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 US8853449(B2) 申请公布日期 2014.10.07
申请号 US201213977799 申请日期 2012.01.04
申请人 Les Laboratoires Servier 发明人 Zard Samir;Sire Béatrice;Boumediene Mehdi
分类号 C07C231/06;C07C255/33;C07C231/02;C07C255/40;C07C255/37;C07C253/30;C07C233/18 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 Cedex FR
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