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    PROCESS FOR PRODUCTION OF THIOPHENE COMPOUND AND INTERMEDIATE THEREOF
    3.
    发明公开
    PROCESS FOR PRODUCTION OF THIOPHENE COMPOUND AND INTERMEDIATE THEREOF 有权
    VERFAHREN ZUR HERSTELLUNG EINER THIOPHENVERBINDUNG UND ZWISCHENPRODUKTDAFÜR

    公开(公告)号：EP2246343A1

    公开(公告)日：2010-11-03

    申请号：EP09714127.9

    申请日：2009-02-27

    申请人： Nissan Chemical Industries, Ltd.

    发明人： YANAGIHARA, Kazufumi ,  UMEZAWA, Shingo ,  MIYAJI, Katsuaki

    IPC分类号： C07D333/32 ,  C07C319/18 ,  C07C323/56 ,  C07C327/32

    CPC分类号： C07D333/32 ,  C07C319/14 ,  C07C327/32 ,  C07C323/56

    摘要： To provide a novel process for producing a 2-aryl-3-hydroxy-4-substituted carbonyl thiophene compound or an intermediate thereof useful as an intermediate for production of medicines and agricultural chemicals.
    A 2-aryl acetate compound represented by the formula (1):

    wherein R 1 is an aryl group or the like, R 4 is a C 1-3 alkyl group or the like, and X is a leaving group, is reacted with a thioacetic acid compound to form a thioacetyl compound (3), the thioacetyl compound (3) is reacted with a vinyl ketone compound to form a γ-ketosulfide compound (5), which is cyclized under basic conditions to form a dihydrothiophene compound (6), and the dihydrothiophene compound (6) is oxidized by using an oxidizing agent to produce a 2-aryl-3-hydroxy-4-substituted carbonyl thiophene compound (7).

    摘要翻译： 提供一种制备2-芳基-3-羟基-4-取代的羰基噻吩化合物或其中间体的新方法，其用作制备药物和农药的中间体。 由式（1）表示的2-芳基乙酸酯化合物：其中R 1为芳基等，R 4为C 1-3烷基等，X为离去基团，与 硫代乙酰化合物形成硫代乙酰化合物（3），硫乙酰化合物（3）与乙烯基酮化合物反应形成3-酮硫醚化合物（5），在碱性条件下环化形成二氢噻吩化合物（6） ，通过使用氧化剂使二氢噻吩化合物（6）氧化，得到2-芳基-3-羟基-4-取代的羰基噻吩化合物（7）。