOR 审中-公开
标题翻译：血小板生成素受体激动剂的制备方法
公开(公告)号：WO2014177517A1
公开(公告)日：2014-11-06
申请号：PCT/EP2014/058610
申请日：2014-04-28
申请人： ESTEVE QUÍMICA, S.A. , GALCHIMIA, S.A.
发明人： BARTRA SANMARTÍ, Martí , SOLSONA ROCABERT, Joan Gabriel , CRUCES COLADO, Jacobo , ENJO BABIO, Juan , PAMPÍN CASAL, María Begoña
IPC分类号： C07C205/59 , C07C201/12 , C07D231/22 , C07C227/04 , C07C249/16
CPC分类号： C07C201/12 , C07C205/59 , C07C227/04 , C07C249/16 , C07D231/22 , C07C229/70 , C07C251/76
摘要： It relates to a preparation process of 2'-(benzyloxy)-3'-nitro-1,1'-biphenyl-3- carboxylic acid or a salt thereof comprising reacting 2-(benzyloxy)-1-bromo- 3-nitrobenzene with a either 3-carboxyphenylboronic acid or a salt thereof or a (C 1 -C 4 )-alkyl ester thereof in the presence of Pd(OAc) 2 , tricydohexylphosphine, a base, an appropriate solvent, and at an appropriate temperature; if appropriate, submitting the compound thus obtained to a hydrolysis reaction; and isolating the compound thus obtained in form of a salt of compound of formula (VI) or in form of the free acid by adding an acid. It also comprises the further preparation to eltrombopag or its salts from the new intermediate thus obtained by subsequent reduction of the nitro group and deprotection of the phenol, conversion of the amine intermediate obtained in a diazonium derivative, and either (1) subsequent reaction with ethyl acetoacetate and with (3,4-dimethylphenyl)hydrazine or a salt thereof, occurring the pyrazole ring formation by intermolecular cyclization, or (2) introduction of the pyrazole ring by reaction with 1-(3,4-dimethylphenyl)-3-methyl-3-pyrazolin-5-one.
摘要翻译：本发明涉及2' - （苄氧基）-3'-硝基-1,1'-联苯-3-甲酸或其盐的制备方法，其包括使2-（苄氧基）-1-溴-3-硝基苯与在Pd（OAc）2，三羟基己基膦，碱，适当的溶剂和适当的温度存在下，3-羧基苯基硼酸或其盐或其（C 1 -C 4） - 烷基酯; 如果合适，将由此获得的化合物提交至水解反应; 并通过添加酸分离由式（VI）化合物的盐形成的化合物或游离酸形式的化合物。它还包括通过随后还原硝基和脱保护苯酚得到的新中间体进一步制备埃曲波帕或其盐，以及在重氮衍生物中获得的胺中间体的转化，以及（1）随后的反应与乙基乙酰乙酸酯和（3,4-二甲基苯基）肼或其盐，通过分子间环化形成吡唑环，或（2）通过与1-（3,4-二甲基苯基）-3-甲基 -3-吡唑啉-5-酮。

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