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11 条记录 (耗时 0.02 秒)

    Methods for preparing macrocyclic products by ring-closing diyne metathessis
    1.
    发明授权
    Methods for preparing macrocyclic products by ring-closing diyne metathessis 失效
    通过闭环二炔复制制备大环产物的方法

    公开(公告)号：US06525197B1

    公开(公告)日：2003-02-25

    申请号：US09601632

    申请日：2000-08-04

    申请人： Alois Fürstner ,  Günter Seidel ,  Antonio Rumbo ,  Christian Mathes

    发明人： Alois Fürstner ,  Günter Seidel ,  Antonio Rumbo ,  Christian Mathes

    IPC分类号： A61K3133

    CPC分类号： C07D315/00 ,  C07B37/10 ,  C07D245/02 ,  C07D321/00 ,  C07D491/04

    摘要： The present invention relates to methods for preparing macrocyclic products having 9 or more ring atoms by ring-closing diyne metathesis of suitable diyne substrates. The diyne substrates can be converted into cycloalkynes or into cycloalkadiynes by cyclodimerization, depending on the particular reaction conditions. Any alkyne metathesis catalyst can be used as the catalyst, regardless of whether said catalysts are heterogeneously or homogeneously present in the reaction medium. The preferred catalysts or pre-catalysts are transition metal alkylidyne complexes, transition metal compounds which form alkylidyne complexes under the reaction conditions, and transition metal compounds with metal-metal triple bonds. The method can be carried out with numerous functional groups, solvents, and additives. Using known methods, the formed macrocyclic cycloalkynes or cycloalkadiynes can be converted into numerous secondary products, especially macrocyclic cycloalkenes with a uniform configuration of the double bond, and used, e.g., for the synthesis of epothilone or epothilone analogues.

    摘要翻译： 本发明涉及通过合适的二炔底物的闭合二炔复分解制备具有9个或更多个环原子的大环产物的方法。 取决于具体的反应条件，二炔底物可以通过环二聚化转化为环炔或环炔二炔。 任何炔烃复分解催化剂都可以用作催化剂，而不管所述催化剂是不均匀还是均匀地存在于反应介质中。 优选的催化剂或预催化剂是过渡金属烷基炔配合物，在反应条件下形成亚烷基二炔配合物的过渡金属化合物和具有金属 - 金属三键的过渡金属化合物。 该方法可以用许多官能团，溶剂和添加剂进行。 使用已知的方法，形成的大环环炔或环链炔二炔可以转化为许多次级产物，特别是具有双键均匀构型的大环环烯烃，并且用于例如合成埃坡霉素或埃坡霉素类似物。

    Enantioselective process for the preparation of both enantiomers of 10,11-dihydro-10-hydroxy-5h-dibenz[b,f]azepine-5-carboxamide and new crystal forms thereof
    2.
    发明申请
    Enantioselective process for the preparation of both enantiomers of 10,11-dihydro-10-hydroxy-5h-dibenz[b,f]azepine-5-carboxamide and new crystal forms thereof 审中-公开
    用于制备10,11-二氢-10-羟基-5h-二苯并[b，f]吖庚因-5-甲酰胺及其新的晶体形式的两种对映体的对映选择性方法

    公开(公告)号：US20060142566A1

    公开(公告)日：2006-06-29

    申请号：US10530617

    申请日：2003-10-06

    申请人： Christian Mathes ,  Gottfried Sedelmeier ,  Fritz Blatter ,  Sabine Pfeffer ,  Dominique Grimler

    发明人： Christian Mathes ,  Gottfried Sedelmeier ,  Fritz Blatter ,  Sabine Pfeffer ,  Dominique Grimler

    IPC分类号： C07D223/18

    CPC分类号： C07D223/24 ,  C07F15/0053

    摘要： The invention relates to a novel process for the manufacture of substituted enantiopure 10hydroxy-dihydrodibenz[b,f]azepines (Ia), (Ib) wherein each of R1 and R2, independently, are hydrogen, halogen, amino or nitro; and each of R3 and R4, independently, are hydrogen or C1-C6alkyl; by transfer hydrogenation of 10-oxo-dihydrodibenz[b,f]azepines; and to novel catalysts of formula (III′a) and (III′b) wherein M is Ru, Rh, Ir, Fe, Co or Ni; L1 is hydrogen; L2 represents an aryl or aryl-aliphatic residue; and the further radicals have the meanings as defined herein; and to new crystal forms of both enantiomers of 10,11-dihydro-10 hydroxy-5Hdibenz[b,f]azepine-5-carboxamide, obtainable by the new processes, their usage in the production of pharmaceutical preparations, new pharmaceutical preparations comprising these new crystal forms and/or the use of these new crystal forms in the treatment of disorders such as epilepsy, or in the production of pharmaceutical formulations which are suitable for this treatment.

    摘要翻译： 本发明涉及用于制备取代的对映体纯的10-羟基 - 二氢二苯并[b，f]吖庚因（Ia），（Ib）的新方法，其中R 1和R 2中的每一个 独立地是氢，卤素，氨基或硝基; R 3和R 4中的每一个独立地是氢或C 1 -C 6烷基; 通过10-氧代 - 二氢二苯并[b，f]吖庚因的转移氢化; 和式（III'a）和（III'b）的新型催化剂，其中M是Ru，Rh，Ir，Fe，Co或Ni; L 1是氢; L 2代表芳基或芳基脂族残基; 并且其它基团具有如本文所定义的含义; 以及可通过新方法获得的10,11-二氢-10羟基-5H-二苯并[b，f]吖庚因-5-甲酰胺的两种对映异构体的新结晶形式，它们在制备药物制剂中的用途，包含这些的新药物制剂 新的晶体形式和/或这些新的晶体形式用于治疗疾病如癫痫或使用适于该治疗的药物制剂。