Polysubstituted Pyridines from 1,4-Oxazinone Precursors

J Org Chem. 2024 Nov 12. doi: 10.1021/acs.joc.4c02389. Online ahead of print.

Abstract

This study describes a general method for the preparation of 1,4-oxazin-2-one intermediates from acetylene dicarboxylate and β-amino alcohol precursors. Oxazinones prepared in this manner were employed in a tandem cycloaddition/cycloreversion reaction sequence with a model alkyne (phenyl acetylene) to give substituted pyridine products. Fundamental reactivity and selectivity studies are complemented by the synthesis of the polycyclic ergot alkaloid natural product xylanigripone A.