Synthesis ( IF 2.2 ) Pub Date : 2017-08-23 , DOI: 10.1055/s-0036-1588523 Mario Ellwart 1 , Georg Höfner 1 , Aaron Gerwien 1 , Klaus Wanner 1 , Paul Knochel 1
Abstract
A range of N-benzylic and N-phenethylic ephedrine derivatives were prepared in a one-pot procedure starting from the two enantiomers of ephedrine using the Potier reagent, and a polyfunctional aryl- or benzylic organozinc halide. The biological activity in indatraline MS Binding Assays addressing hDAT, hNET and hSERT was determined and discussed.
A range of N-benzylic and N-phenethylic ephedrine derivatives were prepared in a one-pot procedure starting from the two enantiomers of ephedrine using the Potier reagent, and a polyfunctional aryl- or benzylic organozinc halide. The biological activity in indatraline MS Binding Assays addressing hDAT, hNET and hSERT was determined and discussed.
中文翻译:
新型N-苄基和N-苯乙基麻黄碱衍生物的合成及生物活性
摘要
使用Potier试剂从麻黄碱的两种对映体开始,通过一锅法制备一系列N-苄基和N-苯乙基麻黄碱衍生物,以及多官能芳基或苄基有机锌卤化物。确定并讨论了indatraline MS结合测定法中针对hDAT,hNET和hSERT的生物活性。
使用Potier试剂从麻黄碱的两种对映体开始,通过一锅法制备一系列N-苄基和N-苯乙基麻黄碱衍生物,以及多官能芳基或苄基有机锌卤化物。确定并讨论了indatraline MS结合测定法中针对hDAT,hNET和hSERT的生物活性。