Glogowski Michal P, Cercizi Noel, Lynch-Colameta Tessa, Ridgers Lance H, Phelan James P, Rowley Ann M, Rauch Martin P
GSK, 1250 South Collegeville Road, Collegeville, Pennsylvania 19426, United States.
Org Lett. 2024 Mar 29;26(12):2420-2424. doi: 10.1021/acs.orglett.4c00577. Epub 2024 Mar 18.
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.
本文的讨论描述了一种金属光氧化还原反应,该反应能够在药物化学中高效地探索苄基结构-活性关系。高通量实验(HTE)和化学微球的使用能够实现快速的反应优化。通过芳基溴化物和苄基溴化物之间的交叉亲电偶联形成二(杂)芳基甲烷,可进入多样化的化学空间。本文将讨论底物范围的广度,以及利用间歇光化学大规模制备这种二(杂)芳基甲烷基序的方法。