Synthesis of beta -pyrazinyl-L-alanine (Paa) and of peptide derivatives

Petermann, C; Fauchere, JL

HERO ID

4933595

Reference Type

Journal Article

Year

1983

HERO ID 4933595
In Press No
Year 1983
Title Synthesis of beta -pyrazinyl-L-alanine (Paa) and of peptide derivatives
Authors Petermann, C; Fauchere, JL
Journal Helvetica Chimica Acta
Volume 66
Issue 5 (1983)
Page Numbers 1513-1518
Abstract The title compound was prepared via a malonic ester synthesis starting with a-chloromethylpyrazine, and ending, after an asymmetric enzymatic hydrolysis of the racemic N-acetyl- beta -2-pyrazinylalanine to the L-form of the new amino acid. The optical purity was ascertained by super(1)H-NMR analysis at 360 MHz of the diastereoisomeric dipeptides L-pyrazinylalanine-L-leucine and D-pyrazinylalanine-L-leucine. Hydrophobic, steric and electronic parameters for its side chain were also estimated. The new amino acid could be introduced in the place of phenylalanine in the enkephalin-like pentapeptide (D-alanyl super(2), leucine super(5))enkephalin, thus showing good stability towards the classical methods of peptide synthesis.
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Keyword enkephalin; dipeptides; beta -pyrazinyl-L-alanine