Maity Saurabh, Karmakar Ujjwal, Samanta Rajarshi
Department of Chemistry, Indian Institute of Technology Kharagpur, Kharagpur 721302, India.
Chem Commun (Camb). 2017 Nov 9;53(90):12197-12200. doi: 10.1039/c7cc07086a.
A straightforward Rh(iii)-catalyzed general strategy was developed for the site-selective remote C4 (sp) and C2 (sp)-methyl thiolation of an indole core, keeping the oxime directing group at the C3 position. The transformation was accomplished under mild conditions with a wide scope and functional group tolerance. The directing group can easily be removed after operation. Methyl substitution at the C2 position of the indole core led to C2 (sp)-methyl thiolation.
开发了一种直接的铑(iii)催化通用策略,用于吲哚核心的位点选择性远程C4 (sp)和C2 (sp)甲基硫醇化反应,同时将肟导向基团保留在C3位置。该转化反应在温和条件下完成,具有广泛的底物范围和官能团耐受性。反应操作后导向基团可轻松去除。吲哚核心C2位置的甲基取代导致了C2 (sp)甲基硫醇化反应。