Journal
JOURNAL OF ORGANIC CHEMISTRY
Volume 76, Issue 3, Pages 766-772Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jo101629v
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Funding
- MESR
- CNRS
- Idenix Pharmaceuticals
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A new linker cis-5-aminopent-3-enoic acid (cis-Apa) was prepared for the synthesis of cyclic pseudopeptides by cyclization-cleavage by using ring-closing methatesis (RCM). We developed a new synthetic pathway for the preparation of the cis-Apa linker that was tested in the cyclization-cleavage process of different RGD peptide sequences. Different macrocyclic peptidomimetics were prepared by using this integrated microwave-assisted method, showing that the readily available cis-Apa amino acid is well adapted as a linker in the cyclization-cleavage process.
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