Etifoxin, Etifoxine, 36-801, Hoe-36-801
艾替伏辛Chemical Name: 6-Chloro-N-ethyl-4-methyl-4-phenyl-4H-3,1-benzoxazin-2-amine
CAS No. 21715-46-8
项目整合开发状态: Biological Testing
项目研究机构:
合成路线:This compound can be obtained by two related ways (1,2):1) The Grignard reaction of 2-amino-5-chlorobenzophenone (I) with methylmagnesium iodide in ether gives 2-amino-5-chloromethylbenzhydrol (II),which by reaction with ethyl isothiocyanate (III) in ether yields 2-(omega-ethylthioureido)-5-chloro-alpha-methylbenzhydrol (IV).Finally this compound is treated with mercuric oxide in refluxing ethanol.2) The reaction of (II) with ethyl isocyanate (V) in ether gives 2-(omega-ethylureido)-5-chloro-alpha-methylbenzhydrol (VI),which is finally cyclized by treatment with aqueous 48% HBr at 100 C.
📌 参考资料/链接：
参考文献标题:2-Ethylamino-6-chloro-4-methyl-4-phenyl-4H-3,1,benzoxazine,a new psychotropic compound
文献作者:Hoffman,I.; et al.
参考来源:Arzneim-Forsch Drug Res 1970,20(7),975
📄 详细内容
合成路线:This compound can be obtained by two related ways (1,2):1) The Grignard reaction of 2-amino-5-chlorobenzophenone (I) with methylmagnesium iodide in ether gives 2-amino-5-chloromethylbenzhydrol (II),which by reaction with ethyl isothiocyanate (III) in ether yields 2-(omega-ethylthioureido)-5-chloro-alpha-methylbenzhydrol (IV).Finally this compound is treated with mercuric oxide in refluxing ethanol.2) The reaction of (II) with ethyl isocyanate (V) in ether gives 2-(omega-ethylureido)-5-chloro-alpha-methylbenzhydrol (VI),which is finally cyclized by treatment with aqueous 48% HBr at 100 C.
参考文献标题:Etifoxine hydrochloride
文献作者:Blancafort,P.; Serradell,M.N.; Castar,J.; Neuman,M.
参考来源:Drugs Fut 1981,6(9),550
合成路线:This compound can be obtained by two related ways (1,2):1) The Grignard reaction of 2-amino-5-chlorobenzophenone (I) with methylmagnesium iodide in ether gives 2-amino-5-chloromethylbenzhydrol (II),which by reaction with ethyl isothiocyanate (III) in ether yields 2-(omega-ethylthioureido)-5-chloro-alpha-methylbenzhydrol (IV).Finally this compound is treated with mercuric oxide in refluxing ethanol.2) The reaction of (II) with ethyl isocyanate (V) in ether gives 2-(omega-ethylureido)-5-chloro-alpha-methylbenzhydrol (VI),which is finally cyclized by treatment with aqueous 48% HBr at 100 C.
参考文献标题:
文献作者:Kuch,H.; et al.(Farbwerke Hoechst A.G.)
参考来源:BE 707013; CA 870620; CH 502366; CH 522671; CH 532603; CH 532604; CH 534174; DE 1670772; FR 1571287; FR M7358; GB 1179856; GB 1197479; JP 7125385; JP 7126945; JP 7126946; JP 7126947; NL 6715652; US 3725404; ZA 6706887
产品链接: CAS No. 21715-46-8››