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1. 发明申请

WO2012013325A1 PROCESS FOR THE PREPARATION OF KEY INTERMEDIATES FOR THE SYNTHESIS OF STATINS OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF 审中-公开
标题翻译：制定合理统计资料的主要中间人或药物可接受的费用的程序
公开(公告)号：WO2012013325A1
公开(公告)日：2012-02-02
申请号：PCT/EP2011/003714
申请日：2011-07-25
申请人： LEK PHARMACEUTICALS D.D. , CASAR, Zdenko , STERK, Damjan , JUKIC, Marko
发明人： CASAR, Zdenko , STERK, Damjan , JUKIC, Marko
IPC分类号： C07D215/14 , C07D239/46 , C07C49/233 , C07C49/235
CPC分类号： C07D239/42 , C07C45/68 , C07C49/807 , C07C49/86 , C07D215/12 , C07D215/14 , C07D239/46
摘要： The invention relates to commercially viable process for the synthesis of key intermediates for the preparation of statins, in particular Rosuvastatin and Pitavastatin or respective pharmaceutically acceptable salts thereof. A new simple and short synthetic route for key intermediates is presented which benefits from the use of cheap and readily available starting materials, by which the conventionally most frequently used DIBAL-H as reducing agent can be avoided.
摘要翻译：本发明涉及用于合成用于制备他汀类药物的关键中间体的商业上可行的方法，特别是罗苏伐他汀和匹伐他汀或其各自的药学上可接受的盐。提出了一种关键中间体的简单且简短的合成路线，其优点是可以使用便宜且易于获得的起始原料，可以避免常规使用的DIBAL-H作为还原剂。

2. 发明申请

WO2009133097A1 PREPARATION OF N-6 DEMETHYLATED, 9-10-DIHYDROLYSERGIC ACID ALKYL ESTERS 审中-公开
标题翻译：制备N-6脱乙酰基9-10-二羟基丙酸酯
公开(公告)号：WO2009133097A1
公开(公告)日：2009-11-05
申请号：PCT/EP2009/055117
申请日：2009-04-28
申请人： LEK PHARMACEUTICALS D.D. , CASAR, Zdenko , MESAR, Tomaz
发明人： CASAR, Zdenko , MESAR, Tomaz
IPC分类号： C07D457/02 , C07D457/04 , C07D457/06 , A61K31/48 , A61P25/00
CPC分类号： C07D457/04 , C07D457/02 , C07D457/06
摘要： A process for producing N -6 demethylated 9,10-dihydrolysergic acid alkyl ester is described, which comprises a step of N -6 demethylation of 9,10-dihydrolysergic acid alkyl esters with chloroformate and wherein the N -6 demethylation step is performed in the presence of an organic catalyst. Further, a process for converting a compound of formula (I) (DHLSAIkyl) into a compound of formula (Il) (DHLSAIkyl-F) comprises the steps of: providing (and maintaining) a reaction medium free of water and/or HCI, and reacting DHLSAIkyl with chloroformate in said reaction medium free of water and/or HCI, to obtain the compound of formula (Il) (DHLSAIkyl-F).
摘要翻译：描述了制备N-6去甲基化9,10-二氢关键酸烷基酯的方法，其包括用氯甲酸酯将9,10-二氢赖氨酸烷基酯N-6脱甲基化的步骤，其中N-6去甲基化步骤在存在有机催化剂。此外，将式（I）（DHLSA烷基）化合物转化成式（II）化合物（DHLSA烷基-F）的方法包括以下步骤：提供（和维持）不含水和/或HCl的反应介质，并在不含水和/或HCl的所述反应介质中使DHLSA烷基与氯甲酸酯反应，得到式（II）化合物（DHLSA-F-F）。

