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Utilization of High-Throughput Experimentation (HTE) and ChemBeads Toward the Development of an Aryl Bromide and Benzyl Bromide Photoredox Cross-Electrophile Coupling
Organic Letters ( IF 5.2 ) Pub Date : 2024-03-18 , DOI: 10.1021/acs.orglett.4c00577
Michal P. Glogowski 1 , Noel Cercizi 1 , Tessa Lynch-Colameta 1 , Lance H. Ridgers 1 , James P. Phelan 1 , Ann M. Rowley 1 , Martin P. Rauch 1
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The discussion herein describes a metallaphotoredox reaction that allows for efficient exploration of benzyl structure–activity relationships in medicinal chemistry. The use of HTE (high-throughput experimentation) and ChemBeads allows for rapid reaction optimization. The formation of di(hetero)arylmethanes via cross-electrophile coupling between aryl bromides and benzyl bromides provides access to diverse chemical space. The breadth of the substrate scope will be discussed, along with the utilization of batch photochemistry for the preparation of this di(hetero)arylmethane motif on a larger scale.

中文翻译:

利用高通量实验 (HTE) 和 ChemBeads 开发芳基溴和苄基溴光氧化还原交叉电偶联

本文的讨论描述了金属光氧化还原反应,该反应允许有效探索药物化学中的苄基结构-活性关系。 HTE(高通量实验)和 ChemBeads 的使用可以实现快速反应优化。通过芳基溴和苄基溴之间的交叉亲电子偶联形成二(杂)芳基甲烷,提供了进入不同化学空间的途径。将讨论底物范围的广度,以及利用批量光化学大规模制备这种二(杂)芳基甲烷图案。
更新日期:2024-03-18
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