The solid phase synthesis of α,α-disubstituted unnatural amino acids and peptides (di-UPS)

Add time:09/03/2019    Source:sciencedirect.com

This paper reports a new, mild procedure (“di-UPS”) for the solid phase synthesis of racemic α,α-disubstituted amino acids (1) and epimeric α,α-disubstituted terminal amino acid residues (2, R3=H) in a resin bound peptide. The synthetic route is compatible with most protected amino acid side chains and can be used in a continuing solid phase synthesis. Di-UPS should find wide applicability in the design and solid phase synthesis of hybrid amino acids and peptides, and the construction of basis units for combinatorial chemistry.

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