作者:Donald McAusland、Sangwon Seo、Didier G. Pintori、Jonathan Finlayson、Michael F. Greaney
DOI:10.1021/ol201413r
日期:2011.7.15
A new approach to the Fischer-indole synthesis is reported that uses the reactive intermediate benzyne. The addition of N-tosyl hydrazones to arynes, generated through fluoride activation of 2-(trimethylsilyl)phenyl triflate precursors, leads to efficient N-arylation. Addition of a Lewis acid to the same reaction pot then affords N-tosylindole products via Fischer cyclization.