Synthesis of N-Substituted 3-Amino-2-pyridones
Philippe N. Bolduc, Magnus Pfaffenbach, Vanna D. Blasczak, Steven R. Mathieu, Emily A. Peterson
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.
Topics & Concepts
Chemistry2-PyridoneCombinatorial chemistryAmine gas treatingPrimary (astronomy)Nitrogen atomOrganic synthesisDrug discoveryNitrogenOrganic chemistryRing (chemistry)CatalysisBiochemistryPhysicsAstronomySynthesis of heterocyclic compoundsSynthesis and Reactivity of HeterocyclesSynthesis and biological activity