Friedel–Crafts Chemistry. Part 39. Unprecedented Facile Route to the Synthesis of Benzo[b][1]benzazepines via Intramolecular Friedel–Crafts Cyclialkylations
作者:Hassan A. K. Abd El-Aal、Ali A. Khalaf
DOI:10.1071/ch12548
日期:——
were cleanly prepared by Friedel–Crafts cyclialkylations of nitrogen-containing alkanols in the presence of AlCl3, 85 % H2SO4 or polyphosphoric acid catalysts. The precursor alkanols (13a–f) were readily prepared by reaction of two synthesized carboxylic acid esters (12a, b) with different Grignard reagents. Also, two dibenzo[b,f]azepinones (15a, b) were prepared by Friedel–Crafts cycliacylation and reduced
一系列六个药学有为5,6-二氢11 ħ -苯并[ b ] [1]苯并吖庚因衍生物(1C - ħ)被干净地由含氮链烷醇的弗瑞德-克莱福特cyclialkylations制备的AlCl存在3,85 %H 2 SO 4或多磷酸催化剂。通过两种合成的羧酸酯(12a,b)与不同的格氏试剂的反应,可以轻松制备前体烷醇(13a – f)。另外,有两个二苯并[ b,f ] ze庚酮(15a,b)由Friedel-Crafts环酰化制备,并还原为相应的5,6-二氢-11 H-苯并[ b ] [1]苯并ze庚因(1a,b)。总的来说,该方法允许容易地和有效地从容易合成的链烷醇或环酮获得聚三环胺。提出了一种合理的碳正离子化机制来解释结果。