Solid-phase synthesis of N-nosyl- and N-Fmoc-N-methyl-alpha-amino acids |
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Authors: | Di Gioia Maria Luisa Leggio Antonella Liguori Angelo Perri Francesca |
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Institution: | Dipartimento di Scienze Farmaceutiche, Università della Calabria, Via Ponte P. Bucci cubo 15/C, I-87036 Arcavacata di Rende (CS), Italy. |
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Abstract: | We report here a convenient and simple solid-phase synthesis of N-nosyl-N-methyl-alpha-amino acids and N-Fmoc-N-methyl-alpha-amino acids, important building blocks for the synthesis of conformationally restricted and protease-resistant natural peptides and peptide analogues. The methodology involves the use of 2-chlorotrityl chloride resin to temporarily protect the carboxylic group of alpha-amino acids and of diazomethane as the reagent to methylate the sulfonamidic function. The approach developed is particularly efficient also with alpha-amino acids bearing appropriately protected functionalized side chains. |
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