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1. 发明申请

WO2005121084A1 A METHOD OF PREPARATION OF RAMIPRIL 审中-公开
标题翻译：一种制备RAMIPRIL的方法
公开(公告)号：WO2005121084A1
公开(公告)日：2005-12-22
申请号：PCT/CZ2005/000048
申请日：2005-06-08
申请人： ZENTIVA, a. s. , STEPANKOVA, Hana , PIHERA, Pavel , HAJICEK, Josef
发明人： STEPANKOVA, Hana , PIHERA, Pavel , HAJICEK, Josef
IPC分类号： C07D209/52
CPC分类号： C07D209/52
摘要： A method of preparation of ramipril of formula (I), during which the benzyl ester hydrochloride of formula (III) is converted to the benzyl ester of formula (II), which in turn affords, by reaction with the carboxyanhydride of formula (V), the benzyl ester of ramipril of formula (IV), which is subsequently converted to ramipril of formula (I).
摘要翻译：制备式（I）的雷米普利的方法，其中式（III）的苄酯盐酸盐转化成式（II）的苄基酯，其又通过与式（V）的羧酸酐反应，，式（IV）的雷米普里的苄基酯，其随后转化成式（I）的雷米普利。

2. 发明申请

WO2005068471A1 NEW CRYSTALLINE FORMS OF CLOPIDOGREL HYDROBROMIDE AND METHODS OF THEIR PREPARATION 审中-公开
标题翻译：氯碳酸氢盐的新型结晶形式及其制备方法
公开(公告)号：WO2005068471A1
公开(公告)日：2005-07-28
申请号：PCT/CZ2004/000089
申请日：2004-12-21
申请人： ZENTIVA, A.S. , HAJICEK, Josef , PIHERA, Pavel , STEPANKOVA, Hana
发明人： HAJICEK, Josef , PIHERA, Pavel , STEPANKOVA, Hana
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The invention concerns clopidogrel hydrobromide in the crystalline Form I characterized by an X-ray diffraction pattern with characteristic interplanar distances d of 4.01; 4.39 and 3.17 ú and which is further characterized by bands in the infrared spectra at 1743; 1421; 1237, 760 and 728 cm -1 . Clopidogrel hydrobromide in the crystalline Form II is characterized by an Xray diffraction pattern with characteristic interplanar distances d of 4.52; 3.83; 3.48 ú, as well as bands in the infrared spectra at 1754; 1436; 1317 and 1223 cm -1 . Crystalline form III is characterized by the following peaks ascertained by X-ray diffraction at 20 positions: 7.796 °; 15.380 °; 18.389 °; 19.369 ° and 23.895 °. The method of preparation of clopidogrel hydrobromide in the crystalline Form I consist in precipitating the clopidogrel base dissolved in toluene with a concentrated solution of hydrobromic acid. The method of preparation of clopidogrel hydrobromide in the crystalline Form II consist in dissolving the clopidogrel base in an organic solvent and precipitating it with a solution of hydrobromic acid in toluene or with gaseous hydrogen bromide. Form III can be used for the preparation of pharmaceutically applicable Form II.
摘要翻译：本发明涉及结晶形式I中的氯吡格雷氢溴酸盐，其特征在于具有4.01的特征性面间距离d的X射线衍射图谱; 4.39和3.17ú，其进一步特征在于1743年红外光谱中的谱带; 1421; 结晶形式II中的氯吡格雷氢溴酸盐的特征在于具有4.52的特征性面间距d的X射线衍射图; 3.83; 3.48ú，以及1754年的红外光谱带; 1436; 1317和1223厘米-1。结晶形式III的特征在于在20个位置通过X射线衍射确定的以下峰：7.796°; 15.380°; 18.389°; 19.369°和23.895°。结晶形式I中氯吡格雷氢溴酸盐的制备方法是用氢溴酸浓溶液沉淀溶解在甲苯中的氯吡格雷碱。在晶型II中制备氯吡格雷氢溴酸盐的方法包括将氯吡格雷碱溶解在有机溶剂中，并用氢溴酸在甲苯或与溴化氢气体的溶液中沉淀。 III型可用于制备药学上适用的II型。

