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:本发明涉及一种通过核亲芳基取代制备芳族羧酸衍生物的方法,该方法涉及仅由一个羧基官能团,或盐的一个或多个盐支持一个羧基的芳族羧酸衍生物。分裂基团,它是氟或氯原子或手性或其他形式的羟基的原子团,在以后的情况下,优选甲氧基。所说的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,最好是由氟原子与MNU试剂取代,其中M是金属,NU是可选的手性核苷,类似核苷在没有催化剂和没有保护/不保护初始化合物的酸的步骤的情况下进行,所述方法是选择性的,因为该反应在反应过程中导致酮类衍生物的形成是非常少见的。

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