SAL-V-11

Chemical Name: 4-(3,4-Dichlorophenyl)-1-methylpiperidine-4-carboxylic acid ethyl ester hydrochloride
CAS No. 258500-91-3 (free base)
项目整合开发状态: Biological Testing
项目研究机构: National Institute on Drug Abuse (Originator)
合成路线:Dialkylation of 2-aryl acetonitrile (I) with bromoacetaldehyde dimethyl acetal (II) by means of NaNH2 in toluene provides diacetal (III),which is cyclized to cyanopiperidine derivative (IV) by first hydrolysis of the acetal groups with HCl,followed by reductive amination with methylamine in the presence of NaBH3CN in MeOH.Finally,the target product is obtained by hydrolysis of the nitrile group of (IV) with aqueous H2SO4,followed by esterification performed by heating with EtOH.
📌 参考资料/链接:
参考文献标题:Synthesis,dopamine and serotonin transporter binding affinities of novel analogues of meperidine
文献作者:Lomenzo,S.A.; Izenwasser,S.; Gerdes,R.M.; katz,J.L.; Kopajtic,T.; Trudell,M.L.
参考来源:Bioorg Med Chem Lett 1999,9(23),3273