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1. 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）。

2. 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.

3. 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。

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

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。

6. 发明申请

WO2012089181A1 O-SUBSTITUTED (2R,3R)-3-(3-HYDROXYPHENYL)-2-METHYL-4-PENTENOIC ACIDS AND A METHOD OF OBTAINING THE SAME 审中-公开
标题翻译： O-取代的（2R，3R）-3-（3-羟基苯基）-2-甲基-4-对硝基苯酸及其获得方法
公开(公告)号：WO2012089181A1
公开(公告)日：2012-07-05
申请号：PCT/CZ2011/000128
申请日：2011-12-30
申请人： ZENTIVA, K.S. , VLASAKOVA, Ruzena , HAJICEK, Josef , ZEZULA, Josef
发明人： VLASAKOVA, Ruzena , HAJICEK, Josef , ZEZULA, Josef
IPC分类号： C07C213/02 , C07C231/02 , C07C51/09 , C07C51/377 , C07C51/60 , C07C59/52 , C07C59/64 , C07C213/08
CPC分类号： C07C213/08 , C07B2200/07 , C07C51/09 , C07C51/377 , C07C51/412 , C07C51/43 , C07C51/60 , C07C59/64 , C07C213/02 , C07C231/02 , C07C217/62 , C07C215/54 , C07C235/34
摘要： The compounds of general formula II are new and represent important intermediates in the synthesis of tapentadol. In the synthesis of tapentadol of formula I and its pharmaceutically acceptable salts, O-protected (2R,3R)-acids of general formula II, in step A, are reacted in an inert organic solvent with an activating agent, optionally in presence of a catalyst or a base; in step B, the obtained compounds of general formula V, wherein R has the above mentioned meaning and X stands for chlorine or alkoxycarbonyloxyl group O-CO-OR 1 or pivaloyloxyl O-CO-t-Bu group, wherein R 1 is methyl or ethyl, are reacted with dimethylamine or its salts optionally in presence of a base; in step C, the obtained N, N-dimethylamides of general formula VI, wherein R has the above mentioned meaning, are reduced by means of hydride agents in a suitable solvent; in step D, the produced alkeneamines of general formula VII, wherein R has the above mentioned meaning, are hydrogenated on a metal catalysts in a suitable solvent; and, finally, in step E, the produced alkaneamines of general formula VIII, wherein R has the above mentioned meaning, are O-dealkylated by means of dealkylating agents, and, if required, the obtained tapentadol is converted by the action of a pharmaceutically acceptable acid to respective salts, e.g. hydrochloride.
摘要翻译：通式II的化合物是新的，并且代表了他喷他多合成中的重要中间体。在式I的他喷他多和其药学上可接受的盐的合成中，步骤A中通式II的O-保护的（2R，3R） - 酸在惰性有机溶剂中与活化剂反应，任选在催化剂或碱; 在步骤B中，得到的通式V的化合物，其中R具有上述含义，X代表氯或烷氧基羰基氧基O-CO-OR1或新戊酰氧基O-CO-t-Bu基团，其中R1是甲基或乙基，与二甲胺或其盐任选在碱存在下反应; 在步骤C中，所得到的通式Ⅵ的N，N-二甲基酰胺，其中R具有上述含义，在合适的溶剂中用氢化剂还原; 在步骤D中，所制备的具有上述含义的通式VII的烯烃在合适的溶剂中在金属催化剂上氢化; 最后，在步骤E中，所制备的通式VIII的烷烃，其中R具有上述含义，通过脱烷基化剂进行O-脱烷基化，如果需要，所得到的他喷他多通过药学上的作用转化各种盐可接受的酸，例如盐酸盐。

7. 发明申请

WO2017063617A1 PREPARATION OF INTERMEDIATES FOR THE SYNTHESIS OF CANAGLIFLOZIN AND DAPAGLIFLOZIN 审中-公开
标题翻译：中间体用于合成格列齐嗪和双吗啉的制备
公开(公告)号：WO2017063617A1
公开(公告)日：2017-04-20
申请号：PCT/CZ2016/000103
申请日：2016-09-14
申请人： ZENTIVA, K.S.
发明人： ZEZULA, Josef , BABIAK, Petr , HAJDUCH, Jan
IPC分类号： C07H1/00 , C07H15/04
CPC分类号： C07H1/00 , C07H15/04
摘要： The present invention relates to a preparation method of the intermediates of structures la (for the synthesis of canagliflozin) and 1b (for the synthesis of dapagliflozin), where in structure la X is methyl and Ar represents 2-(5-(4-fluorophenyl)-thienyl) and in structure 1b X is chlorine and Ar represents 4-ethoxyphenyl.
摘要翻译：本发明涉及结构1a（用于合成坎格列净）和1b（用于合成达格列净）的中间体的制备方法，其中在结构1a中X为甲基且Ar表示2 - （5-（4-氟苯基） - 噻吩基）并且在结构1b中X是氯并且Ar代表4-乙氧基苯基。

