Synthesis of 3-(5-nitrocyclohex-1-enyl) acrylic acid and esters thereof
    3.
    发明申请
    Synthesis of 3-(5-nitrocyclohex-1-enyl) acrylic acid and esters thereof 失效
    3-(5-硝基环己-1-烯基)丙烯酸及其酯的合成

    公开(公告)号:US20080009651A1

    公开(公告)日:2008-01-10

    申请号:US11824246

    申请日:2007-06-29

    IPC分类号: C07C61/35 C07C201/06

    摘要: This application discloses provides a process for the introduction of nitro-group functionality into a compound which contains also a site of unsaturation and/or oxygen functionality by direct (one step) oxidation of an oxime functional group mediated by a molybdenum VI/VII peroxo complex, the process comprising: (a) providing a substrate of Formula I containing an oxime functional group;  wherein R1 and R2 are selected independently from linear, branched or cyclic alkyl and linear, branched or cyclic alkenyl groups, optionally substituted, with the proviso that at least one of R1 or R2 contains a carbon/carbon double bond; and (b) contacting said substrate of Formula I with a molybdenum oxidation complex, thereby oxidizing said oxime functional group to a nitro functional group to yield the structure of Formula III. Where R1 and R2 are as defined above.

    摘要翻译: 本申请公开提供了一种通过由钼VI / VII过氧配合物介导的肟官能团的直接(一步)氧化将硝基官能团引入到还含有不饱和位和/或氧官能团位点的化合物的方法 该方法包括:(a)提供含有肟官能团的式I的底物; 其中R 1和R 2独立地选自直链,支链或环状的烷基和直链,支链或环状烯基,任选被取代,条件是至少一个 R 1或R 2 2含有碳/碳双键; 和(b)使式I的底物与钼氧化络合物接触,从而将所述肟官能团氧化为硝基官能团,得到式III的结构。 其中R 1和R 2如上定义。

    Synthesis of diethyl{[5-(3-fluorophenyl)-pyridine-2yl]methyl}phosphonate
    6.
    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

    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。

    Process for the synthesis of azetidinones
    8.
    发明申请
    Process for the synthesis of azetidinones 审中-公开
    合成氮杂环丁酮的方法

    公开(公告)号:US20060135755A1

    公开(公告)日:2006-06-22

    申请号:US11305926

    申请日:2005-12-19

    IPC分类号: C07D205/02 C07H17/02

    CPC分类号: C07D205/08 C07H17/02

    摘要: A process is provided for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, comprising reacting a β-(substituted-amino)amide, a β-(substituted-amino)acid ester, or a β-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent selected from the group consisting of alkali metal carboxylates, quaternary ammonium carboxylates, quaternary ammonium hydroxides, quaternary ammonium alkoxides, quaternary ammonium aryloxides and hydrates thereof, or the reaction product of: (i) at least one quaternary ammonium halide and at least one alkali metal carboxylate; or (ii) at least one quaternary ammonium chloride, quaternary ammonium bromide, or quaternary ammonium iodide and at least one alkali metal fluoride, wherein a quaternary ammonium moiety of the cyclizing agent is unsubstituted or substituted by one to four groups independently selected from the group consisting of alkyl, arylalkyl and arylalkyl-alkyl.

    摘要翻译: 提供了一种制备氮杂环丁酮的方法,该氮杂环丁酮可用作Penems的合成中的中间体和低胆固醇血症药,包括使β-(取代的 - 氨基)酰胺,β-(取代的 - 氨基)酸酯或β-(取代的 - 氨基) 氨基)硫代碳酸酯与甲硅烷基化剂和选自碱金属羧酸盐,季铵羧酸盐,季铵氢氧化物,季铵醇盐,季铵氧化物及其水合物的环化剂,或其反应产物:(i )至少一种季铵卤化物和至少一种碱金属羧酸盐; 或(ii)至少一种季铵氯化物,季铵溴化物或季铵碘化物和至少一种碱金属氟化物,其中环化剂的季铵部分是未取代的或被一至四个独立地选自 由烷基,芳烷基和芳基烷基 - 烷基组成。