An efficient approach for monosulfide bridge formation in solid-phase peptide synthesis |
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| Authors: | Pietro Campiglia Luigi Longobardo Ettore Novellino |
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| Institution: | a Dipartimento di Chimica Farmaceutica e Tossicologica, University of Naples, ‘Federico II’, 80131 Naples, Italy
b Dipartimento di Scienza degli Alimenti, University of Naples ‘Federico II’, Naples, Italy |
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| Abstract: | An efficient approach for the synthesis of cyclic peptides containing unnatural thioether side-chain bridges, based on the use of (2S)-9-fluorenylmethyl-2-(tert-butoxycarbonyl)amino]-4-iodobutanoate and its homologue 5-iodopentanoate, derived from Boc-l-Asp-OFm and Boc-l-Glu-OFm, respectively, is reported. The synthesis was performed by a tandem combination of solid-phase peptide synthesis and microwave-assisted cyclization strategy. |
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| Keywords: | Thioether bridge Solid-phase peptide synthesis Macrocyclization |
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