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Updated: Sep 1, 2025

Syntheses, Crystallization, and Spectroscopic Characterization of 3,5-Lutidine N-Oxide Dehydrate
Published on: April 24, 2018
Synthesis of N-Substituted 3-Amino-2-pyridones
Philippe N Bolduc1, Magnus Pfaffenbach1, Vanna D Blasczak1
1Biogen, 225 Binney Street, Cambridge, Massachusetts 02142, United States.
Abstract:
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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