| Abstract
| - Herein we report a solid-phase synthetic approach to [Ala7]-phalloidin (1). Prior syntheses ofphallotoxins were carried out using solution-phase routes that required large scale and precludelibrary production. The route presented here consists of solution-phase preparation of keyorthogonally protected amino acid building blocks, followed by a solid-phase peptide synthesissequence, featuring two resin-bound macro-cyclization reactions. The final product mixture wascomposed of two atropisomeric compounds, one designated “natural” (1) and the other designated“non-natural” (1‘). The structures of these species were modeled using restrained energy minimization with NMR-derived restraints.
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