RP-64406-药物合成数据库

【药物名称】RP-64406

化学结构式(Chemical Structure):

参考文献No.	545788
标题:	Riluzole series. Synthesis and in vivo "antiglutamate" activity of 6-substituted-2-benzothiazolamines and 3-substituted-2-imino-benzothiazolines
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.
来源:	J Med Chem 1999,42(15),2828

合成路线图解说明: 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.

合成路线图解说明: 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.