Rh（III）催化区域选择性C-H活化/[4+2]环化级联合成γ-羰基衍生物

IF 5 1区化学 Q1 CHEMISTRY, ORGANIC

Organic Letters Pub Date : 2025-06-09 DOI:10.1021/acs.orglett.5c01984

Zhangshun Luo, Yao Chen, Lijie Lv, Lida Wang, Yue Wei, Yi He, Shenyou Nie

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引用次数: 0

摘要

在面临区域选择性控制等挑战的同时，过渡金属催化环化是构建多种生物活性分子的一种有吸引力的方法。本文建立了一种由2h -咪唑和炔烃组成的高功能化γ-羰基衍生物的高效组装方法。这是通过铑（III）催化的C-H活化/[4+2]串联环化级联实现的，促进了以中等产量获得具有良好抗癌活性的γ-羰基化合物的化学和区域选择性。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Synthesis of γ-Carboline Derivatives via the Rh(III)-Catalyzed Regioselective C–H Activation/[4+2] Annulation Cascade

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Synthesis of γ-Carboline Derivatives via the Rh(III)-Catalyzed Regioselective C–H Activation/[4+2] Annulation Cascade

Transition-metal-catalyzed annulation represents an attractive approach for constructing diverse bioactive molecules while facing challenges like regioselective control. Herein, an efficient assembly of diverse highly functionalized γ-carboline derivatives from 2H-imidazoles and alkynes has been established. This was achieved through a rhodium(III)-catalyzed C–H activation/[4+2] tandem cyclization cascade, facilitating chemo- and regioselective access to γ-carbolines, which exhibit good anticancer activity, in moderate yields.

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来源期刊

Organic Letters 化学-有机化学

CiteScore

9.30

自引率

11.50%

发文量

1607

审稿时长

1.5 months

期刊介绍： Organic Letters invites original reports of fundamental research in all branches of the theory and practice of organic, physical organic, organometallic,medicinal, and bioorganic chemistry. Organic Letters provides rapid disclosure of the key elements of significant studies that are of interest to a large portion of the organic community. In selecting manuscripts for publication, the Editors place emphasis on the originality, quality and wide interest of the work. Authors should provide enough background information to place the new disclosure in context and to justify the rapid publication format. Back-to-back Letters will be considered. Full details should be reserved for an Article, which should appear in due course.