构建吲哚氮取代环戊烯酮衍生物
吲哚结构在天然产物和药物化合物中广泛存在,本文提出了一种新颖的吲哚衍生物合成方法,以官能化的2-苯基乙炔基胺和2-呋喃甲醇为底物,通过Br?nsted酸催化呋喃醇重排反应生成炔基官能化的环戊烯酮中间体,随后通过PdBr?催化的氢胺化环化反应实现了多官能化吲哚氮取代环戊烯酮衍生物的高效合成。该方法反应条件温和,产物收率较高,为吲哚衍生物的合成提供了新思路,具有重要的应用前景。
Indole structures are widely present in natural products and drug compounds. This paper proposes a novel synthetic method for indole derivatives. Functionalized 2-phenylacetylenylamine and 2-furaldehyde are used as substrates. Through the Br?nsted acid-catalyzed rearrangement of furaldehyde, aynyl-functionalized cyclopentenone intermediate is generated. Subsequently, the efficient synthesis of multifunctionalized indole nitrogen-substituted cyclopentenone derivatives is achieved through palladium(II) bromide (PdBr?)-catalyzed hydroamination-cyclization. This method features mild reaction conditions and high product yields, offering a new approach for the synthesis of indole derivatives and holding significant application potential.
谢开俊、唐雨榕
重庆大学化学化工学院,重庆 041331重庆大学化学化工学院,重庆 041331
化学药学
有机化学吲哚环戊烯酮重排
Organic Chemistryindolecyclopentenonerearrangement
谢开俊,唐雨榕.构建吲哚氮取代环戊烯酮衍生物[EB/OL].(2025-04-17)[2025-05-02].http://www.paper.edu.cn/releasepaper/content/202504-159.点此复制
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