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简洁的克级规模合成带有用于化学选择性交叉偶联的功能手柄的呋喃并[2,3-]吡啶。

Concise, gram-scale synthesis of furo[2,3-]pyridines with functional handles for chemoselective cross-coupling.

作者信息

O'Byrne Sean N, Eduful Benjamin J, Willson Timothy M, Drewry David H

机构信息

Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.

出版信息

Tetrahedron Lett. 2020 Sep 17;61(38). doi: 10.1016/j.tetlet.2020.152353. Epub 2020 Aug 16.

Abstract

A concise 4-step synthesis of furo[2,3-]pyridines, with handles in the 3- and 5-positions for palladium mediated cross-coupling reactions, is described. The synthetic route has been optimized, with only one step requiring purification by column chromatography. The route is amenable to scale-up, and was successfully executed on a multi-gram scale. Furopyridines are of growing interest in medicinal chemistry, and this route should enable easy access to the core for structure-activity relationship (SAR) studies.

摘要

本文描述了一种简洁的4步合成呋喃并[2,3 -]吡啶的方法,该方法在3位和5位带有用于钯介导交叉偶联反应的官能团。合成路线已得到优化,仅一步需要通过柱色谱法进行纯化。该路线适合放大规模,并已成功在数克规模上实施。呋喃并吡啶在药物化学中的关注度日益增加,此路线应能便于获取该核心结构用于构效关系(SAR)研究。

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