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1: Org Lett. 2007 Mar 1;9(5):809-11. Epub 2007 Feb 1.Click here to read Links

Synthesis of IB-01211, a cyclic peptide containing 2,4-concatenated thia- and oxazoles, via Hantzsch macrocyclization.

Hernández D, Vilar G, Riego E, Cañedo LM, Cuevas C, Albericio F, Alvarez M.

Barcelona Science Park Josep Samitier 1-5, E-08028 Barcelona, Spain.

[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.

PMID: 17266322 [PubMed - indexed for MEDLINE]