以醛为前体的自动化一锅文库合成

IF 6.1 Q1 CHEMISTRY, MULTIDISCIPLINARY
Adrián Luguera Ruiz, Brenda Pijper, Maria Lourdes Linares, Santiago Cañellas, Stefano Protti, Maurizio Fagnoni, Jesús Alcázar
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引用次数: 0

摘要

对Csp3富集基序的合成需求的增加和发现新药的紧迫性要求开发更有效的技术和合成工具来加速药物发现过程。在此,我们报告了一种完全自动化的策略,通过Giese添加将富含Csp3的构建块添加到烯烃上以形成Csp3 - Csp3键。开发的全自动方案允许醛(非氧化还原活性物质)原位转化为电活性咪唑烷,并在光氧化还原催化条件下作为c中心自由基的前体,通过合成富含sp3的化合物来合成构建块和生物活性化合物库。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Automated One-Pot Library Synthesis with Aldehydes as Radical Precursors

Automated One-Pot Library Synthesis with Aldehydes as Radical Precursors

The increased demand for the synthesis of Csp3 enriched motifs and the urgency of discovering new drugs requires the development of more efficient technologies and synthetic tools to accelerate drug discovery processes. Herein, we report a fully automated strategy for the addition of Csp3 enriched building blocks onto olefins via Giese addition to forge Csp3−Csp3 bonds. The developed fully automated protocol allowed the in-situ conversion of aldehydes (non-redox-active species) to electroactive imidazolidines and their use as precursors of C-centered radicals under photoredox catalyzed conditions for the synthesis of building blocks and bioactive compound libraries by synthesizing sp3-enriched compounds.

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来源期刊
CiteScore
7.30
自引率
0.00%
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