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1. 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。

2. 发明申请

WO2010091652A1 A METHOD FOR THE MANUFACTURE OF (S) -5-METHOXY-2- [ [ (4-METHOXY-3, 5-DIMETHYL-2-PYRIMIDINYL) METHYL] SULFINYL] -IH-BENZ IMIDAZOLE USING A CHIRAL COMPLEX WITH LACTIC ACID 审中-公开
标题翻译：（S）-5-甲氧基-2 - [[（4-甲氧基-3,5-二甲基-2-吡啶基）甲基]硫代] -1H-苯并咪唑的制备方法，其使用具有乳酸的乳酸复合物
公开(公告)号：WO2010091652A1
公开(公告)日：2010-08-19
申请号：PCT/CZ2010/000018
申请日：2010-02-16
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 method of manufacturing ( S )-5-methoxy-2-[[(4- methoxy-3,5-dimethyl-2-pyridinyl)methyl]sulfinyl]-1 H -benzimidazole of formula (I) and its salts of general formula (II), wherein the sulfide of general formula (III) is oxidized with hydroperoxides on a catalyst consisting of a chiral metallic complex containing ligands constituted by chiral functional derivatives of lactic acid.
摘要翻译：本发明涉及制备式（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-苯并咪唑的新方法和其通式（II）的盐，其中通式（III）的硫化物用氢过氧化物在由含有由乳酸的手性功能衍生物构成的配体的手性金属配合物组成的催化剂上被氧化。

3. 发明申请

WO2009106021A1 INTERMEDIATES FOR THE PREPARATION OF (3R, 4S) -1- (4-FLUOROPHENYL) -3- [ (3S) -3- (4-FLUOROPHENYL) -3-HYDROXYPROPYL) ] -4- (4-HYDROXYPHENYL) -2-AZETIDINONE 审中-公开
标题翻译：制备的中间体（3
公开(公告)号：WO2009106021A1
公开(公告)日：2009-09-03
申请号：PCT/CZ2009/000016
申请日：2009-02-13
申请人： ZENTIVA, K.S. , STEPANKOVA, Hana , HAJICEK, Josef , SLAVIKOVA, Marketa , ZEZULA, Josef
发明人： STEPANKOVA, Hana , HAJICEK, Josef , SLAVIKOVA, Marketa , ZEZULA, Josef
IPC分类号： C07D263/26 , C07D205/08
CPC分类号： C07D263/26 , C07D205/08 , Y02P20/55
摘要： A method for the preparation of ( S )-alcohol oxazolidides of general formula II, in which PG represents hydrogen or a hydroxyl protecting group, such as trimethylsilyl, tert -butyldimethylsilyl, benzyloxycarbonyl, tert -butoxycarbonyl, benzyl, benzhydryl or trityl, in which a ketal oxazolidide of general formula III, where PG has the same meaning as above and R means an alkyl with 1-4 carbon atoms, linear or branched, such as methyl, ethyl, isopropyl or butyl, or R+R together represents a divalent alkyl, or substituted with 1 or 2 alkyl groups, e.g. 1,2-ethylene, 1,2-propylene, 1,2-butylene, 1,3-propylene or 2,2-dimethyl-l,3- propylene, is deprotected by the action of acidic reagents in a mixture of water and a water- miscible solvent in the temperature range of 0 to 100 °C (stage A), and the obtained ketone oxazolidide of general IV, in which PG has the same meaning as above, is reduced with asymmetrical reagents in an inert organic solvent in the temperature range of -30 to +40 °C (stage B).
摘要翻译：制备通式II的（S） - 醇恶唑烷的方法，其中PG代表氢或羟基保护基，如三甲基甲硅烷基，叔丁基二甲基甲硅烷基，苄氧羰基，叔丁氧基羰基，苄基，二苯甲基或三苯甲基，其中通式III的缩酮恶唑烷，其中PG具有与上述相同的含义，R表示具有1-4个碳原子的直链或支链的烷基，例如甲基，乙基，异丙基或丁基，或R + R一起表示二价烷基，或被1或2个烷基取代，例如 1,2-亚乙基，1,2-亚丙基，1,2-亚丁基，1,3-丙烯或2,2-二甲基-1,3-丙烯，通过在水和水的混合物中的酸性试剂的作用脱保护在0〜100℃的温度范围（A阶段）的水溶性溶剂，所得到的通式IV的酮恶唑烷（其中PG具有与上述相同的含义）在惰性有机溶剂中用不对称试剂还原温度范围为-30至+40°C（B级）。

