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Solid support synthesis of 14- and 17-membered macrocycles via the SNAr methodology
Authors:Alexander S Kiselyov  Leon Smith  II  Paul Tempest
Institution:

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.
Keywords:macrocycles  supported reagents/reactions  solid-phase synthesis
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