[EN] METHOD OF SYNTHESIS OF FERROQUINE BY CONVERGENT REDUCTIVE AMINATION<br/>[FR] PROCÉDÉ DE SYNTHÈSE DE FERROQUINE PAR AMINATION RÉDUCTRICE CONVERGENTE
申请人:SANOFI SA
公开号:WO2011154923A1
公开(公告)日:2011-12-15
The invention relates to a method of synthesis of ferroquine of formula (F) or of its metabolite of formula (Fm): comprising a reaction of reductive amination, said reaction comprising: (i) a stage of condensation of the aldhehyde-amino ferrocene of formula (1 ), which R represents a hydrogen atom or a methyl group, with the 7-chloroquinolin- amine of formula (2) as shown below, followed by (ii) a stage of reduction of the product of condensation obtained in the preceding stage (iii) then a stage of hydrolysis of the reaction mixture in the presence of an aqueous solution of ammonia or of citric acid.
本发明涉及合成Ferroquine的方法,其化学式为(F),或其代谢产物的化学式为(Fm),包括还原胺反应,该反应包括:(i)将化学式为(1)的醛氨基二茂铁(其中R代表氢原子或甲基基团)与化学式为(2)的7-氯喹啉胺缩合,然后(ii)还原得到的缩合产物,(iii)最后在氨水或柠檬酸水溶液存在下进行反应混合物的水解。