3. 发明申请

WO2012062229A1 A METHOD OF MANUFACTURING (-)-L-(3-HYDROXYPROPYL)-5-[(2R)-2-({2,2,2-TRIFLUOROETHOXY)- PHENOXYETHYL}AMINO)PROPYL]-2,3-DIHYDRO-LH-INDOLE-7-CARBOXAMIDE 审中-公开
标题翻译：制备（ - ） - L-（3-羟基丙基）-5 - [（2R）-2 - （{2,2,2-三氟甲基） - 苯氧基]氨基]丙基] -2,3-二氢-2H- - 吲哚-7-甲酰胺
公开(公告)号：WO2012062229A1
公开(公告)日：2012-05-18
申请号：PCT/CZ2011/000106
申请日：2011-11-07
申请人： ZENTIVA, K.S. , VLASAKOVA, Ruzena , HAJICEK, Josef , SLAVIKOVA, Marketa
发明人： VLASAKOVA, Ruzena , HAJICEK, Josef , SLAVIKOVA, Marketa
IPC分类号： C07D209/08
CPC分类号： C07D209/08
摘要： A method of manufacturing optically pure or optically enriched silodosin of formula I and of its pharmaceutically acceptable salts, in which a secondary amine of general formula II, wherein Bn denotes a phenylmethyl group, substituted or unsubstituted in the benzene ring, e.g. benzyl or 4-methoxybenzyl, or the benzhydryl or trityl group, (a) is N -alkylated with an alkylating agent of general formula III, wherein X denotes a good leaving group, such as a halogen or an alkane sulfonyloxyl group RS0 2 0 or an arene SLilfonyloxyl group ArS0 2 0, R means an alkyl group with 1 to 4 carbon atoms and Ar is a substituted or unsubstituted phenyl group; (b) the obtained tertiary amine of general formula IV, wherein Bn is as defined above, is hydrogenolyzed with hydrogen on a metal catalyst; (c) and the resulting nitrile of formula V, wherein Bn is as defined above, is hydrolyzed by treatment with alkaline agents; and optionally, (d) additional O -debenzylation of the amide-ether of general formula VI, wherein Bn is as defined above, with dealkylating agents is carried out; and, if desired, the obtained silodosin is transformed to the respective salts by treatment with pharmaceutically acceptable acids.
摘要翻译：制备式I的光学纯的或光学富集的西洛多辛及其药学上可接受的盐的方法，其中通式II的仲胺，其中Bn表示苯基中的苯甲基，在苯环中被取代或未取代。苄基或4-甲氧基苄基，或二苯甲基或三苯甲基，（a）与通式III的烷基化剂N-烷基化，其中X表示良好的离去基团，例如卤素或烷烃磺酰氧基基团RS020或芳烃二苯甲酰氧基ArS020，R表示碳原子数为1〜4的烷基，Ar为取代或未取代的苯基; （b）得到的通式Ⅳ的叔胺，其中Bn如上定义，用氢在金属催化剂上氢解; （c）和其中Bn如上定义的所得到的式V的腈通过用碱剂处理而水解; 并且任选地，（d）进行其中Bn如上定义的通式VI的酰胺 - 醚与脱烷基化剂的额外的O-脱苄基化; 并且如果需要，通过用药学上可接受的酸处理将获得的西洛多辛转化成各自的盐。

