title: Direct regioselective oxidative cross-coupling of indoles with methyl ketones: a novel route to C3-dicarbonylation of indoles.
abstract: The first C3-dicarbonylation of indoles was realized through direct oxidative cross-coupling of indoles with methyl ketones in the presence of molecular iodine and pyrrolidine. This reaction constructed a highly efficient indolyl diketones scaffold, which might be regarded as a useful biological and pharmacological tool in the exploration of therapeutic A2BAR modulators. The use of inexpensive molecular iodine and pyrrolidine and a broad substrate scope make this protocol very practical. Preliminary mechanistic studies indicate that two paths are involved in this process.
authors.affiliation: Key Laboratory of Pesticide & Chemical Biology, Ministry of Education, College of Chemistry, Central China Normal University , Wuhan 430079, P. R. China.
authors.forename: Qinghe
authors.initials: Q
authors.lastname: Gao
authors.forename: Jingjing
authors.initials: J
authors.lastname: Zhang
authors.forename: Xia
authors.initials: X
authors.lastname: Wu
authors.forename: Shan
authors.initials: S
authors.lastname: Liu
authors.forename: Anxin
authors.initials: A
authors.lastname: Wu