Department of Chemistry, University of Calcutta, 92 APC Road, Kolkata-700009, India.
Org Lett. 2011 Sep 2;13(17):4664-7. doi: 10.1021/ol201877v. Epub 2011 Aug 1.
This is the first report of an innovative, one-pot, catalyst-free, pseudo-five-component synthesis of 1,2-dihydro[1,6]naphthyridines from methyl ketones, amines, and malononitrile in ecofriendly solvent water. The protocol avoids the use of expensive catalysts, toxic organic solvents and anhydrous condition. The approach to naphthyridines presented herein offers for the first time an unprecedented coupling which leads to the construction of both the nitrogen containing rings during the synthesis without starting from any nitrogen-containing heterocycle moiety.
这是首例在环保溶剂水中,由甲基酮、胺和丙二腈一锅、无催化剂、假五元合成 1,2-二氢[1,6]萘啶的创新报告。该方案避免了使用昂贵的催化剂、有毒有机溶剂和无水条件。本文提出的萘啶合成方法首次提供了一种前所未有的偶联,在合成过程中无需任何含氮杂环部分即可构建含氮环。