4. 发明申请

WO2011120475A1 A METHOD OF MANUFACTURING (S)-5-METHOXY-2-[[(4-METHOXY-3,5-DIMETHYL-2- PYRIMIDINYL)METHYL]SULFINYL]-1H-BENZIMIDAZOLE USING A CHIRAL COMPLEX WITH MANDELIC ACID 审中-公开
标题翻译：制备（S）-5-甲氧基-2 - [[（4-甲氧基-3,5-二甲基-2-吡啶基）甲基]硫代] -1H-苯并咪唑的方法，其使用具有仲胺酸的主要复合物
公开(公告)号：WO2011120475A1
公开(公告)日：2011-10-06
申请号：PCT/CZ2010/000031
申请日：2010-03-17
申请人： ZENTIVA, K.S. , STEPANKOVA, Hana , ZEZULA, Josef , HAJICEK, Josef , KRAL, Vladimir
发明人： STEPANKOVA, Hana , ZEZULA, Josef , HAJICEK, Josef , KRAL, Vladimir
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： The invention deals with a new manufacturing method of ( S )-5-methoxy-2-[[(4-methoxy- 3,5-dimethyl-2-pyridinyl)methyl]sulphinyl]-1 H -benzimidazole of formula (I) and its salts of general formula (II), wherein the sulfide of general formula (III) is oxidized by hydroperoxides on a catalyst consisting of a chiral metallic complex containing ligands constituted by chiral functional derivatives of mandelic acid.
摘要翻译：本发明涉及式（I）的（S）-5-甲氧基-2 - [[（4-甲氧基-3,5-二甲基-2-吡啶基）甲基]亚磺酰基] -1H-苯并咪唑的新制备方法和其通式（II）的盐，其中通式（III）的硫化物被氢过氧化物氧化在由含有由扁桃酸的手性功能衍生物构成的配体的手性金属络合物组成的催化剂上。

5. 发明申请

WO2011069473A1 A METHOD FOR THE PREPARATION OF PRASUGREL HYDROCHLORIDE IN POLYMORPHOUS FORM B 审中-公开
标题翻译：在多形态B中制备前体氢氯化物的方法
公开(公告)号：WO2011069473A1
公开(公告)日：2011-06-16
申请号：PCT/CZ2010/000126
申请日：2010-12-09
申请人： ZENTIVA, K.S. , STEPANKOVA, Hana , KAMINSKA, Katerina , HAJICEK, Josef
发明人： STEPANKOVA, Hana , KAMINSKA, Katerina , HAJICEK, Josef
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The invention relates to a method for the manufacture of 5-[2-cyclopropyl-l-(2- fluorophenyl)-2-oxoethyl]-4,5,6,7-tetrahydrothieno[3,2-c]pyridin-2-yl acetate hydrochloride of formula I (prasugrel hydrochloride) in crystalline form B, wherein prasugrel base of formula II is dissolved or suspended in an organic solvent and reacted with hydrogen chloride dissolved in an organic solvent or in water at a temperature in the range of -20 °C to 75°C and crystallized, optionally after addition of a co-solvent.
摘要翻译：本发明涉及制备5- [2-环丙基-1-（2-氟苯基）-2-氧代乙基] -4,5,6,7-四氢噻吩并[3,2-c] 乙酸盐酸盐（结晶形式B的盐酸普拉格雷），其中式Ⅱ的普拉格雷碱溶解或悬浮在有机溶剂中，并与溶解在有机溶剂中或在水中的氯化氢反应，其温度范围为 - 20℃至75℃，任选地在加入共溶剂后结晶。

6. 发明申请

WO2006094468A1 METHOD OF RACEMIZATION OF THE R(-) ISOMER OF THE (2-CHLOROPHENYL)-6,7- DIHYDROTHIENO[3,2-c]PYRIDINE-5(4H)-ACETIC ACID METHYL ESTER 审中-公开
标题翻译：（2-氯苯基）-6,7-二氢苯并[3,2-c]吡啶-5（4H） - 甲酸甲酯的R（ - ）异构体的研究方法
公开(公告)号：WO2006094468A1
公开(公告)日：2006-09-14
申请号：PCT/CZ2006/000010
申请日：2006-03-03
申请人： ZENTIVA, A.S. , HAJICEK, Josef , STEPANKOVA, Hana , KALIDOVA, Jan
发明人： HAJICEK, Josef , STEPANKOVA, Hana , KALIDOVA, Jan
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： Racemization of the R(-) isomer of the (2-chlorophenyl) -6, 7-dihydrothieno [3, 2-c]pyridine- 5 (4H) -acetic acid methyl ester (Formula II) (also called R clopidogrel) is performed via conversion of a portion thereof to the S (+) isomer and it takes place in an organic solvent selected from alcohols , esters, ketones or ethers, or in their mixtures, in the presence of a base selected from substances of formula R1R2R3R4N+OH" wherein R1, R2, R3 and R4 are identical or different substituents selected from C1-C5 alkyls or C5, C6 cycloalkyls or aryls, C7-C9 alkyl-cycloalkyls or alkyl-aryls, the molar ratio of the base to the starting substance being 1: 1 to 1: 10. ,OMe Cl I Cl
摘要翻译：（2-氯苯基）-6,7-二氢噻吩并[3,2-c]吡啶-5（4H） - 乙酸甲酯（式II）（也称为氯吡格雷）的R（ - ）异构体的外消旋化为通过将其一部分转化成S（+）异构体而进行，并且其在选自醇，酯，酮或醚的有机溶剂或其混合物中，在选自式R 1 R 2 R 3 R 4 N + OH“，其中R 1，R 2，R 3和R 4是相同或不同的选自C 1 -C 5烷基或C 5，C 6环烷基或芳基的取代基，C 7 -C 9烷基 - 环烷基或烷基 - 芳基，碱与起始物质的摩尔比为1：1至1：10，OMe Cl I Cl

