Coupling of thioamides with 4-bromocrotonate esters and subsequent conjugate addition for the rapid one-pot synthesis of functionalized thiazolines |
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| Authors: | Patrick D. Parker Yonghe Ge Joshua G. Pierce |
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| Affiliation: | Department of Chemistry, College of Sciences, NC State University, Raleigh, NC 27695, USA |
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| Abstract: | An efficient one-pot synthesis of functionalized thiazolines via the coupling of thioamides with 4-bromocrotonate esters is described. A range of aryl- and alkyl-thioamides with various substitutions are well-tolerated. Additionally, the presence of the exocyclic ester functionality provides a convenient handle for the synthesis of more complex thiazoline-containing natural products and biologically-relevant compounds. |
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| Keywords: | Heterocycle Natural products Medicinal chemistry Alkylation Thiazoline |
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