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    Epoxycarboxylic acid amides, azides and amino alcohols and processes for preparation of alpha-keto amides by using them
    46.
    发明公开
    Epoxycarboxylic acid amides, azides and amino alcohols and processes for preparation of alpha-keto amides by using them 审中-公开
    环氧羧基芥酸酰胺，叠氮和氨基烷醇洗涤剂Verfahren zur Herstellung von Alpha-Ketoamiden damit

    公开(公告)号：EP2289888A3

    公开(公告)日：2011-07-13

    申请号：EP10011261.4

    申请日：2001-06-29

    申请人： SEIKAGAKU CORPORATION

    发明人： Kobayashi, Nubuo ,  Koji, Tsuneo ,  Fujita, Takashi ,  Nishimura, Tomofumi ,  Hosoda, Akihiko

    IPC分类号： C07D303/48 ,  C07D295/20 ,  C07D317/66 ,  C07D207/16 ,  C07C247/12 ,  C07C237/22 ,  C07C271/22 ,  C07C231/12 ,  C07C231/16

    CPC分类号： C07D295/215 ,  C07C231/12 ,  C07C231/16 ,  C07C237/22 ,  C07C247/12 ,  C07C271/22 ,  C07C2601/14 ,  C07D207/16 ,  C07D295/18 ,  C07D303/46 ,  C07D303/48 ,  C07D317/66 ,  C07D405/12 ,  C07D407/12 ,  C07D413/12

    摘要： The present invention is to provide manufacturing intermediates which can be led to useful α-ketoamide compounds having protease-inhibiting activity extremely economically and stereoselectively, and to provide amino alcohol compounds represented by the following formula:

    wherein R 1 and R 2 each represents alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group; R 3 represents alkyl group, alkenyl group, aromatic hydrocarbon group, heterocyclic group, R 6 -O- or R 7 -N(R 8 )-; where R 6 represents alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group; R 7 and R 8 each represents hydrogen atom, alkyl group, alkenyl group, aromatic hydrocarbon group or heterocyclic group, and, R 4 and R 5 represent the same groups as R 7 and R 8 , respectively, and R 9 and R 5 optionally form a ring together; and X represents -O- or -N(R 9 )-, where R 9 represents hydrogen atom or alkyl group, and X optionally forms a ring together with R 4 or R 5 ,
    and processes for preparing α-keto amide compound using the same.

    摘要翻译： 本发明提供制造中间体，其可以被极端经济和立体选择性地引入具有蛋白酶抑制活性的有用的α-酮酰胺化合物，并提供由下式表示的环氧羧酰胺化合物，叠氮化合物和氨基醇化合物： CHEM> 其中R 1和R 2各自表示烷基，烯基，芳族烃基或杂环基; R 3表示烷基，烯基，芳族烃基，杂环基，R 6 -O-或R 7 -N（R 8） - ; 其中R 6表示烷基，烯基，芳族烃基或杂环基; R 7和R 8各自表示氢原子，烷基，链烯基，芳香族烃基或杂环基，R 4和R 5表示与R 7和R 7相同的基团， 8>，R 4和R 5任选地形成环; 并且X表示-O-或-N（R 9） - ，其中R 9表示氢原子或烷基，X任选地与R 4或R 5一起形成环，并且 用相同的方法制备α-酮酰胺化合物。

    Synthesis Of Renin Inhibitors Involving A Cycloaddition Reaction
    47.
    发明公开
    Synthesis Of Renin Inhibitors Involving A Cycloaddition Reaction 审中-公开
    Synthese von Reninhemmern mit einer Cycloadditionsreaktion

    公开(公告)号：EP2287153A1

    公开(公告)日：2011-02-23

    申请号：EP10178025.2

    申请日：2006-09-26

    申请人： Novartis AG

    发明人： Mickel, Stuart, John ,  Marterer, Wolfgang

    IPC分类号： C07D207/16 ,  C07C251/24 ,  C07C237/22

    CPC分类号： C07C251/24 ,  C07C231/12 ,  C07D207/08 ,  C07D207/16 ,  C07C237/22

    摘要： The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a process for the manufacture of a compound of the formula III,

    wherein R, R 1 , and R' are as defined in the specification, or a salt thereof, and a compound of formula IV

    wherein R, R 1 , R 2 and R' are as defined in the specification, and processes of manufacturing these.

    摘要翻译： 本发明涉及可用于合成药物活性化合物，特别是如阿利吉仑的肾素抑制剂的新方法，新方法步骤和新型中间体。 特别地，本发明涉及制备式III化合物的方法，其中R，R 1和R'如本说明书中所定义，或其盐和式IV化合物，其中R， R 1，R 2和R'如说明书中所定义，及其制造方法。