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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
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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
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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.
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