A versatile method for the construction of C(sp)-linked cyclophane peptide macrocycles via Pd-catalyzed picolinamide-directed intramolecular arylation of aryl and alkenyl C-H bonds of amino acid side chains with aryl iodides is developed. This method provides simple and efficient access to a variety of cyclophane-braced structures from readily accessible linear peptide precursors.
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| http://dx.doi.org/10.1021/acs.orglett.0c02422 | DOI Listing |
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