3. 发明申请

WO2009115585A1 CATALYZED CARBONYLATION IN THE SYNTHESIS OF ANGIOTENSIN II ANTAGONISTS 审中-公开
标题翻译：合成二氧化钛拮抗剂中的催化羰基化
公开(公告)号：WO2009115585A1
公开(公告)日：2009-09-24
申请号：PCT/EP2009/053269
申请日：2009-03-19
申请人： LEK PHARMACEUTICALS D.D. , CASAR, Zdenko , COPAR, Anton , CLUZEAU, Jerome , PREMRL, Andrej
发明人： CASAR, Zdenko , COPAR, Anton , CLUZEAU, Jerome , PREMRL, Andrej
IPC分类号： C07D403/04
CPC分类号： C07C17/263 , C07C17/14 , C07C17/2632 , C07D235/20 , Y10T436/147777 , C07C25/18
摘要： One embodiment disclosed in the invention is the efficient synthesis of halogenated biaryl starting material via Grignard chemistry and the use thereof. Another embodiment of the invention is the reaction of catalyzed carbonylation of the 3'-(2'-halo-biphenyl-4-ylmethyl)-1,7'-dimethyl-2'-propyl-1H,3'H-[2,5']bibenzoimidazolyl (TLMH) using either gaseous carbon monoxide in a solvent mixture containing water; or formic acid salts optionally together with acetic acid in anhydrous solvent.
摘要翻译：本发明公开的一个实施方案是通过格利雅化学及其用途有效地合成卤化联芳基原料。本发明的另一个实施方案是3' - （2'-卤代 - 联苯-4-基甲基）-1,7'-二甲基-2'-丙基-1H，3'H- [2， 5']联苯并咪唑基（TLMH），使用气态一氧化碳在含水的溶剂混合物中; 或甲酸盐任选地与乙酸一起在无水溶剂中。

4. 发明申请

WO2013150125A1 ß-BORATION OF ALKENE AND ALKYNE INTERMEDIATES 审中-公开
标题翻译：碱性和碱性中间体的β-沸石
公开(公告)号：WO2013150125A1
公开(公告)日：2013-10-10
申请号：PCT/EP2013/057159
申请日：2013-04-05
申请人： LEK PHARMACEUTICALS D.D. , STAVBER, Gaj , CASAR, Zdenko
发明人： STAVBER, Gaj , CASAR, Zdenko
IPC分类号： C07F5/04
CPC分类号： C07F5/04
摘要： The present invention relates to the field of organic chemistry, and in particular to the preparation of β-borated compounds. These β-borated compounds can be used as intermediates in the synthesis pharmaceutically active agents such as sitagliptin.
摘要翻译：本发明涉及有机化学领域，特别涉及β-硼酸化合物的制备。这些β-硼酸化合物可以用作合成药物活性剂如西他列汀的中间体。

5. 发明申请

WO2013104774A1 PREPARATION OF OPTICALLY PURE ß-AMINO ACID TYPE ACTIVE PHARMACEUTICAL INGREDIENTS AND INTERMEDIATES THEREOF 审中-公开
标题翻译：光学纯型β-氨基酸类活性药物成分的制备及其中间体
公开(公告)号：WO2013104774A1
公开(公告)日：2013-07-18
申请号：PCT/EP2013/050518
申请日：2013-01-11
申请人： LEK PHARMACEUTICALS D.D. , STAVBER, Gaj , CASAR, Zdenko
发明人： STAVBER, Gaj , CASAR, Zdenko
IPC分类号： C07C211/27 , C07C231/06 , C07C239/20 , C07F5/02 , C07C227/34 , C07C269/06 , C07C303/40 , C07C67/31
CPC分类号： C07C231/06 , C07B53/00 , C07B2200/07 , C07C67/31 , C07C211/27 , C07C227/34 , C07C239/20 , C07C269/06 , C07C303/40 , C07F5/02 , C07F7/0892 , C07F7/10 , C07C233/47 , C07C229/34 , C07C271/22 , C07C311/19 , C07C69/732
摘要： The present invention relates to the preparation of optically resolved chiral compounds of β-amino acid type active pharmaceutical ingredients (API), more specifically to β-aminobutyryl substituted compounds and especially β-aminobutyryl compounds having γ-bound aryl groups. The present invention more particularly relates to the preparation of enantiomerically enriched chiral compounds useful as intermediates for the preparation of anti-diabetic agents, preferably sitagliptin.
摘要翻译：本发明涉及β-氨基酸型活性药物成分（API）的光学拆分的手性化合物的制备，更具体地涉及具有γ-结合的芳基的β-氨基丁酰取代的化合物，特别是β-氨基丁酰基化合物。本发明更具体地涉及可用作制备抗糖尿病药物，优选西他列汀的中间体的对映异构体富集的手性化合物的制备。

