Improved methodologies for the preparation of highly substituted pyridines.
[reaction: see text] Two separate strategies have been developed for the preparation of highly substituted pyridines from 1,2,4-triazines via the inverse-electron-demand Diels-Alder reaction: a microwave-promoted, solvent-free procedure and a tethered imine-enamine (TIE) approach. Both routes avoid the need for a discrete aromatization step and offer significant advantages over the classical methods, giving a wide variety of tri-, tetra-, and penta-substituted pyridines in high, optimized yields.
Fernández Sainz
Yolanda
Y
Department of Chemistry, University of York, Heslington, York YO10 5DD, UK.
Raw
Steven A
SA
Taylor
Richard J K
RJ
D015394:Molecular Structure; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry; D013237:Stereoisomerism
D011725:Pyridines