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    SYNTHESIS Of DIETHYLPHOSPHONATE
    5.
    发明申请
    SYNTHESIS Of DIETHYLPHOSPHONATE 有权
    二乙基磷酸酯的合成

    公开(公告)号：US20100137597A1

    公开(公告)日：2010-06-03

    申请号：US12701174

    申请日：2010-02-05

    申请人： Kelvin H. Yong ,  Ilia A. Zavialov ,  Jianguo Yin ,  Xiaoyong Fu ,  Tiruvettipuram K. Thiruvengadam

    发明人： Kelvin H. Yong ,  Ilia A. Zavialov ,  Jianguo Yin ,  Xiaoyong Fu ,  Tiruvettipuram K. Thiruvengadam

    IPC分类号： C07F9/40

    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R9选自具有1-10个碳原子的烷基，芳基杂芳基和芳基烷基，R11各自独立地选自烷基，芳基杂芳基和具有1至 10个碳原子和氢，X2是Cl，Br或I; X3选自Cl和Br; PdLn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。

    Process for the preparation of cyclopropylacetylene
    6.
    发明授权
    Process for the preparation of cyclopropylacetylene 有权
    环丙基乙炔的制备方法

    公开(公告)号：US06297410B1

    公开(公告)日：2001-10-02

    申请号：US09481812

    申请日：2000-01-12

    申请人： Joseph M. Fortunak ,  Zhe Wang ,  Jianguo Yin

    发明人： Joseph M. Fortunak ,  Zhe Wang ,  Jianguo Yin

    IPC分类号： C07C202

    CPC分类号： C07C51/353 ,  C07C1/30 ,  C07C13/04 ,  C07C17/093 ,  C07C51/38 ,  C07C2601/02 ,  C07C2601/04 ,  C07C22/00 ,  C07C57/26

    摘要： The present invention relates generally to novel methods for the synthesis of cyclopropylacetylene which is an essential reagent in the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one; a useful human immunodeficiency virus (HIV) reverse transcriptase inhibitor. In the process, cyclopropane carboxaldehyde is condensed with malonic acid to form 3-cyclopropylacrylic acid; 3-cyclopropylacrylic acid is halogenated to form (E,Z)-1-halo-2-cyclopropylethylene; and (E,Z)-1-halo-2-cyclopropylethylene is dehydrohalogenated to form cyclopropyl acetylene. This improvement provides for high conversion of inexpensive, readily available starting materials into cyclopropylacetylene, high overall yields and can be conducted on an industrial scale.

    摘要翻译： 本发明一般涉及用于合成环己基乙炔的新方法，其是不对称合成（S）-6-氯-4-环丙基乙炔基-4-三氟甲基-1,4-二氢-2H-3,1 苯并恶嗪-2-酮; 一种有用的人类免疫缺陷病毒（HIV）逆转录酶抑制剂。 在此过程中，环丙烷甲醛与丙二酸缩合形成3-环丙基丙烯酸; 将3-环丙基丙烯酸卤化形成（E，Z）-1-卤代-2-环丙基乙烯; 和（E，Z）-1-卤代-2-环丙基乙烯脱卤化氢形成环丙基乙炔。 这种改进提供了廉价的，容易获得的起始原料转化成环丙基乙炔的高转化率，高的总收率并且可以在工业规模上进行。

    Synthesis of diethyl{[5-(3-fluorophenyl)-pyridine-2yl]methyl}phosphonate
    9.
    发明授权
    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：US07687631B2

    公开(公告)日：2010-03-30

    申请号：US11824245

    申请日：2007-06-29

    申请人： Kelvin H. Yong ,  Ilia A. Zavialov ,  Jianguo Yin ,  Xiaoyong Fu ,  Tiruvettipuram K. Thiruvengadam

    发明人： Kelvin H. Yong ,  Ilia A. Zavialov ,  Jianguo Yin ,  Xiaoyong Fu ,  Tiruvettipuram K. Thiruvengadam

    IPC分类号： C07D405/06

    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R9选自具有1-10个碳原子的烷基，芳基杂芳基和芳基烷基，R11各自独立地选自烷基，芳基杂芳基和具有1至 10个碳原子和氢，X2是Cl，Br或I; X3选自Cl和Br; PdLn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。