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    Process and intermediates for the synthesis of (3-alkyl-5-piperidin-1-yl-3,3a-dihydro-pyrazolo[1,5-a]pyrimidin-7-yl)-amino derivatives and intermediates
    2.
    发明授权
    Process and intermediates for the synthesis of (3-alkyl-5-piperidin-1-yl-3,3a-dihydro-pyrazolo[1,5-a]pyrimidin-7-yl)-amino derivatives and intermediates 有权
    合成（3-烷基-5-哌啶-1-基-3,3a-二氢 - 吡唑并[1,5-a]嘧啶-7-基） - 氨基衍生物和中间体的方法和中间体

    公开(公告)号：US08076479B2

    公开(公告)日：2011-12-13

    申请号：US11893857

    申请日：2007-08-17

    申请人： Frank Xing Chen ,  Kartik M. Keertikar ,  Shen-Chun Kuo ,  Hong-Chang Lee ,  Ramani R. Raghavan ,  George G. Wu ,  Ji Xie

    发明人： Frank Xing Chen ,  Kartik M. Keertikar ,  Shen-Chun Kuo ,  Hong-Chang Lee ,  Ramani R. Raghavan ,  George G. Wu ,  Ji Xie

    IPC分类号： C07D487/04 ,  A61K31/519

    CPC分类号： C07D487/04

    摘要： Disclosed is a process for the synthesis of compounds of Formula I by sequentially aminating, first with a primary amine and then with a secondary amine, an intermediate compound of the structure of Formula E1, wherein R1 is a linear, branched, or cyclic alkyloxy functional group of the structure (—R2a—OH), R2a is a linear, branched or cyclic alkyl group, R2 is a linear, branched or cyclic alkyl group, and R3 is an alkylene-heterocycle, said process comprising forming intermediate compound of Formula E1 by reacting, in a refluxing reaction solvent selected from alcohols having 5 or less carbon atoms and mixtures of two or more thereof, a methanol solution of a salt of a 4-alkyl-3-amino-pyrazole compound of Formula C1, with a diamidization reagent selected from dimethylmalonate, monomethylmalonyl-chloride, and malonyl dichloride in the presence of a Lewis base having sufficient proton affinity to abstract a proton from the 1-position nitrogen on the pyrazole ring.

    摘要翻译： 公开了通过依次胺化伯胺，然后通过仲胺，式E1结构的中间体化合物，其中R 1是直链，支链或环烷基官能的化合物来合成式I化合物的方法 （-R2a-OH）基，R2a是直链，支链或环状烷基，R2是直链，支链或环状的烷基，R3是亚烷基 - 杂环，所述方法包括形成式E1的中间体化合物 通过使选自具有5个或更少碳原子的醇的回流反应溶剂及其两种或更多种的混合物，将式C1的4-烷基-3-氨基 - 吡唑化合物的盐与二酰胺化反应 在具有足够的质子亲和力的路易斯碱存在下，选自丙二酸二甲酯，单甲基丙二酰氯和丙二酰氯的试剂从吡唑环上的1位氮抽出质子。

    Enantioselective alkylation of tricyclic compounds
    7.
    发明授权
    Enantioselective alkylation of tricyclic compounds 有权
    三环化合物的对映选择性烷基化

    公开(公告)号：US06307048B1

    公开(公告)日：2001-10-23

    申请号：US09442511

    申请日：1999-11-18

    申请人： Shen-Chun Kuo ,  Charles F. Bernard ,  Frank Xing Chen ,  Donald Hou ,  Agnes S. Kim-Meade ,  George G. Wu

    发明人： Shen-Chun Kuo ,  Charles F. Bernard ,  Frank Xing Chen ,  Donald Hou ,  Agnes S. Kim-Meade ,  George G. Wu

    IPC分类号： C07D40102

    CPC分类号： C07D401/04 ,  C07D401/14 ,  Y02P20/55

    摘要： Disclosed is a process for preparing a compound of the formula: wherein X1, X2, X3, X4, and X5 are independently selected from the group consisting of H, halo, alkyl, alkoxy, aryl, and aryloxy, and R is a protecting group, in which a compound having the formula wherein X1, X2, X3, X4, and X5 are as defined above, is treated with the following, in any sequence: (a) a non-nucleophilic strong base; (b) a chiral amino alcohol; and (c) a compound having the formula wherein L is a leaving group and R is as defined above. The compounds made by this process are useful intermediates for preparing compounds that are inhibitors of farnesyl protein transferase.

    摘要翻译： 公开了一种制备下式化合物的方法：其中X 1，X 2，X 3，X 4和X 5独立地选自H，卤素，烷基，烷氧基，芳基和芳氧基，R是保护基 其中具有如下定义的具有如下定义的化合物：（a）非亲核性强碱;（b）手性氨基醇（其中R 1，R 2，R 3，X 4， ; 和（c）具有甲醛的化合物L是离去基团，R如上定义。 通过该方法制备的化合物是制备法呢基蛋白转移酶抑制剂的化合物的有用中间体。