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筛选与DNA编码化学文库兼容的铜和钯介导的反应。

Screening of copper and palladium-mediated reactions compatible with DNA-encoded chemical libraries.

作者信息

Favalli Nicholas, Bassi Gabriele, Zanetti Tania, Scheuermann Jörg, Neri Dario

机构信息

Institute of Pharmaceutical Sciences, ETH Zürich, 8093 Zürich (Switzerland).

出版信息

Helv Chim Acta. 2019 Apr 1;102(4). doi: 10.1002/hlca.201900033. eCollection 2019 Apr 15.

DOI:10.1002/hlca.201900033
PMID:32292208
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7156289/
Abstract

The construction of DNA-encoded chemical libraries (DECLs) crucially relies on the availability of chemical reactions, which are DNA-compatible and which exhibit high conversion rates for a large number of diverse substrates. In this work, we present our optimization and validation procedures for three copper and palladium-catalyzed reactions (Suzuki cross-coupling, Sonogashira cross-coupling and copper(I)-catalyzed alkyne-azide cycloaddition (CuAAC)), which have been successfully used by our group for the construction of large encoded libraries.

摘要

DNA编码化学文库（DECLs）的构建关键依赖于化学反应的可用性，这些反应需与DNA兼容，并且对大量不同的底物表现出高转化率。在这项工作中，我们展示了我们对三种铜催化和钯催化反应（铃木交叉偶联反应、Sonogashira交叉偶联反应以及铜（I）催化的炔烃-叠氮环加成反应（CuAAC））的优化和验证程序，我们团队已成功地将这些反应用于构建大型编码文库。