Key Laboratory of Pesticide & Chemical Biology, Ministry of Education, College of Chemistry, Central China Normal University, Hubei, Wuhan 430079, P. R. China.
Org Lett. 2012 Jul 6;14(13):3392-5. doi: 10.1021/ol301366p. Epub 2012 Jun 26.
A molecular I(2)-promoted sp(3) C-H bond dual-(het)arylation protocol was developed for the synthesis of 2,2-bisindolyl-1-arylethanones. Through a logical design, three mechanism-different reactions (iodination, Kornblum oxidation, and Friedel-Crafts reaction) were assembled in a single reactor. A variety of 2,2-bisindolyl-1-aryl ethanones were synthesized from simple and readily available aryl methyl ketones and indoles. In the reaction, metal, base, and ligand were all avoidable.
发展了一种分子碘促进的 sp(3) C-H 键双(杂)芳基化的方法,用于合成 2,2-双吲哚基-1-芳基乙酮。通过合理的设计,三种不同机理的反应(碘化、Kornblum 氧化和傅克反应)被组装在同一个反应器中。各种 2,2-双吲哚基-1-芳基乙酮可以由简单易得的芳基甲基酮和吲哚合成。在反应中,避免了金属、碱和配体的使用。