Abstract
We describe an efficient solid-phase synthesis of 14-membered macrocycles derived from 4-hydroxyproline and 3-fluoro-4-nitrobenzoic acid. The procedure is based on the aromatic nucleophilic displacement of fluoride with the OH function. The targeted macrocycles are obtained in good yields, and are 90–95% pure. The diversity elements in the synthesis are: amine immobilized on solid support and amino acids.
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