O'Byrne Sean N, Eduful Benjamin J, Willson Timothy M, Drewry David H
Structural Genomics Consortium, UNC Eshelman School of Pharmacy, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA.
Tetrahedron Lett. 2020 Sep 17;61(38). doi: 10.1016/j.tetlet.2020.152353. Epub 2020 Aug 16.
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.
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。