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    PREPARATION OF KETONE AMIDES
    1.
    发明公开
    PREPARATION OF KETONE AMIDES 审中-公开
    酮酮的制备

    公开(公告)号：EP1838695A2

    公开(公告)日：2007-10-03

    申请号：EP06717452.4

    申请日：2006-01-05

    申请人： Schering Corporation

    发明人： KUO, Shen-Chun ,  TSAI, David, Jieh-Shyh ,  LIAO, Hongbiao

    IPC分类号： C07D401/06

    CPC分类号： C07D211/74 ,  C07D401/06 ,  C07D401/14

    摘要： The present invention discloses a novel process to prepare ketone amides, which are useful intermediates for the preparation of antagonists of CCR5 receptor and therefore useful for the treatment of HIV virus infected mammals. It specifically discloses a novel process to synthesize 1 -(2,4-dimethylpyrimidine-5-carbonyl)-4-piperidone, 1 -[(2,4-dimethyl-3- pyridinyl)carbonyl]-4-piperidone and related compounds. A salient feature of the invention is the use of a three-phase reaction medium with an organic phase and a buffer salt slurry. (formule I)

    摘要翻译： 本发明公开了一种制备酮酰胺的新方法，它是用于制备CCR5受体拮抗剂并因此可用于治疗HIV病毒感染的哺乳动物的有用中间体。 它具体公开了合成1-（2,4-二甲基嘧啶-5-羰基）-4-哌啶酮，1 - [（2,4-二甲基-3-吡啶基）羰基] -4-哌啶酮和相关化合物的新方法。 本发明的显着特征是使用具有有机相和缓冲盐浆液的三相反应介质。 （Formule I）

    PROCESS AND INTERMEDIATES FOR THE SYNTHESIS OF (3-ALKYL-5-PIPERIDIN-1-YL-3,3A-DIHYDRO- PYRAZOLOÝ1,5-A¨PYRIMIDIN-7-YL)-AMINO DERIVATIVES AND INTERMEDIATES
    8.
    发明公开
    PROCESS AND INTERMEDIATES FOR THE SYNTHESIS OF (3-ALKYL-5-PIPERIDIN-1-YL-3,3A-DIHYDRO- PYRAZOLOÝ1,5-A¨PYRIMIDIN-7-YL)-AMINO DERIVATIVES AND INTERMEDIATES 有权
    VERFAHREN UND ZWISCHENPRODUKTE ZUR HERSTELLUNG VON（3-ALKYL-5-PIPERIDIN-1-YL-3,3A-二氢吡唑并[1,5-A]吡啶基-7-YL） - 氨基衍生物

    公开(公告)号：EP2057166A2

    公开(公告)日：2009-05-13

    申请号：EP07837015.2

    申请日：2007-08-17

    申请人： Schering Corporation

    发明人： CHEN, Frank Xing ,  KEERTIKAR, Kartik M. ,  KUO, Shen-Chun ,  LEE, Hong-Chang ,  RAGHAVAN, Ramani R. ,  WU, George G. ,  XIE, Ji

    IPC分类号： C07D487/04

    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： 公开了一种合成式I化合物的方法，首先用伯胺，然后与仲胺，式E1结构的中间体化合物，其中R 1是直链，支链或环状烷氧基官能团 （-R2a-OH）基团，R2a是直链，支链或环状的烷基，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 选自二甲基丙二酸二甲酯，单甲基丙二酸酰氯和丙二酰氯的试剂在具有足够质子亲和力的路易斯碱存在下从吡唑环上的1-位氮抽出质子。