Suppr超能文献

通过将高性能光反应器与台式分析相结合来加速基于片段的文库生成。

Accelerating fragment-based library generation by coupling high-performance photoreactors with benchtop analysis.

作者信息

Lefebvre Quentin, Salomé Christophe, Fessard Thomas C

机构信息

SpiroChem AG, Rosental area, WRO-1047-3, Mattenstrasse 24, 4058 Basel, Switzerland.

出版信息

Beilstein J Org Chem. 2020 May 12;16:982-988. doi: 10.3762/bjoc.16.87. eCollection 2020.

Abstract

Herein we report a workflow coupling photoredox-nickel dual-catalyzed -arylation reactions to benchtop analysis for the efficient generation of fragment-based libraries. Technological advances in photoreactor design facilitated reliable and reproducible experimentation. Knowledge on the reactivity under previously reported reaction conditions of spirocyclic and strained heterocyclic building blocks, viewed as chemistry informers, could thus be rapidly accessed, identifying privileged or challenging scaffolds and paving the way for further exploration.

摘要

在此,我们报告了一种将光氧化还原-镍双催化的芳基化反应与台式分析相结合的工作流程,用于高效生成基于片段的文库。光反应器设计的技术进步促进了可靠且可重复的实验。因此,可以快速获取作为化学信息源的螺环和张力杂环构建块在先前报道的反应条件下的反应性知识,识别出有优势或具有挑战性的支架,并为进一步探索铺平道路。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e6a4/7237803/8bb7268992de/Beilstein_J_Org_Chem-16-982-g005.jpg

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