发明名称 Process for the synthesis of agomelatine
摘要 Process for the industrial synthesis of the compound of formula (I);
申请公布号 USRE46218(E1) 申请公布日期 2016.11.29
申请号 US201514619284 申请日期 2015.02.11
申请人 LES LABORATOIRES SERVIER 发明人 Zard Samir;Sire Béatrice;Boumediene Mehdi
分类号 C07C231/06;C07C255/33;C07C231/02;C07C233/18;C07C253/30;C07C255/37;C07C255/40 主分类号 C07C231/06
代理机构 Hueschen and Sage 代理人 Hueschen and Sage
主权项 1. A process for the synthesis of a compound of formula (I): wherein allyl cyanide of formula (II): is reacted, in the presence of a free radical initiator, with a compound of formula (III): wherein Xa represents a group —S—C(S)—OR in which R represents a linear or branched (C1-C6)alkyl group, to yield the compound of formula (IV): wherein Xa is as defined hereinbefore, wherein this latter compound may be optionally isolated, before being subjected to a cyclisation reaction in the presence of a free radical initiator in order to form the compound of formula (V): which compound of formula (V) may also be optionally isolated, which compound of formula (V) is subjected to a reduction-dehydration reaction to yield the compound of formula (VI): which is then subjected to an aromatisation reaction to yield the compound of formula (VII): which is subjected to reduction using hydrogen in the presence of Raney nickel in a polar protic medium and to reaction with acetic anhydride to yield the compound of formula (I), which is isolated in the form of a solid.
地址 Suresnes FR
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