1,4-二酰基-2-甲基哌嗪类衍生物的合成研究
Synthesis of 1,4-Diacyl-2-Methylpiperazine Derivatives
DOI: 10.12677/HJCET.2023.134028, PDF,    科研立项经费支持
作者: 王博艺, 彭莞祺, 齐珍珠, 张静怡*：郑州师范学院，化学化工学院，河南 郑州
关键词: 2-甲基哌嗪；酰氯；亲核取代；合成；2-Methylpiperazine； Acyl Chloride； Acylation； Synthesis
摘要: 哌嗪及其衍生物是药物化学中常见的一类氮杂环，如帕博西尼、洛美沙星、替马沙星等小分子药物中均含有哌嗪环。本文在氮气保护下，以二氯甲烷为溶剂，三乙胺为碱，将2-甲基哌嗪与酰氯类化合物进行酰化反应得到了多种多样的1,4-二酰基-2-甲基哌嗪类衍生物；其次，通过哌嗪上氮原子的选择性保护、酰化、脱保护等方法得到了1,4-二不同酰基取代的2-甲基哌嗪类衍生物。
Abstract: Piperazine and its derivatives are a common class of nitrogen-containing heterocycles in medic-inal chemistry. Small molecule drugs such as Pazopanib, Lomefloxacin, and Temafloxacin all contain piperazine ring. In this article, various 1,4-diacyl-2-methylpiperazine derivatives were obtained through acylation reactions between 2-methylpiperazine and acyl chloride in the presence of N2 and using triethylamine as a base in DCM. Furthermore, 1,4-different diacyl sub-stituted 2-methylpiperazine derivatives were obtained through selective N-protection, acylation, and deprotection of 2-methylpiperazine.
文章引用：王博艺, 彭莞祺, 齐珍珠, 张静怡. 1,4-二酰基-2-甲基哌嗪类衍生物的合成研究[J]. 化学工程与技术, 2023, 13(4): 244-251. https://doi.org/10.12677/HJCET.2023.134028

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