6. 发明申请

WO2011154152A1 PROCESS FOR DEMETHYLATING AROMATIC METHYL ETHERS USING 3 -MERCAPTOPROPIONIC ACID 审中-公开
标题翻译：使用3-巯基丙酸酸化芳香族甲基醚的方法
公开(公告)号：WO2011154152A1
公开(公告)日：2011-12-15
申请号：PCT/EP2011/002866
申请日：2011-06-10
申请人： LEK PHARMACEUTICALS D.D. , CASAR, Zdenko , FURLAN, Borut
发明人： CASAR, Zdenko , FURLAN, Borut
IPC分类号： C07B41/02 , C07C213/08 , C07C215/64 , C07C45/67 , C07C49/84 , C07C201/12 , C07C205/25 , C07C253/30 , C07C255/53
CPC分类号： C07B41/02 , C07C45/673 , C07C201/12 , C07C213/08 , C07C253/30 , C07C2601/14 , C07C49/83 , C07C49/84 , C07C205/25 , C07C215/64 , C07C255/53 , C07C255/54
摘要： The present application discloses a process for demethylating aromatic methyl ethers by reaction with 3 -mercaptopropionic acid or salts thereof. One preferred example is the demethylation of venlafaxine forming 0 - desmethylvenlafaxine.
摘要翻译：本申请公开了通过与3-巯基丙酸或其盐反应来使芳族甲基醚脱甲基的方法。一个优选的实例是文拉法辛形成O-去甲基文拉法辛的去甲基化。

7. 发明申请

WO2011009831A1 PROCESS FOR THE PURIFICATION OF OLANZAPINE 审中-公开
标题翻译： OLANZAPINE的纯化方法
公开(公告)号：WO2011009831A1
公开(公告)日：2011-01-27
申请号：PCT/EP2010/060399
申请日：2010-07-19
申请人： LEK PHARMACEUTICALS D.D. , MESAR, Tomaz , CASAR, Zdenko
发明人： MESAR, Tomaz , CASAR, Zdenko
IPC分类号： C07D495/04 , A61K31/551 , A61P25/18
CPC分类号： C07D495/04
摘要： The present invention relates to a process for the purification of olanzapine, characterized in that said process comprises at least the following steps: (A) providing a solution of olanzapine in at least one organic solvent, (B) treating the solution obtained in step (A) with at least one non-acidic oxide adsorbent, and (C) removing the said non-acidic oxide adsorbent from the solution obtained in step (B), in order to obtain a solution of olanzapine in a pure form, to a mixture comprising olanzapine and at least one addition product of methylene chloride and olanzapine in an amount of 10 to 280 ppm, to a pharmaceutical formulation, to the use of said mixture and to a method of treating mental diseases and conditions, which comprises administering a therapeutically effective amount of said mixture in conjunction with a pharmaceutically acceptable diluent or carrier.
摘要翻译：本发明涉及一种纯化奥氮平的方法，其特征在于所述方法至少包括以下步骤：（A）在至少一种有机溶剂中提供奥氮平溶液，（B）将步骤 A）与至少一种非酸性氧化物吸附剂，和（C）从步骤（B）中获得的溶液中除去所述非酸性氧化物吸附剂，以获得纯的形式的奥氮平溶液至混合物包括奥氮平和至少一种10至280ppm的二氯甲烷和奥氮平的加成产物，药物制剂，使用所述混合物和治疗精神疾病和病症的方法，其包括施用治疗有效的所述混合物的量与药学上可接受的稀释剂或载体结合。

