- Diverse methyl sulfone-containing benzo[b] thiophene library via iodocyclization and palladium-catalyzed coupling
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Parallel solution-phase methods for the synthesis of a 72-membered benzo[b]thiophene library are reported. Medicinally interesting, drug-like, methyl sulfone-substituted benzo[b]thiophenes have been prepared by the palladium-catalyzed substitution of 3-iodobenzo[b]thiophenes by Suzuki-Miyaura, Sonogashira, Heck, carboalkoxylation, and aminocarbonylation chemistry. The key intermediates for library generation, methyl sulfone-containing 3-iodobenzo[b]thiophenes, are readily prepared by iodocyclization and oxidation methodologies from readily available alkynes.
- Cho, Chul-Hee,Neuenswander, Benjamin,Larock, Richard C.
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supporting information; experimental part
p. 278 - 285
(2010/08/06)
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