4. 发明申请

WO2009140932A3 METHOD OF PRODUCING (3R,4S)-L-(4-FLUOROPHENYL)-3-[(3S)-3-(4-FLUOROPHENYL)- HYDROXYPROPYL)]-4-(4-HYDROXYPHENYL)-2-AZETIDINONE 审中-公开
公开(公告)号：WO2009140932A3
公开(公告)日：2009-11-26
申请号：PCT/CZ2009/000070
申请日：2009-05-15
申请人： ZENTIVA, K.S. , SLAVIKOVA, Marketa , STEPANKOVA, Hana , ZEZULA, Josef , HAJlCEK, Josef
发明人： SLAVIKOVA, Marketa , STEPANKOVA, Hana , ZEZULA, Josef , HAJlCEK, Josef
IPC分类号： C07D263/26 , C07D205/08
摘要： Method of producing (3R,4S)1 -(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3- hydroxypropyl)]-4-(4-hydroxyphenyl)-2-azetidinone (ezetimibe) of formula 1, in which alcohol-oxazolidide of general formula II, wherein PG is a phenol protecting group, is silylated by silylation agents in an inert organic solvent in the temperature range of -10°C to the boiling temperature of the mixture; the obtained silylether-oxazolidide of general formula III, wherein PG is as defined above and X is a silyl group is cyclized by action of bis(trimethyIsilyl)acetamide and a base in an inert organic solvent in the temperature range of, -20 to 40°C; and, finally, the obtained protected azetidinone of general formula IV is deprotected by action of deprotecting hydrogenolytic agents and/or acidic agents in an inert organic solvent.

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

WO2011057592A1 METHOD OF PRODUCING HIGHLY PURE PRASUGREL AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF 审中-公开
标题翻译：生产高纯度原料的方法及其药学上可接受的盐
公开(公告)号：WO2011057592A1
公开(公告)日：2011-05-19
申请号：PCT/CZ2010/000115
申请日：2010-11-12
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： A method for the production of 5-[2-cyclopropyl-1-(2-fluorophenyl)-2-oxoethyl]- 4,5,6,7-tetrahydrothieno[3,2-c]pyridin-2-yl acetate of formula (I) or its salts, characterized in that the compound of formula (III) in the form of a salt with an arene sulfonic acid is reacted with the compound of formula (XV), wherein Y means: chlorine, bromine, or an OR 4 group, wherein R 4 means an alkane sulfonic group or arene sulfonic group, in an organic solvent in the presence of an inorganic base or organic base, to give, after addition of an acetylating reagent and organic base to the reaction mixture, the compound of formula (I), which, after addition of a co-solvent, is crystallized from the reaction mixture, and the compound of formula (I) is optionally purified by crystallization and optionally converted to a salt by reaction with an organic or inorganic acid in a suitable solvent. (Formulae (I), (III), (XV)
摘要翻译：制备式（I）的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]吡啶-2-基乙酸酯的方法（I）化合物或其盐，其特征在于与式（ⅩⅤ）化合物反应呈与磺酰基磺酸盐形式的式（Ⅳ）化合物，其中Y表示：氯，溴或OR 4 基团，其中R 4表示烷基磺酸基或芳烃磺酸基，在有机溶剂中，在无机碱或有机碱的存在下，在反应混合物中加入乙酰化试剂和有机碱后，得到式（I），其在加入共溶剂之后从反应混合物中结晶，并且式（I）化合物任选地通过结晶进行纯化，并任选地通过与有机或无机酸反应形成盐合适的溶剂。（式（I），（III），（XV）

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

WO2011057593A2 NEW SALTS OF PRASUGREL AND A METHOD OF THEIR PRODUCTION 审中-公开
标题翻译： PRASUGREL的新销售及其生产方法
公开(公告)号：WO2011057593A2
公开(公告)日：2011-05-19
申请号：PCT/CZ2010/000116
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。

9. 发明申请

WO2010060389A1 A METHOD FOR THE MANUFACTURE OF HIGHLY PURE PRASUGREL 审中-公开
标题翻译：一种制备高纯度原料的方法
公开(公告)号：WO2010060389A1
公开(公告)日：2010-06-03
申请号：PCT/CZ2009/000139
申请日：2009-11-24
申请人： ZENTIVA, K.S. , STEPANKOVA, Hana , HAJICEK, Josef , DOUSA, Michal
发明人： STEPANKOVA, Hana , HAJICEK, Josef , DOUSA, Michal
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The invention deals with preparation of the substance prasugrel, using 3- cyclopropyl-1 -(2-fluorophenyl)-3-oxopropyl methanesulfonate for alkylation of 2-oxo- thienotetrahydropyridine, which may be in the form of a salt, e.g. with hydrochloric acid or p-toluenesulfonic acid. The resulting compound of formula II is acylated, preferably with acetanhydride, preferably directly in the reaction mixture without isolation, and the produced prasugrel of formula I can then be crystallized directly from the reaction mixture.
摘要翻译：本发明涉及使用3-环丙基-1-（2-氟苯基）-3-氧代丙基甲磺酸酯来制备物质普拉格雷，用于烷基化2-氧代 - 噻吩并四氢吡啶，其可以是盐形式。用盐酸或对甲苯磺酸。所得到的式II化合物优选用乙酸酐进行酰化，优选直接在反应混合物中进行分离，然后可以将所生成的式I的普拉格雷直接从反应混合物中结晶。

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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