7. 发明申请

WO2012089180A1 FORM C OF PRASUGREL HYDROBROMIDE AND A METHOD FOR ITS PRODUCTION 审中-公开
标题翻译：前体氢溴酸盐的形式及其生产方法
公开(公告)号：WO2012089180A1
公开(公告)日：2012-07-05
申请号：PCT/CZ2011/000127
申请日：2011-12-29
申请人： ZENTIVA, K.S. , KAMINSKA, Katerina , STEPANKOVA, Hana , HAJICEK, Josef
发明人： KAMINSKA, Katerina , STEPANKOVA, Hana , HAJICEK, Josef
IPC分类号： C07D495/04 , A61K31/4365 , A61P7/00
CPC分类号： C07D495/04
摘要： A polymorphous form of the hydrobromide of prasugrel, a well-known substance reducing blood coagulation, prasugrel of formula (I), which is characterized by high chemical stability, and a method for its production. (Formula (I))
摘要翻译：普拉格雷氢溴酸盐的多晶形式，一种众所周知的减少血液凝结的物质，具有高化学稳定性的式（I）的普拉格雷及其生产方法。（式（I））

8. 发明申请

WO2012089177A1 METHOD OF PRODUCING (2R,3R)-NA-DIMETHYL-3-(3-HYDROXYPHENYI)-2-METHYLPENTYLAMINE (TAPENTADOL) 审中-公开
标题翻译：（2R，3R）-N-二甲基-3-（3-羟基苯基）-2-甲基戊胺（TAPENTADOL）的制备方法
公开(公告)号：WO2012089177A1
公开(公告)日：2012-07-05
申请号：PCT/CZ2011/000122
申请日：2011-12-23
申请人： ZENTIVA, K.S. , VLASAKOVA, Ruzena , HAJICEK, Josef
发明人： VLASAKOVA, Ruzena , HAJICEK, Josef
IPC分类号： C07C213/02 , C07C213/08 , C07C217/62 , C07C231/02 , C07C235/34 , C07C51/60
CPC分类号： C07C213/08 , C07B2200/07 , C07C213/02 , C07C217/62 , C07C231/02 , C07C235/34 , C07C215/54
摘要： The present solution relates to a method comprising, as a key step, production of optically pure or optically enriched tapentadol of formula I, in which optically pure or optically enriched (2 R ,3 R )-amines of general formula V, wherein R stands for a phenylmethyl group, substituted or non-substituted in the benzene ring, e.g. benzyl or 4-methoxybenzyl, benzhydryl or trityl group, are hydrogenated on a metal catalyst and, if desired, the obtained tapentadol is converted by the action of pharmaceutically acceptable acids to respective salts, such as to hydrochloride.
摘要翻译：本解决方案涉及一种方法，其包括作为关键步骤的制备光学纯的或光学富集的式I的他喷他多，其中通式V的光学纯的或光学富集的（2R，3R） - 胺，其中R代表苯甲基，在苯环中被取代或未取代，例如苄基或4-甲氧基苄基，二苯甲基或三苯甲基，在金属催化剂上氢化，如果需要，通过药学上可接受的酸的作用将得到的他喷他多酮转化为各种盐，例如盐酸盐。

