发明公开
EP2536682A1 PROCEDE DE PREPARATION DE COMPOSES CHIMIQUES D'INTERET PAR SUBSTITUTION NUCLEOPHILE AROMATIQUE DE DERIVES D'ACIDES CARBOXYLIQUES AROMATIQUES PORTANT AU MOINS UN GROUPEMENT ELECTROATTRACTEUR 审中-公开
程序对某些化合物进行亲核芳香取代,至少有一个电子吸引基团芳香族羧酸衍生物的制备

PROCEDE DE PREPARATION DE COMPOSES CHIMIQUES D'INTERET PAR SUBSTITUTION NUCLEOPHILE AROMATIQUE DE DERIVES D'ACIDES CARBOXYLIQUES AROMATIQUES PORTANT AU MOINS UN GROUPEMENT ELECTROATTRACTEUR
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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