8. 发明申请

WO2019047989A3 CRYSTALLINE FORMS OF (3α,5β,6α,7α)-6-ETHYL-3,7-DIHYDROXYCHOLAN-24-IC ACID 审中-公开
公开(公告)号：WO2019047989A3
公开(公告)日：2019-03-14
申请号：PCT/CZ2018/000040
申请日：2018-08-31
申请人： ZENTIVA, K.S.
发明人： SLAVIKOVA, Marketa , ZEZULA, Josef , CERNY, Josef , DAMMER, Ondrej , SIMEK, Michal
IPC分类号： C07J9/00 , A61K31/575 , A61P1/16
摘要： Crystalline form J-1 and J-2 of obeticholic acid, whereas crystalline form J-1 shows characteristic reflections in an X-ray powder record using CuKα radiation: 6.3; 9.4; 12.2; 14.4; 16.5 and 19.0 ± 0.2° 2-theta and crystalline form J-2 shows characteristic reflections in an X- ray powder record using CuKα radiation: 6.3; 8.9; 10.8; 15.8; 16.5; 18.4 and 20.3 ± 0.2° 2-theta.

9. 发明申请

WO2016095879A1 PREPARATION OF A HIGHLY PURE INTERMEDIATE FOR THE SYNTHESIS OF ODANACATIB 审中-公开
标题翻译：制备用于合成ODANACATIB的高纯度中间体
公开(公告)号：WO2016095879A1
公开(公告)日：2016-06-23
申请号：PCT/CZ2015/000151
申请日：2015-12-14
申请人： ZENTIVA, K.S.
发明人： BABIAK, Peter , ZEZULA, Josef
IPC分类号： C07C253/30
CPC分类号： C07C253/30 , C07C2601/02 , C07C255/46
摘要： A process for producing (S)-2-(((S)-1-(4-bromophenyl)-2,2,2-trifluoroethyl)amino)-N- (1-cyanocyclopropyl)-4-fluoro-4-methylpentanamide of formula 1 by reaction of the acid or its salts of formula 3 with the compound of formula 4, the reaction being performed in a solvent in the presence of the n-propanephosphonic acid anhydride of formula 5 and a base.
摘要翻译：制备（S）-2 - （（（S）-1-（4-溴苯基）-2,2,2-三氟乙基）氨基）-N-（1-氰基环丙基）-4-氟-4-甲基戊酰胺式1的酸或其盐与式4的化合物反应，反应在溶剂中，在式5的正丙酸膦酸酐和碱的存在下进行。

10. 发明申请

WO2017032350A1 CRYSTALLINE FORM A OF RILPIVIRINE ADIPATE AND A METHOD OF ITS PREPARATION 审中-公开
标题翻译：脯氨酸的晶体形式及其制备方法
公开(公告)号：WO2017032350A1
公开(公告)日：2017-03-02
申请号：PCT/CZ2016/000090
申请日：2016-08-12
申请人： ZENTIVA, K.S.
发明人： CERNY, Josef , ZEZULA, Josef , SLAVIKOVA, Marketa , DAMMER, Ondrej , PEKAREK, Tomas
IPC分类号： C07D239/48 , A61K31/505 , A61P31/18
CPC分类号： C07D239/48
摘要： The invention relates to crystalline Form A of rilpivirine adipate of formula I, with the systematic name 4-((4-((4-((lE)-2-Cyanoethenyl)-2,6- dimethyIphenyl)amino)-2-pyrimidinyl) amino)benzo- nitrile adipate and a preparation method of this crystalline form.
摘要翻译：本发明涉及式I的具有系统名称的4 - （（4 - （（4 - （（E）-2-氰基乙烯基）-2,6-二甲基苯基）氨基）-2-嘧啶基的系列名称的结晶形式A ）氨基）苯甲酸己二酸酯和该结晶形式的制备方法。

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