发明公开
- 专利标题: PROCEDE DE PREPARATION DE COMPOSES CHIMIQUES D'INTERET PAR SUBSTITUTION NUCLEOPHILE AROMATIQUE DE DERIVES D'ACIDES CARBOXYLIQUES AROMATIQUES PORTANT AU MOINS UN GROUPEMENT ELECTROATTRACTEUR
- 专利标题(英): Method for preparing chemical compounds of interest by nucleophilic aromatic substitution of aromatic carboxylic acid derivatives supporting at least one electro-attractive group
- 专利标题(中): 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
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申请号: EP11712606.0申请日: 2011-02-18
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公开(公告)号: EP2536682A1公开(公告)日: 2012-12-26
- 发明人: MORTIER, Jacques , CASTANET, Anne-Sophie , NOURRY, Arnaud , BELAUD-ROTUREAU, Mickael
- 申请人: Centre National de la Recherche Scientifique , Université du Maine
- 申请人地址: 3 rue Michel Ange 75016 Paris FR
- 专利权人: Centre National de la Recherche Scientifique,Université du Maine
- 当前专利权人: Centre National de la Recherche Scientifique,Université du Maine
- 当前专利权人地址: 3 rue Michel Ange 75016 Paris FR
- 代理机构: Icosa
- 优先权: PCT/FR2010/052674 20101210; FR1054645 20100611; FR1051226 20100219
- 国际公布: WO2011101604 20110825
- 主分类号: C07C51/353
- IPC分类号: C07C51/353 ; C07C227/08 ; C07D295/155 ; C07C229/56 ; C07C229/58 ; C07C229/64 ; C07C229/68
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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