Synthesis of 2-amidoindenone derivatives through an ynamide carbosilylation/Houben-Hoesch cyclization 2-step sequence

Herein we report the efficient and selective two-step synthesis of various 3-silyl-2-amidoindenones from easily accessible ynamides. This sequence involves a regio- and stereo-selective silylcyanation followed by a Houben-Hoesch type cyclization. Thanks to post-transformations, various 3-substituted 2-amidoindenones could be obtained. A simple and selective two-step sequence is reported for the synthesis of polyfunctionalized 2-amidoindenones. Remarkably, this method achieves true structural diversity at position 3.