Sibutramine hydrochloride monohydrate, KES-524, BTS-54524, Meridia, Reductil
盐酸西布曲明西布曲明Chemical Name: (?-N-[1-[1-(4-Chlorophenyl)cyclobutyl]-3-methylbutyl]-N,N-dimethylamine hydrochloride monohydrate
CAS No. 84485-00-7 (anhydrous, non-specified stereoch.), 106650-56-0 (free base, anhydrous)
项目整合开发状态: Launched-1998
项目研究机构: Abbott (Originator), Eisai (Licensee)
合成路线:4-Chlorobenzyl cyanide (I) is cycloalkylated with 1,3-dibromopropane to yield 1-(4-chlorophenyl)cyclobutyl cyanide (II).The cyclobutyl cyanide (II) is treated with 2-methylpropyl magnesium bromide te give the imine salt (III),which may be either hydrolyzed to the ketone (IV),which is then formylaminated with formamide and formic acid and subsequently hydrolyzed,or reduced with sodium borohydride in ethanol to give 1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutylamine (V).Eschweiler-Clarke methylation and hydrochloride formation yield N-[1-[1-(4-chlorophenyl)cyclo butyl]-3-methylbutyl]-N,N-dimethylamine hydrochloride monohydrate
📌 参考资料/链接：
参考文献标题:Substd.cyclobutanes,process for their preparatio
文献作者:Jeffery,J.E.; Kozlik,A.; Wilmshurst,E.C.(The Boots Company plc)
参考来源:DE 3212682; GB 2098602; US 4806570
📄 详细内容
合成路线:4-Chlorobenzyl cyanide (I) is cycloalkylated with 1,3-dibromopropane to yield 1-(4-chlorophenyl)cyclobutyl cyanide (II).The cyclobutyl cyanide (II) is treated with 2-methylpropyl magnesium bromide te give the imine salt (III),which may be either hydrolyzed to the ketone (IV),which is then formylaminated with formamide and formic acid and subsequently hydrolyzed,or reduced with sodium borohydride in ethanol to give 1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutylamine (V).Eschweiler-Clarke methylation and hydrochloride formation yield N-[1-[1-(4-chlorophenyl)cyclo butyl]-3-methylbutyl]-N,N-dimethylamine hydrochloride monohydrate
参考文献标题:N,N-Dimethyl-1-[1-(4-chlorophenyl)cyclobutyl]-3-me
文献作者:Jeffery,J.E.(The Boots Company plc)
参考来源:GB 2184122; US 4929629
合成路线:4-Chlorobenzyl cyanide (I) is cycloalkylated with 1,3-dibromopropane to yield 1-(4-chlorophenyl)cyclobutyl cyanide (II).The cyclobutyl cyanide (II) is treated with 2-methylpropyl magnesium bromide te give the imine salt (III),which may be either hydrolyzed to the ketone (IV),which is then formylaminated with formamide and formic acid and subsequently hydrolyzed,or reduced with sodium borohydride in ethanol to give 1-[1-(4-chlorophenyl)cyclobutyl]-3-methylbutylamine (V).Eschweiler-Clarke methylation and hydrochloride formation yield N-[1-[1-(4-chlorophenyl)cyclo butyl]-3-methylbutyl]-N,N-dimethylamine hydrochloride monohydrate
参考文献标题:SIBUTRAMINE HYDROCHLORIDE < Rec INN; BAN >
文献作者:Buckett,W.R.; Harris,P.J.
参考来源:Drugs Fut 1988,13(8),736
产品链接: CAS No. 84485-00-7›› 产品链接: CAS No.106650-56-0››