8. 发明申请

WO2010086438A1 KEY INTERMEDIATES FOR THE SYNTHESIS OF ROSUVASTATIN OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF 审中-公开
标题翻译：用于合成罗司伐他汀或其药学上可接受的盐的主要中间体
公开(公告)号：WO2010086438A1
公开(公告)日：2010-08-05
申请号：PCT/EP2010/051163
申请日：2010-02-01
申请人： LEK PHARMACEUTICALS D.D. , CASAR, Zdenko , KOSMRLJ, Janez
发明人： CASAR, Zdenko , KOSMRLJ, Janez
IPC分类号： C07D239/42 , A61K31/505 , A61P3/06
CPC分类号： C07D239/42 , A61K31/505 , A61K31/506 , C07D405/06 , C07F9/535 , C07F9/54
摘要： The present invention relates in general to the field of organic chemistry and in particular to the preparation of N -(4-(4-fluorophenyl)-6-isopropyl-5-methylpyrimidin-2-yl)- N - methylmethanesulfonamide (I), N -(4-(4-fluorophenyl)-5-(bromomethyl)-6-isopropylpyrimidin-2- yl)- N -methylmethanesulfonamide (II) and N -(4-(4-fluorophenyl)-5-(hydroxymethyl)-6- isopropylpyrimidin-2-yl)- N -methylmethanesulfonamide (III), key intermediates in preparation of Rosuvastatin.
摘要翻译：本发明一般涉及有机化学领域，特别涉及N-（4-（4-氟苯基）-6-异丙基-5-甲基嘧啶-2-基）-N-甲基甲磺酰胺（I）的制备， N-（4-（4-氟苯基）-5-（溴甲基）-6-异丙基嘧啶-2-基）-N-甲基甲磺酰胺（II）和N-（4-（4-氟苯基）-5-（羟甲基） 6-异丙基嘧啶-2-基）-N-甲基甲磺酰胺（III）是制备罗苏伐他汀的关键中间体。

9. 发明申请

WO2010012775A1 PROCESS FOR THE SYNTHESIS OF EZETIMIBE AND INTERMEDIATES USEFUL THEREFOR 审中-公开
标题翻译：合成EZETIMIBE及其有用的中间体的方法
公开(公告)号：WO2010012775A1
公开(公告)日：2010-02-04
申请号：PCT/EP2009/059813
申请日：2009-07-29
申请人： LEK PHARMACEUTICALS D.D. , MRAVLJAK, Janez , SOVA, Matej , KOVAC, Andreja , GOBEC, Stanislav , CASAR, Zdenko
发明人： MRAVLJAK, Janez , SOVA, Matej , KOVAC, Andreja , GOBEC, Stanislav , CASAR, Zdenko
IPC分类号： C07C57/60 , C07C69/65 , C07D205/08 , C07D263/26
CPC分类号： C07D263/26 , C07B2200/07 , C07C51/09 , C07C57/60 , C07C67/343 , C07C69/65 , C07D205/08
摘要： The present invention discloses novel and useful intermediates for the synthesis of ezetimibe (EZT), which intermediates share a characteristic Z-isomeric structure. Based on Z-5-(4-fluorophenyl)-pent-4-enoic acid, and proceeding the synthesis through further Z-intermediates, a total synthesis is presented to obtained final ezetimibe in high yields.
摘要翻译：本发明公开了用于合成依泽替米贝（EZT）的新型和有用的中间体，其中间体具有特征的Z-异构体结构。基于Z-5-（4-氟苯基） - 戊-4-烯酸，并通过进一步的Z-中间体进行合成，总共合成以高产率得到最终的依泽替米贝。

10. 发明申请

WO2009092702A3 ((2S,4R)-4,6-DIHYDROXYTETRAHYDRO-2H-PYRAN-2-YL)METHYL CARBOXYLATE AND PROCESS FOR THE PRODUCTION EMPLOYING A 2-DEOXYRIBOSE-5-PHOSPHATE ALDOLASE 审中-公开
公开(公告)号：WO2009092702A3
公开(公告)日：2009-07-30
申请号：PCT/EP2009/050583
申请日：2009-01-20
申请人： LEK PHARMACEUTICALS D.D. , CLUZEAU, Jerome , CASAR, Zdenko , MRAK, Peter , OSLAJ, Matej , KOPITAR, Gregor
发明人： CLUZEAU, Jerome , CASAR, Zdenko , MRAK, Peter , OSLAJ, Matej , KOPITAR, Gregor
IPC分类号： C12P17/06 , C07C67/00 , C07D239/00 , C07D309/00
摘要： The present invention relates to ((2S,4R)-4,6-dihydroxytetrahydro-2H-pyran-2-yl)methyl carboxylates and a process for the production thereof. Furthermore, the present invention relates to a process for the production of statins and in particular of Rosuvastatin and derivates thereof, wherein the above mentioned compounds are used as intermediates.

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