We thank Merck Serono KGaA, Darmstadt, for financial support.
Three-Component Synthesis of Ynediones by a Glyoxylation/Stephens–Castro Coupling Sequence†
Article first published online: 23 FEB 2011
Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Angewandte Chemie International Edition
Volume 50, Issue 13, pages 2966–2969, March 21, 2011
How to Cite
Merkul, E., Dohe, J., Gers, C., Rominger, F. and Müller, T. J. J. (2011), Three-Component Synthesis of Ynediones by a Glyoxylation/Stephens–Castro Coupling Sequence. Angew. Chem. Int. Ed., 50: 2966–2969. doi: 10.1002/anie.201007194
- Issue published online: 15 MAR 2011
- Article first published online: 23 FEB 2011
- Manuscript Received: 16 NOV 2010
- Merck Serono KGaA, Darmstadt
- CC coupling;
- multicomponent reactions
One step back, two steps forward! Starting from diverse heterocycles, the title reaction furnishes ynediones under very mild conditions in a direct and preparatively simple one-pot process. The key to avoiding decarbonylation is the CuI-catalyzed Stephens–Castro alkynylation rather than the usually more efficient Sonogashira coupling. In addition, novel highly atom-economical four-component syntheses of various heterocycles can be achieved.