铑(III)催化下喹啉-氧化物与马来酰亚胺的 C8 位选择性烷基化反应。
Site-Selective C8-Alkylation of Quinoline -Oxides with Maleimides under Rh(III) Catalysis.
机构信息
School of Pharmacy, Sungkyunkwan University, Suwon 16419, Republic of Korea.
Division of Bio and Drug Discovery, Korea Research Institute of Chemical Technology, Daejeon 34113, Republic of Korea.
出版信息
J Org Chem. 2021 Jun 4;86(11):7579-7587. doi: 10.1021/acs.joc.1c00612. Epub 2021 May 5.
The site-selective modification of quinolines and their analogs has emerged as a pivotal topic in medicinal chemistry and drug discovery. Herein, we describe the rhodium(III)-catalyzed C8-alkylation of quinoline -oxides with maleimides as alkylating agents, resulting in the formation of bioactive succinimide-containing quinoline derivatives. The reaction proceeds under mild conditions with complete functional group tolerance.
喹啉及其类似物的位点选择性修饰已经成为药物化学和药物发现中的一个关键课题。在此，我们描述了铑(III)催化的喹啉 -氧化物与马来酰亚胺作为烷基化试剂的 C8-烷基化反应，生成了含有生物活性琥珀酰亚胺的喹啉衍生物。该反应在温和的条件下进行，具有完全的官能团容忍性。
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