Title

Metal-Free Arylation of Ethyl Acetoacetate with Hypervalent Diaryliodonium Salts: An Immediate Access to Diverse 3-Aryl-4(1H)-Quinolones

Document Type

Article

Publication Date

2015

Digital Object Identifier (DOI)

https://doi.org/10.1021/jo5023958

Abstract

A clean arylation protocol of ethyl acetoacetate was developed using hypervalent diaryliodonium salts under mild and metal-free conditions. The scope of the reaction, using symmetric and unsymmetric iodonium salts with varying sterics and electronics, was examined. Further, this method has been applied for the synthesis of antimalarial compound ELQ-300, which is currently in preclinical development.

Was this content written or created while at USF?

Yes

Citation / Publisher Attribution

The Journal of Organic Chemistry, v. 80, issue 5, p. 2513-2520

Share

COinS