An environmentally benign multi-component reaction: regioselective synthesis of fluorinated 2-aminopyridines using diverse properties of the nitro group
By: Xuan-Xuan Du, Quan-Xing Zi, Yu-Meng Wu, Yi Jin, Jun Lin and Sheng-Jiao Yan
Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming, P. R. China
Green Chemistry
Published Online
Abstract
An efficient and concise one-pot procedure was developed for the synthesis of two kinds of fluorinated 2-aminopyridine compounds, 4 and 5, based on the reactions of different types of 1,1-enediamines(EDAMs), 1, with a variety of benzaldehyde derivatives, 2, and 1,3-dicarbonyl compounds, 3, involving the Knoevenagel, Michael and cyclization reactions under heating. This protocol is especially suitable for efficient and rapid parallel synthesis of fluorinated 2-aminopyridine compounds with pharmacological activity. The usefulness of this environmentally benign, mild, and multicomponent one-pot reaction procedure was demonstrated by easily synthesizing two kinds of fluorinated 2-aminopyridine libraries.
全文链接：https://pubs.rsc.org/en/Content/ArticleLanding/2019/GC/C8GC03698E#!divAbstract
