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通过光催化后期官能团化方案获得SCF取代的中氮茚。

Access to SCF-Substituted Indolizines via a Photocatalytic Late-Stage Functionalization Protocol.

作者信息

Stefanoni Kevin Klaus, Wilhelm René

机构信息

Institute of Organic Chemistry, Clausthal University of Technology, Leibnizstr. 6, 38678 Clausthal-Zellerfeld, Germany.

出版信息

Org Lett. 2025 Aug 8;27(31):8389-8393. doi: 10.1021/acs.orglett.5c02079. Epub 2025 Jul 21.

Abstract

A mild, scalable, and highly chemoselective photocatalytic method was developed for direct indolizine functionalization with -((trifluoromethyl)thio)saccharin, yielding high amounts of desired products while tolerating various functional groups. The photoredox catalyst employed offers a straightforward and inexpensive alternative to commercially available catalysts. Additionally, a 3-SCF analogue of a histamine H3 receptor antagonist was synthesized with excellent yield, demonstrating the strategy's potential in developing biologically relevant molecules.

摘要

开发了一种温和、可扩展且具有高度化学选择性的光催化方法,用于用-((三氟甲基)硫代)糖精直接对中氮茚进行官能化,在容忍各种官能团的同时产生大量所需产物。所使用的光氧化还原催化剂为市售催化剂提供了一种直接且廉价的替代方案。此外,以优异的产率合成了一种组胺H3受体拮抗剂的3-SCF类似物,证明了该策略在开发具有生物学相关性的分子方面的潜力。

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