杂芳香硫醚与有机锌试剂的自动烷基化库合成

IF 5 1区化学 Q1 CHEMISTRY, ORGANIC

Organic Letters Pub Date : 2025-05-19 DOI:10.1021/acs.orglett.5c0152010.1021/acs.orglett.5c01520

Javier Mazuela, Aritz Martinez, Paula Cervantes-Cerrada, Lucía Alcaide, Belén Chaves-Arquero, Santiago Cañellas, Jesús Alcazar and José Enrique Gómez*,

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引用次数: 0

摘要

在这项研究中，我们描述了一个自动化的高通量工作流程的实现，以在流动中使用不同的烷基有机锌试剂有效地功能化与药物化学相关的杂芳基硫醚。观察到与不同芳基硫醚底物和有机锌试剂的成功偶联，突出了该平台在快速文库多样化方面的广泛适用性。该平台极大地提高了C（sp3）中心杂芳硫醚修饰的速度和效率，从而促进了新的生物活性化合物的发现，并将其定位为药物化学项目的宝贵资源。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Automated Alkylation of Heteroaromatic Thioethers with Organozinc Reagents for Library Synthesis

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Automated Alkylation of Heteroaromatic Thioethers with Organozinc Reagents for Library Synthesis

In this study, we describe the implementation of an automated high-throughput workflow to efficiently functionalize medicinal-chemistry-relevant heteroaryl thioethers with diverse alkyl organozinc reagents in flow. The successful coupling observed with different aryl thioether substrates and organozinc reagents highlights the broad applicability of this platform for rapid library diversification. This platform greatly improves the speed and efficiency of modifying heteroaromatic thioethers featuring C(sp³) centers, thereby facilitating the discovery of novel bioactive compounds and positioning it as a valuable resource for medicinal chemistry projects.

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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.