Cédric Kalinski, Michael Umkehrer, Jurgen G Schmidt
Jul 3, 2006
Citations
1
Influential Citations
48
Citations
Journal
Tetrahedron Letters
Abstract
A novel one-pot two-step multi component reaction of acrylic aldehydes, bromoanilines, acids and isocyanides yielding polysubstituted indoles is described. The reaction is based on the combination of an Ugi four-component reaction followed by an intramolecular Heck-reaction. The simultaneous use of formic acid and cinnamaldehydes affords in situ generation of 1H-indoles. Convertible isocyanides can also be used with success in this Ugi/Heck strategy and enable synthesis of 1H-indole-2-carboxylic acid building blocks.