Synthesis of IB-01211, a cyclic peptide containing 2,4-concatenated thia- and oxazoles, via Hantzsch macrocyclization |
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Authors: | Hernández Delia Vilar Gemma Riego Estela Cañedo Librada M Cuevas Carmen Albericio Fernando Alvarez Mercedes |
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Institution: | Barcelona Science Park Josep Samitier 1-5, E-08028 Barcelona, Spain. |
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Abstract: | structure: see text] An efficient and versatile convergent synthesis of IB-01211 based on a combination of peptide and heterocyclic chemistry is described. The key step in the synthesis is macrocyclization through intramolecular Hantzsch formation of the thiazole ring. Dehydration of a free primary alcohol to furnish the exocyclic methylidene present in the natural product was applied during the macrocyclization. |
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