Synthesis of conformationally constrained cyclic peptides using an intramolecular sonogashira coupling |
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Authors: | Balraju V Reddy D Srinivasa Periasamy Mariappan Iqbal Javed |
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Affiliation: | Discovery Research, Dr. Reddy's Laboratories Ltd., Bollaram Road, Miyapur, Hyderabad, 500 049, A.P., India. |
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Abstract: | [Reaction: see text]. Small peptides having a 3-bromobenzyl group at the C-termini and n-alkynoyl group at the N-termini undergo a smooth copper-free intramolecular Sonogashira coupling reaction to afford the corresponding cyclic peptides in moderate yields. Scope and limitations of this macrocyclization is demonstrated with di-, tri-, and tetrapeptides. |
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