Setastine hydrochloride, EGYT-2062, EGIS-2062, Loderix
盐酸司他斯汀 司他斯汀 Chemical Name: 1-[2-[1-(4-Chlorophenyl)-1-phenylethoxy]ethyl]hexahydro-1H-azepine hydrochloride
CAS No. 59767-13-4, 64294-95-7 (free base)
项目整合开发状态: Launched-1987
项目研究机构: Egis (Originator)
合成路线:4-Chloro-alpha-methylbenzhydrol (I) is alkylated with N-(2-chloroethyl)hexamethyleneimine (II) in benzene in the presence of sodium amide to give setastine.The starting products are obtained as follows; Caprolactame (III) is O-alkylated with dimethyl sulfate to yield the lactimether (IV),which is reduced with sodium borohydride to hexamethyleneimine (II).Friedel Cratts acylation of chlorobenzene (V) with benzoyl chloride (VI) affords the benzophenone (VII),to which methylmagnesium bromide is added to give the carbinol (I).
📌 参考资料/链接：
参考文献标题:New benzhydryloxy-alkylamine derivs.and process f
文献作者:Rakoczi,J.; Bolla,K.; Beck,I.; Porszasz,K.(Egis Pharmaceuticals Ltd.)
参考来源:DE 2528194; GB 1463038
📄 详细内容
合成路线:4-Chloro-alpha-methylbenzhydrol (I) is alkylated with N-(2-chloroethyl)hexamethyleneimine (II) in benzene in the presence of sodium amide to give setastine.The starting products are obtained as follows; Caprolactame (III) is O-alkylated with dimethyl sulfate to yield the lactimether (IV),which is reduced with sodium borohydride to hexamethyleneimine (II).Friedel Cratts acylation of chlorobenzene (V) with benzoyl chloride (VI) affords the benzophenone (VII),to which methylmagnesium bromide is added to give the carbinol (I).
参考文献标题:Setastine hydrochloride
文献作者:Nogradi,M.
参考来源:Drugs Fut 1987,12(4),357
产品链接: CAS No. 59767-13-4›› 产品链接: CAS No.64294-95-7››