发明名称 NEW PROCESS FOR THE SYNTHESIS OF (7-METHOXY-1-NAPHTHYL)ACETONITRILE AND APPLICATION IN THE SYNTHESIS OF AGOMELATINE
摘要 Disclosed herein is a process for the industrial synthesis of the compound of 7-methoxy-1-naphthyl)acetonitrile (compound of formula I), characterised in that 7-methoxy1-1naphthoic acid of formula (III) is used for the reaction which is further subjected to the action of a reducing agent to yield the compound 7-methoxy-1-naphthyl)methanol (formula (IV)), wherein the OH function of the compound of formula (IV) is converted into a leaving group and which is reacted with a cyanation reagent to yield the compound of formula (I), which is isolated in the form of a solid. Also disclosed is a process for the synthesis of agomelatine (compound of formula (II))starting from the compound of formula (I), characterised in that the compound of formula(I) is obtained by the synthesis process described above and is subjected to reduction and then to coupling with acetic anhydride.
申请公布号 NZ583064(A) 申请公布日期 2011.07.29
申请号 NZ20080583064 申请日期 2008.08.01
申请人 LES LABORATOIRES SERVIER 发明人 HERMET, JEAN-PAUL;DUBUFFET, THIERRY;LECOUVE, JEAN-PIERRE
分类号 C07C231/02;C07C233/18;C07C253/14;C07C255/37 主分类号 C07C231/02
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