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

被引：7

作者：

Bolduc, Philippe N. ^{[1
]}

Pfaffenbach, Magnus ^{[1
]}

Blasczak, Vanna D. ^{[1
]}

Mathieu, Steven R. ^{[1
]}

Peterson, Emily A. ^{[1
]}

机构：

[1] Biogen, Cambridge, MA 02142 USA

来源：

ORGANIC LETTERS | 2022年 / 24卷 / 33期

关键词：

2-PYRIDONES; REGIO;

D O I：

10.1021/acs.orglett.2c02189

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Pyridones are versatile building blocks in organic synthesis and a privileged motif in drug discovery. However, N substituted 2-pyridones bearing an alpha-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.

引用

页码：6133 / 6136

页数：4

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