新产品编号:1014571
Chemical Name: 3-[2-(Methylthio)ethyl]-6-(trifluoromethoxy)benzothiazolin-2-imine
项目整合开发状态: Preclinical
项目研究机构: Aventis Pharma (Originator)
合成路线:Treatment of 4-(trifluoromethoxy)aniline (I) with thiocyanogen,generated from KSCN and Br2 in cold AcOH,afforded riluzole (II).Regioselective alkylation of (II) with 2-(methylthio)ethyl chloride (III) in refluxing methyl ethyl ketone then gave the title compound.
合成路线:Treatment of 4-(trifluoromethoxy)aniline (I) with thiocyanogen,generated from KSCN and Br2 in cold AcOH,afforded riluzole (II).Regioselective alkylation of (II) with 2-(methylthio)ethyl chloride (III) in refluxing methyl ethyl ketone then gave compound (IV),which was finally oxidized to the title sulfoxide by means of m-chloroperbenzoic acid.
📌 参考资料/链接：
参考文献标题:Riluzole series.Synthesis and in vivo "antiglutamate" activity of 6-substituted-2-benzothiazolamines and 3-substituted-2-imino-benzothiazolines
文献作者:Jimonet,P.; Audiau,F.; Barreau,M.; Blanchard,J.C.; Boireau,A.; Bour,Y.; Coleno,M.A.; Doble,A.; Doerflinger,G.; Huu,C.D.; Donat,M.H.; Duchesne,J.M.; Ganil,P.; Gueremy,C.; Honor,E.; Just,B.; Kerphirique,R.; Gontier,S.; et al.
参考来源:J Med Chem 1999,42(15),2828