首页> 外国专利> METHOD FOR PREPARING CHEMICAL COMPOUNDS OF INTEREST BY NUCLEOPHILIC AROMATIC SUBSTITUTION OF AROMATIC CARBOXYLIC ACID DERIVATIVES SUPPORTING AT LEAST ONE ELECTRO-ATTRACTIVE GROUP

METHOD FOR PREPARING CHEMICAL COMPOUNDS OF INTEREST BY NUCLEOPHILIC AROMATIC SUBSTITUTION OF AROMATIC CARBOXYLIC ACID DERIVATIVES SUPPORTING AT LEAST ONE ELECTRO-ATTRACTIVE GROUP

机译:支撑至少一个电吸引基的芳族羧酸衍生物的亲核芳族取代基制备兴趣化合物的方法

摘要

The present invention relates to a method for preparing aromatic carboxylic acid derivatives by nucleophilic aromatic substitution, which involves reacting an aromatic carboxylic acid derivative supporting only one carboxyl function, or one of the salts thereof, said carboxylic acid derivative supporting, orthogonally to the carboxyl function, a splitting group which is an atom of fluorine or chlorine or an alcoxy group, chiral or otherwise and, in the latter case, a methoxy group is preferred; said carboxylic acid derivative being substituted by at least one electro-attractive group other than the splitting group, preferably by a fluorine atom, with a MNu reagent, wherein M is a metal and Nu is an optionally chiral nucleophile, said nucleophilic aromatic substitution reaction being carried out without a catalyst and without a step of protecting/unprotecting the acid function of the initial compound, said method being selective in that the reaction leads to the formation of ketone derivatives in a very minority fashion during the reaction.
机译:本发明涉及通过亲核芳族取代制备芳族羧酸衍生物的方法,该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反应,所述羧酸衍生物垂直于羧基官能团进行支持。 ,作为氟或氯或烷氧基的原子的拆分基,手性或其它,在后一种情况下,优选甲氧基;所述羧酸衍生物被MNu试剂所取代,所述羧酸衍生物被除分裂基团以外的至少一个电吸引基团取代,优选被氟原子取代,其中M是金属且Nu是任选的手性亲核试剂,所述亲核芳族取代反应是在没有催化剂且没有保护/未保护起始化合物的酸官能的步骤的条件下进行,所述方法是选择性的,因为该反应导致在反应期间以非常少的方式形成酮衍生物。

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