微流控反应器中C-O键的形成：杂芳基氯的高产率SAr取代反应
C-O bond Formation in a Microfluidic Reactor: High Yield SAr Substitution of Heteroaryl Chlorides.
作者信息
Alam Mohammad Parvez, Jagodzinska Barbara, Campagna Jesus, Spilman Patricia, John Varghese
机构信息
Drug Discovery Laboratory, Department of Neurology, Mary S. Easton Center for Alzheimer's Disease Research, University of California, Los Angeles, CA 90095.
出版信息
Tetrahedron Lett. 2016 May 11;57(19):2059-2062. doi: 10.1016/j.tetlet.2016.03.095.
This study describes our development of a novel and efficient procedure for C-O bond formation under mild conditions, for coupling heteroaryl chlorides with phenols or primary aliphatic alcohols. We utilized a continuous-flow microfluidic reactor for C-O bond formation in electron-deficient pyrimidines and pyridines in a much more facile manner with a cleaner reaction profile, high yield, quick scalability and without the need for the transition metal catalyst. This approach can be of general utility to make C-O bond containing intermediates of industrial importance in a continuous and safe manner.
本研究描述了我们开发的一种新型高效的方法，用于在温和条件下形成C-O键，使杂芳基氯化物与酚类或伯脂肪醇偶联。我们利用连续流动微流反应器，以更简便的方式在缺电子嘧啶和吡啶中形成C-O键，反应过程更清洁，产率高，可快速放大，且无需过渡金属催化剂。这种方法可普遍用于以连续、安全的方式制备具有工业重要性的含C-O键中间体。
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