posted on 2022-08-12, 18:20authored byPhilippe N. Bolduc, Magnus Pfaffenbach, Vanna D. Blasczak, Steven R. Mathieu, Emily A. Peterson
Pyridones are versatile building blocks in organic synthesis
and
a privileged motif in drug discovery. However, N-substituted 2-pyridones
bearing an α-tertiary carbon, cyclopropyl, or heterocycle off
of the pyridone nitrogen atom remain challenging to prepare. Herein,
we describe the efficient synthesis of a large variety of N-substituted
2-pyridones from ethyl nitroacetate and readily available primary
amine building blocks, which can be utilized on a large scale and
in parallel medicinal chemistry applications.