Process for preparing N-substituted 1H-pyrazole-5-carboxylate compounds and derivatives thereof
    38.
    发明授权
    Process for preparing N-substituted 1H-pyrazole-5-carboxylate compounds and derivatives thereof 有权
    制备N-取代的1H-吡唑-5-羧酸酯化合物及其衍生物的方法

    公开(公告)号:US09556141B2

    公开(公告)日:2017-01-31

    申请号:US14359446

    申请日:2012-11-20

    Applicant: BASF SE

    CPC classification number: C07D401/04 C07D471/10

    Abstract: The present invention relates to a process for preparing an N-substituted 1H-pyrazole-5-carboxylate compound of the formula (I-A) comprising the steps of i) deprotonating a compound of the formula (II) in which the variables R1, R2 and r are each as defined in the description and the claims, with a magnesium-organic base having a carbon bound magnesium; and ii) subjecting the product obtained in step (i) to a carbonylation by reacting it with a reagent selected from the group consisting carbon dioxide or a carbon dioxide equivalent, to obtain a compound of formula (I-A); and it relates to further conversions to yield a N-substituted 1H-pyrazole-5-carbonyl chloride compound of the formula (I)

    Abstract translation: 本发明涉及制备式(IA)的N-取代的1H-吡唑-5-羧酸酯化合物的方法,包括以下步骤:i)将式(II)的化合物去质子化,其中变量R1,R2和 r各自如说明书和权利要求中所定义,其中镁 - 有机碱具有碳结合的镁; 和ii)通过使步骤(i)中获得的产物与选自二氧化碳或二氧化碳当量的试剂反应来进行羰基化,得到式(I-A)化合物; 并且涉及进一步转化得到式(I)的N-取代的1H-吡唑-5-碳酰氯化合物,

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