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1. 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。

2. 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。

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。

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