Department of Chemistry, Rice University, BioScience Research Collaborative, 6500 Main Street, Rm 380, Houston, Texas 77030, United States.
Discovery Process Research, Janssen Research & Development L.L.C., 3210 Merryfield Row, San Diego, California 92121, United States.
J Org Chem. 2021 Sep 17;86(18):12945-12955. doi: 10.1021/acs.joc.1c01625. Epub 2021 Aug 31.
Herein a method for the radical alkylation of heteroaryl halides that relies upon the combination of photoredox and nickel catalysis is described. The use of aliphatic -(acyloxy)phthalimides as redox-active esters affords primary and secondary radicals for the decarboxylative dual cross-coupling with pyrimidine and pyridine heteroaryl chlorides, bromides, and iodides. The method provides an additional synthetic tool for the incorporation of medicinally relevant heterocyclic motifs.
本文描述了一种依靠光氧化还原和镍催化相结合的杂芳基卤化物的自由基烷基化方法。使用脂肪族-(acyloxy)邻苯二甲酰亚胺作为氧化还原活性酯，可提供与嘧啶和吡啶杂芳基氯化物、溴化物和碘化物进行脱羧双重交叉偶联的一级和二级自由基。该方法为引入具有药用相关性的杂环基序提供了另一种合成工具。
