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    PREPARATION OF N-6 DEMETHYLATED, 9-10-DIHYDROLYSERGIC ACID ALKYL ESTERS
    1.
    发明申请
    PREPARATION OF N-6 DEMETHYLATED, 9-10-DIHYDROLYSERGIC ACID ALKYL ESTERS 审中-公开
    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）。

    ß-BORATION OF ALKENE AND ALKYNE INTERMEDIATES
    3.
    发明申请
    ß-BORATION OF ALKENE AND ALKYNE INTERMEDIATES 审中-公开
    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。

    PROCESS FOR HYDROGENATION OF HALOGENOALKENES WITHOUT DEHALOGENATION
    6.
    发明申请
    PROCESS FOR HYDROGENATION OF HALOGENOALKENES WITHOUT DEHALOGENATION 审中-公开
    没有脱盐的氢化氢加氢过程

    公开(公告)号：WO2010146176A3

    公开(公告)日：2011-02-24

    申请号：PCT/EP2010058672

    申请日：2010-06-18

    申请人： LEK PHARMACEUTICALS ,  GAZIC SMILOVIC IVANA ,  CASAR ZDENKO

    发明人： GAZIC SMILOVIC IVANA ,  CASAR ZDENKO

    IPC分类号： C07F5/02

    CPC分类号： C07F5/025

    摘要： The present invention relates to a process for preparing a compound of Formula (Vl), wherein R1 and R6 are hydrogen, substituted or unsubstituted alkyl substituted or unsubstituted aryl, or substituted or unsubstituted aralkyl; R5 is OR2, NR2R3, SR2, B (OR2)(OR3), or X" selected from F, Cl, Br, I, OCOR2, OSO2R2, wherein R2 and R3 independently from each other represent substituted or unsubstituted alkyl, substituted or unsubstituted aryl, or substituted or unsubstituted aralkyl; or R2 and R3 cooperatively form a part of a 5- to 10-membered fused or unfused ring, optionally a chiral 5- to 10- membered fused or unfused ring; X is selected from F1 Cl, Br, I; and * indicates a chiral center; by hydrogenation of a compound of Formula (V), wherein R1, R5, R6 and X are as defined above; wherein hydrogenation is conducted in the presence of a catalyst selected from complexes comprising at least one transition metal, wherein dehalogenation occurs in less than 10 molar % relative to the molar amount of the compound of formula Vl.

    摘要翻译： 本发明涉及制备式（VI）化合物的方法，其中R 1和R 6是氢，取代或未取代的烷基取代或未取代的芳基或取代或未取代的芳烷基; R5是选自F，Cl，Br，I，OCOR2，OSO2R2中的OR2，NR2R3，SR2，B（OR2）（OR3）或X“，其中R2和R3彼此独立地表示取代或未取代的烷基，取代或未取代的 芳基或取代或未取代的芳烷基;或R 2和R 3协同形成5至10元稠合或未稠合的环的一部分，任选的手性5-至10-元稠合或未稠合的环; X选自F1 C1， Br，I和*表示手性中心;通过氢化式（V）的化合物，其中R 1，R 5，R 6和X如上所定义;其中氢化在催化剂存在下进行，所述催化剂选自： 至少一种过渡金属，其中相对于式VI化合物的摩尔量，脱卤发生在小于10摩尔％的范围内。

    PROCESS FOR THE PURIFICATION OF OLANZAPINE
    7.
    发明申请
    PROCESS FOR THE PURIFICATION OF OLANZAPINE 审中-公开
    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。

    KEY INTERMEDIATES FOR THE SYNTHESIS OF ROSUVASTATIN OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF
    8.
    发明申请
    KEY INTERMEDIATES FOR THE SYNTHESIS OF ROSUVASTATIN OR PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF 审中-公开
    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。

    NEW SYNTHETIC ROUTE FOR THE PREPARATION OF ALPHA-AMINO BORONIC ESTERS
    9.
    发明申请
    NEW SYNTHETIC ROUTE FOR THE PREPARATION OF ALPHA-AMINO BORONIC ESTERS 审中-公开
    用于制备ALPHA-AMINO BORONIC ESTER的新合成路线

    公开(公告)号：WO2010146172A3

    公开(公告)日：2012-02-23

    申请号：PCT/EP2010058666

    申请日：2010-06-18

    申请人： LEK PHARMACEUTICALS ,  GAZIC SMILOVIC IVANA ,  CASAR ZDENKO

    发明人： GAZIC SMILOVIC IVANA ,  CASAR ZDENKO

    IPC分类号： C07F5/02 ,  C07C209/68 ,  C07F5/06 ,  C07F17/00 ,  C07K5/06

    CPC分类号： C07F5/025

    摘要： The present invention relates in general to the field of organic chemistry and in particular to the preparation of alpha-amino boronic esters. These compounds can be used as intermediates in the synthesis of boronic acid and ester compounds such as N- terminal peptidyl boronic acid derivatives, for example N-(pyrazin-2-yl)carbonyl-L-phenylalanine-L-leucine boronic acid, i.e. bortezomib.

    摘要翻译： 本发明一般涉及有机化学领域，特别涉及α-氨基硼酸酯的制备。 这些化合物可以用作硼酸合成中的中间体，例如N-末端肽基硼酸衍生物等酯化合物，例如N-（吡嗪-2-基）羰基-L-苯丙氨酸-L-亮氨酸硼酸，即 硼替佐米。