3,4-二氢嘧啶-2-硫酮与炔烃的氧化脱氢交叉偶联反应构建 2-炔基嘧啶。
Oxidative Dehydrosulfurative Cross-Coupling of 3,4-Dihydropyrimidine-2-thiones with Alkynes for Access to 2-Alkynylpyrimidines.
机构信息
Department of Chemistry, Chungnam National University, Daejeon 34134, Republic of Korea.
Yonsung Fine Chemicals R&D Center, Suwon 16675, Republic of Korea.
出版信息
J Org Chem. 2020 Apr 3;85(7):5087-5096. doi: 10.1021/acs.joc.0c00091. Epub 2020 Mar 16.
A reaction method is described for the one-step synthesis of 2-alkynylpyrimidines from 3,4-dihydropyrimidin-1-2-thiones (DHPMs) via dehydrosulfurative Sonogashira cross-coupling with concomitant oxidative dehydrogenation using a Pd/Cu catalytic system. Together with the ready availability of DHPMs possessing various substituents at the C4-C6 positions, this transformation offers rapid and general access to diverse 2-alkynylpyrimidine derivatives.
描述了一种通过 3,4-二氢嘧啶-1-2-硫酮（DHPMs）的脱水硫代 Sonogashira 交叉偶联与同时的氧化脱氢反应，在 Pd/Cu 催化体系中一步合成 2-炔基嘧啶的反应方法。DHPMs 具有在 C4-C6 位置的各种取代基，因此这种转化提供了快速和通用的方法来获得各种 2-炔基嘧啶衍生物。
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