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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, R 3 =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...
Sodium dimethyl malonate couples effectively with Schiff base acetate 1 using an in situ generated palladium catalyst system and bis-phosphine ligands.
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