Solution-Phase Parallel Synthesis of a Multi-substituted Benzo[b]thiophene Library
- 1 July 2009
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Combinatorial Chemistry
- Vol. 11 (5), 900-906
- https://doi.org/10.1021/cc9000604
Abstract
Generation of a library using parallel syntheses of multi-substituted benzo[b]thiophenes is described. The requisite 3-iodobenzo[b]thiophenes are readily prepared in excellent yields from various alkynes bearing electron-rich aromatic rings by electrophilic cyclization using I2 in CH2Cl2. The heteroaromatic carbon−iodine bonds allow further diversification by palladium-catalyzed Suzuki−Miyaura, Sonogashira, Heck, and carboalkoxylation chemistry to give multi-substituted benzo[b]thiophene derivatives.Keywords
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