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项目整合精选>>>Bupropion hydrochloride, Amfebutamone hydrochloride, BW-323U66(free base), Wellbutrin XL, Quomem, Zyban, Wellbutrin, Wellbatrin
Bupropion hydrochloride, Amfebutamone hydrochloride, BW-323U66(free base), Wellbutrin XL, Quomem, Zyban, Wellbutrin, Wellbatrin
盐酸安非他酮 安非他酮 Chemical Name: (?-1-(3-Chlorophenyl)-2-(tert-butylamino)propan-1-one hydrochloride
CAS No. 31677-93-7, 34911-55-2 (free base)
项目整合开发状态: Launched-1989
项目研究机构: GlaxoSmithKline (Originator), National Institute on Drug Abuse (Not Determined), Biovail (Licensee), Esteve (Licensee), Watson (Generic)
合成路线:By reaction of alpha,m-(dichloropropiophenone (I) with tert-butylamine (B) in refluxing acetonitrile or by reaction of alpha-bromo-m-chloropropiophenone (VI) with tert-butylamine (B) in acetonitrile at room temperature.The starting product (I) can be obtained in two different ways:1) The Grignard condensation of m-chlorobenzonitrile (II) with ethyl magnesium bromide (A) in refluxing ether gives m-chloropropiophenone (III),which is then treated with SO2Cl2 in tetrachloroethane.2) The reaction of propiophenone (IV) with SO2Cl2 in tetrachloroethane gives alpha-chloropropiophenone (V),which is then chlorinated in the ring by means of SO2Cl2 and AlCl3 in tetrachloroethane.The starting product (VI) is obtained by bromination of m-chloropropiophenone (III) with Br2 in methylene chloride
📌 参考资料/链接：
参考文献标题:Bupropion
文献作者:Hopkins,S.J.; Castar,J.
参考来源:Drugs Fut 1978,3(10),723
📄 详细内容
合成路线:By reaction of alpha,m-(dichloropropiophenone (I) with tert-butylamine (B) in refluxing acetonitrile or by reaction of alpha-bromo-m-chloropropiophenone (VI) with tert-butylamine (B) in acetonitrile at room temperature.The starting product (I) can be obtained in two different ways:1) The Grignard condensation of m-chlorobenzonitrile (II) with ethyl magnesium bromide (A) in refluxing ether gives m-chloropropiophenone (III),which is then treated with SO2Cl2 in tetrachloroethane.2) The reaction of propiophenone (IV) with SO2Cl2 in tetrachloroethane gives alpha-chloropropiophenone (V),which is then chlorinated in the ring by means of SO2Cl2 and AlCl3 in tetrachloroethane.The starting product (VI) is obtained by bromination of m-chloropropiophenone (III) with Br2 in methylene chloride
参考文献标题:Intermediates for biologically active ketones
文献作者:Mehta,N.B.; Yeowell,D.A.
参考来源:CA 977778
合成路线:By reaction of alpha,m-(dichloropropiophenone (I) with tert-butylamine (B) in refluxing acetonitrile or by reaction of alpha-bromo-m-chloropropiophenone (VI) with tert-butylamine (B) in acetonitrile at room temperature.The starting product (I) can be obtained in two different ways:1) The Grignard condensation of m-chlorobenzonitrile (II) with ethyl magnesium bromide (A) in refluxing ether gives m-chloropropiophenone (III),which is then treated with SO2Cl2 in tetrachloroethane.2) The reaction of propiophenone (IV) with SO2Cl2 in tetrachloroethane gives alpha-chloropropiophenone (V),which is then chlorinated in the ring by means of SO2Cl2 and AlCl3 in tetrachloroethane.The starting product (VI) is obtained by bromination of m-chloropropiophenone (III) with Br2 in methylene chloride
参考文献标题:Amino-propioph閚ones et m閐icaments contenant ces substances
文献作者:Mehta,N.B.; Yeowell,D.A.
参考来源:DE 2059618; DE 2064934; FR 2081326; US 3819706
产品链接: CAS No. 31677-93-7›› 产品链接: CAS No.34911-55-2››