发明名称 Formation of Carbon-nitrogen bond
摘要 The present invention relates to a process to create a carbon-nitrogen bond by the reaction of an aromatic compound carrying at least one electro attractive group with one nitrogenous heterocyclic type nucleophile compound. The invention aims, in particular, at a link reaction between an aromatic compound carrying at least one electro attractive group and an imidazole heterocycle type. The invention process, consisting of the reaction of an aromatic compound carrying one leaving group and at least one electro attractive group and a nitrogenous heterocyclic type nucleophile compound comprising a N—H pattern likely to substitute the leaving group, thereby creating a carbon-nitrogen bond in the presence of a copper catalyst, of a base in an organic solvent, is characterized by the fact that the said nitrogenous heterocycle reacts with an aromatic type electrophile compound carrying one leaving group (Y) chosen from bromine, chlorine or sulfonic ester and at least one electro attractive group (Z1), in the presence of a copper catalyst, of a mineral or organic base, of an extracting agent selected from aliphatic diamines, aliphatic amino alcohols and diols in a polar aprotic organic solvent with a dielectric constant less than about 20 and a basicity such that its “donor number” is less than about 25.
申请公布号 US2010113800(A1) 申请公布日期 2010.05.06
申请号 US20060990012 申请日期 2006.08.04
申请人 SHASUN PHARMA SOLUTIONS LIMITED 发明人 MAUGER CHRISTELLE;MIGNANI GERARD;JACQUOT ROLAND
分类号 C07D233/00 主分类号 C07D233/00
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