Hareram Mishra Deepak, El Gehani Albara A M A, Harnedy James, Seastram Alex C, Jones Andrew C, Burns Matthew, Wirth Thomas, Browne Duncan L, Morrill Louis C
Cardiff Catalysis Institute, School of Chemistry, Cardiff University, Main Building, Park Place, Cardiff, CF10 3AT, United Kingdom.
Chemical Development, Pharmaceutical Technology & Development, Operations, AstraZeneca, Macclesfield, SK10 2NA, United Kingdom.
Org Lett. 2022 Jun 3;24(21):3890-3895. doi: 10.1021/acs.orglett.2c01552. Epub 2022 May 23.
Herein, we report a new electrochemical method for alkoxy radical generation from alcohols using a proton-coupled electron transfer (PCET) approach, showcased via the deconstructive functionalization of cycloalkanols. The electrochemical method is applicable across a diverse array of substituted cycloalkanols, accessing a broad range of synthetically useful distally functionalized ketones. The orthogonal derivatization of the products has been demonstrated through chemoselective transformations, and the electrochemical process has been performed on a gram scale in continuous single-pass flow.
在此,我们报告了一种利用质子耦合电子转移(PCET)方法从醇类生成烷氧基自由基的新电化学方法,通过环烷醇的解构官能化得以展示。该电化学方法适用于多种取代环烷醇,可得到一系列具有广泛合成用途的远端官能化酮。已通过化学选择性转化证明了产物的正交衍生化,并且该电化学过程已在克级规模上以连续单通道流动方式进行。