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Developments in Photoredox-Mediated Alkylation for DNA-Encoded Libraries
Trends in Chemistry ( IF 15.7 ) Pub Date : 2020-12-29 , DOI: 10.1016/j.trechm.2020.11.010
Shivani Patel 1 , Shorouk O Badir 1 , Gary A Molander 1
Affiliation  

Recently, DNA-encoded library (DEL) technology has emerged as an innovative screening modality for the rapid discovery of therapeutic candidates in pharmaceutical settings. This platform enables a cost-effective, time-efficient, and large-scale assembly and interrogation of billions of small organic ligands against a biological target in a single experiment. An outstanding challenge in DEL synthesis is the necessity for water-compatible transformations under ambient conditions. To access uncharted chemical space, the adoption of photoredox catalysis in DELs, including Ni-catalyzed manifolds and radical/polar crossover reactions, has enabled the construction of novel structural scaffolds through regulated odd-electron intermediates. Herein, a critical discussion of the validation of photoredox-mediated alkylation in DEL environments is presented. Current synthetic gaps are highlighted and opportunities for further development are speculated upon.



中文翻译:

光氧化还原介导的 DNA 编码文库烷基化的进展

最近,DNA 编码文库 (DEL) 技术已成为一种创新的筛选方式,用于在制药环境中快速发现治疗候选者。该平台可以在单个实验中对数十亿个小型有机配体针对生物靶标进行经济高效、省时且大规模的组装和检测。DEL 合成的一个突出挑战是在环境条件下进行水相容性转化的必要性。为了进入未知的化学空间,在 DEL 中采用光氧化还原催化,包括 Ni 催化的歧管和自由基/极性交叉反应,使得能够通过调节的奇电子中间体构建新型结构支架。本文对 DEL 环境中光氧化还原介导的烷基化验证进行了批判性讨论。

更新日期:2021-02-24
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