RESUMO
N-terminal fragment of emerimicin III has been synthesized by the repetitive method in solution, involving triazine ,,superactive esters". The synthetic protocol, equivalent to the classic REMA procedure, has been applied in the step by step approach, and in the fragment coupling affording all the peptide bonds. By monitoring the progress of the synthesis by FAB-MS, 1H-NMR and HPLC, the structure and high purity of the final products have been confirmed.
Assuntos
Oligopeptídeos/síntese química , Triazinas/síntese química , Cromatografia Líquida de Alta Pressão , Ésteres , Espectroscopia de Ressonância Magnética , Peptaibols , Peptídeos/análise , Peptídeos/química , Tecnologia Farmacêutica/métodos , Triazinas/químicaRESUMO
A new synthetic protocol which considerably improves the classic REMA procedure is proposed herein. The offered modification is based on the application of triazine "superactive esters" as the superior substitutes for mixed anhydrides, which have been used as acylating reagent in the classic procedure. The improved repetitive procedure in solution was applied to the preparation of [54-59] fragment of human beta-casein. The structure and high purity of the intermediates, as well as of the final products, was confirmed by FAB-MS, 1H-NMR and HPLC.
