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    Synthesis of diethyl{[5-(3-fluorophenyl)-pyridine-2yl]methyl}phosphonate
    5.
    发明申请
    Synthesis of diethyl{[5-(3-fluorophenyl)-pyridine-2yl]methyl}phosphonate 有权
    {[5-（3-氟苯基） - 吡啶-2-基]甲基}膦酸二乙酯的合成

    公开(公告)号：US20080004449A1

    公开(公告)日：2008-01-03

    申请号：US11824245

    申请日：2007-06-29

    申请人： Kelvin Yong ,  Ilia Zavialov ,  Jianguo Yin ,  Xiaoyong Fu ,  Tiruvettipuram Thiruvengadam

    发明人： Kelvin Yong ,  Ilia Zavialov ,  Jianguo Yin ,  Xiaoyong Fu ,  Tiruvettipuram Thiruvengadam

    IPC分类号： C07D405/02

    CPC分类号： C07D405/06 ,  C07F9/58

    摘要： This application discloses a novel process for the preparation of phosphonate esters useful as intermediates in the preparation of himbacine analogs, themselves useful as thrombin receptor antagonists. The chemistry taught herein can be exemplified by the following scheme: wherein R9 is selected from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms, and R11 is selected independently for each occurrence from alkyl, aryl heteroaryl and arylalkyl groups having 1 to 10 carbon atoms and hydrogen, X2 is Cl, Br, or I; X3 is selected from Cl and Br; and PdLn is a supported palladium metal catalyst or a soluble heterogeneous palladium catalyst. The L-derivatizing reagent is a moiety which converts the alcohol functional group of compound 137D to any leaving group which can be displaced by a triorgano-phosphite phosphonating agent.

    摘要翻译： 本申请公开了一种制备膦酸酯的新方法，其可用作制备作为凝血酶受体拮抗剂的替卡宾类似物的中间体。 本文教导的化学实例可以通过以下方案来举例说明：其中R 9选自具有1至10个碳原子的烷基，芳基杂芳基和芳基烷基，R 11是 从烷基，芳基杂芳基和具有1-10个碳原子的芳基烷基和氢独立地选择，X 2是Cl，Br或I; X 3选自Cl和Br; 并且PdL n是负载型钯金属催化剂或可溶性多相钯催化剂。 L-衍生试剂是将化合物137D的醇官能团转化成可被三有机 - 亚磷酸酯膦酸酯取代的任何离去基团的部分。