123rd General Meeting of the KCS

Type Poster Presentation
Area Medicinal Chemistry
Room No. Exhibition Hall 2
Time 4월 18일 (목요일) 11:00~12:30
Code MEDI.P-412
Subject C-H Aminocarbonylation of N-(Hetero)aryl-7-azaindoles with Isocyanate under Ruthenium(II) Catalysis
Authors Taejoo Jeong, Kunyoung Kim, Na Yeon Kwon, In Su Kim*
School of Pharmacy, Sungkyunkwan University, Korea
Abstract 7-Azaindoles as bioisosteres of indoles have been known to display diverse biological profiles. With great advances in organic and medicinal chemistry, a number of 7-azaindoles have been synthesized and screened for clinical trial. For examples, vemurafenib (ZelborafTM), decernotinib, PLX647, GSK1070916, and BMS378806, are currently on the market or under clinical phase. In this context, the directing group-assisted C–H functionalization of 7-azaindoles has been recognized as the useful strategy to generate the highly substituted 7-azaindole derivatives. However, to our best knowledge, the Ru(II)-catalyzed 7-azaindole-directed C–H aminocarbonylation has been unexplored. In our recent studies on the synthesis of biologically active compounds based on catalytic C−H functionalization, we herein disclose the site-selective Ru(II)-catalyzed C−H aminocarbonylation of 7-azaindoles with alkyl and aryl isocyanates to afford the corresponding ortho-amidated 7-azaindoles.
E-mail bonbatj@nate.com