Me3SiCl-promoted intramolecular cyclization of aromatic compounds tethered with N,O-acetals leading to the facile preparation of 1,4-benzodiazepine skeletons
作者:Norio Sakai、Akimasa Watanabe、Reiko Ikeda、Yumi Nakaike、Takeo Konakahara
DOI:10.1016/j.tet.2010.09.077
日期:2010.11
synthesis from N-alkylaniline derivatives and N-alkyl-2-oxazolidinones that leads to the production of pharmaceutically useful 1,4-benzodiazepine skeletons with a variety of functional groups is described. This method was successfully applied to the facile preparation of both tricyclic benzodiazepine derivatives and a 1,4-benzoxazepine derivative via 7-exo-trig cyclization.
Me 3 SiCl促进的新型N,O-乙缩醛的分子内氨甲基化反应,是由N-烷基苯胺衍生物和N-烷基-2-恶唑烷酮通过容易的三步合成法制备的,可生产药学上有用的物质描述了具有各种官能团的1,4-苯并二氮杂skeleton骨架。此方法经7-成功地应用于两个三环苯并二氮杂衍生物的制备容易和1,4-苯并氧氮杂衍生物外切- trig的环化。