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Synthesis of N‑Substituted 3‑Amino-2-pyridones

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posted on 2022-08-12, 18:20 authored by Philippe 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.

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