Small Molecule Drug Discovery, Amgen Inc., One Amgen Center Drive, Thousand Oaks, CA 91320-1789, U.S.A.
Abstract:
Efficient assembly of 14-membered macrocycles utilizing the SNAr of fluorine in 3-fluoro-4-nitrobenzoic acid with the OH of 3-hydroxytyrosine on solid support is reported. The flexibility of this synthesis, as well as the excellent purity (>90%) of the final products are the distinctive characteristic of the resultant library.