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    PROCESS FOR PREPARING CHEMICAL COMPOUNDS OF INTEREST BY NUCLEOPHILIC AROMATIC SUBSTITUTION OF AROMATIC CARBOXYLIC ACID DERIVATIVES SUPPORTING AT LEAST ONE ELECTRO-ATTRACTIVE GROUP
    2.
    发明申请
    PROCESS FOR PREPARING CHEMICAL COMPOUNDS OF INTEREST BY NUCLEOPHILIC AROMATIC SUBSTITUTION OF AROMATIC CARBOXYLIC ACID DERIVATIVES SUPPORTING AT LEAST ONE ELECTRO-ATTRACTIVE GROUP 审中-公开
    制备化学化合物的方法，由支持至少一个电吸引剂组的芳香羧酸衍生物的核化学取代芳族取代基

    公开(公告)号：US20120330056A1

    公开(公告)日：2012-12-27

    申请号：US13578973

    申请日：2011-02-18

    申请人： Jacques Mortier ,  Anne-Sophie Castanet ,  Arnaud Nourry ,  Mickael Belaud-Rotureau

    发明人： Jacques Mortier ,  Anne-Sophie Castanet ,  Arnaud Nourry ,  Mickael Belaud-Rotureau

    IPC分类号： C07C51/347 ,  C07C227/06 ,  C07C51/367

    CPC分类号： C07B37/04 ,  C07B43/04 ,  C07C51/353 ,  C07C227/08 ,  C07C63/04 ,  C07C63/70 ,  C07C63/331 ,  C07C229/56 ,  C07C229/58 ,  C07C63/72

    摘要： A method for preparing aromatic carboxylic acid derivatives by nucleophilic aromatic substitution, involves reacting an aromatic carboxylic acid derivative supporting only one carboxyl function, or one of the salts thereof, the carboxylic acid derivative supporting, orthogonally to the carboxyl function, a leaving group which is a fluorine or chlorine atom or an alkoxy group, chiral or otherwise and, in the latter case, preferably a methoxy group; the carboxylic acid derivative being substituted by at least one electro-attractive group other than the leaving group, preferably by a fluorine atom, with a MNu reagent, wherein M is a metal and Nu an optionally chiral nucleophile, the nucleophilic aromatic substitution reaction being carried out without a catalyst and without a step of protecting/unprotecting the acid function of the initial compound, the method being selective in that the reaction leads to the formation of ketone derivatives in a very minority fashion during the reaction.

    摘要翻译： 通过亲核芳族取代制备芳族羧酸衍生物的方法包括使仅支持一个羧基官能团的芳族羧酸衍生物或其盐之一，与羧基官能团正交地支持的羧酸衍生物， 氟或氯原子或烷氧基，手性或其它，在后一种情况下优选为甲氧基; 所述羧酸衍生物被除了离开基团以外的至少一个电吸引基团，优选氟原子被MNu试剂取代，其中M是金属，Nu是任选手性亲核试剂，携带亲核芳族取代反应 在没有催化剂的情况下，没有保护/不保护初始化合物的酸功能的步骤，该方法是选择性的，因为反应导致在反应期间以非常少数形式形成酮衍生物。