Multigram Synthesis of α‐ and γ‐((Hetera)cyclo)alkylpyridines through α‐Arylation of (Hetero)aliphatic Nitriles
作者:Dmytro I. Sierov、Illia V. Dzhulai、Kateryna I. Siryk、Kostiantyn V. Shvydenko、Tetiana I. Shvydenko、Kostiantyn Nazarenko、Aleksandr Kostyuk、Oleksandr S. Liashuk、Oleksandr O. Grygorenko
DOI:10.1002/ejoc.202300538
日期:2023.9.6
A systematic study on the SNAr arylation of nitrile and ester anions with 2- and 4-flurropyridine derivatives is described. In combination with hydrolysis and decarboxylation, the method provides an efficient approach to the multigram synthesis of functionalized pyridines decorated with alkyl, cycloalkyl, and saturated heterocyclic substituents at the α or γ positions – valuable building blocks for
(环)烷基吡啶:描述了用 2- 和 4- 氟吡啶衍生物对腈和酯阴离子进行S N Ar 芳基化的系统研究。结合水解和脱羧,该方法为多克合成在 α 或 γ 位上用烷基、环烷基和饱和杂环取代基修饰的官能化吡啶提供了一种有效的方法,这些取代基是药物化学的重要组成部分。