9. 发明申请

WO2011057593A3 SALTS OF PRASUGREL AND A METHOD OF THEIR PRODUCTION 审中-公开
标题翻译： PRASUGREL的销售及其生产方法
公开(公告)号：WO2011057593A3
公开(公告)日：2011-07-07
申请号：PCT/CZ2010000116
申请日：2010-11-12
申请人： ZENTIVA K S , STEPANKOVA HANA , KAMINSKA KATERINA , HAJICEK JOSEF , BRUSOVA HANA
发明人： STEPANKOVA HANA , KAMINSKA KATERINA , HAJICEK JOSEF , BRUSOVA HANA
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The invention relates to new pharmaceutically acceptable salts of the well-known substance reducing coagulation of blood, prasugrel of formula (I), which are characterized by high chemical stability, and a method of their production. The prasugrel salts are prepared from prasugrel of formula (I) in the base form by reaction with an inorganic or organic acid in a suitable solvent or in mixtures of solvents. The inorganic acid means hydrobromic acid, hydrogen bromide, hydroiodic and sulphuric acid and the organic acid means cyclamic, ethane sulfonic, benzene sulfonic and 2-naphthalene sulfonic acid.
摘要翻译：本发明涉及众所周知的减少血液凝血的药学上可接受的盐，具有高化学稳定性的式（I）的普拉格雷及其制备方法。普拉格雷盐通过与无机或有机酸在合适的溶剂或溶剂的混合物中反应而以碱形式由式（I）的普拉格雷制备。无机酸是指氢溴酸，溴化氢，氢碘酸和硫酸，有机酸表示环己烷氨基磺酸，苯磺酸和2-萘磺酸。

10. 发明申请

WO2009067960A2 A METHOD OF MANUFACTURING (3R,4S)-L-(4-FLUOROPHENYL)-3-[(3S)-3-(4-FLUOROPHENYL)-3- HYDROXYPROPYL)]-4-(4-HYDROXYPHENYL)-2-AZETIDINONE AND ITS INTERMEDIATES 审中-公开
标题翻译：制备（3R，4S）-L-（4-氟代苯基）-3 - [（3S）-3-（4-氟苯基）-3-羟基丙基）] -4-（4-羟基苯基）-2-氮杂环丁酮的方法及其中介
公开(公告)号：WO2009067960A2
公开(公告)日：2009-06-04
申请号：PCT/CZ2008/000136
申请日：2008-11-05
申请人： ZENTIVA, A.S. , STEPANKOVA, Hana , HAJICEK, Josef , SLAVIKOVA, Marketa , ZEZULA, Josef
发明人： STEPANKOVA, Hana , HAJICEK, Josef , SLAVIKOVA, Marketa , ZEZULA, Josef
IPC分类号： C07C251/24 , C07D205/08 , C07D407/06 , C07D413/06
CPC分类号： C07C251/24 , C07D205/08 , C07D405/06 , C07D413/06 , Y02P20/55
摘要： A method of manufacturing (3 R ,4 S )-l-(4-fluorophenyl)-3-[(3 S )-3-(4-fluorophenyl)-3- hydroxypropyl)]-4-(4-hydroxyphenyl)-2-azetidinone (ezetimibe) of formula I, in which a protected ketone of general formula II, wherein R stands for a protective group, such as benzyloxycarbonyl, tert -butoxycarbonyl, benzhydryl or trityl, is reduced with asymmetrical borane agents in an inert organic solvent in the temperature range of -30 to +40 °C, and finally the obtained protected alcohol of general formula III, wherein R has the same meaning as above, is deprotected by the action of hydro genolytic or acidic agents in an inert organic solvent.
摘要翻译：制备（3R，4S）-1-（4-氟苯基）-3 - [（3S）-3-（4-氟苯基）-3-羟丙基）] - 4-（4-羟基苯基）-2-氮杂环丁酮（ezetimibe）其中R代表保护基团的通式II的受保护酮如苄氧羰基，叔丁氧基羰基，二苯甲基或三苯甲基，在不饱和硼烷试剂中在惰性有机溶剂中还原 -30℃〜+ 40℃的温度范围内，最后得到的通式III的保护醇，其中R具有与上述相同的含义，在惰性有机溶剂中由氢解酸或酸性剂的作用脱保护。

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