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Synthesis of RGD analogues containing α-Tfm-arginine as potential fibrinogen receptor antagonists

✍ Scribed by Alma Dal Pozzo; Laura Muzi; Maurizio Moroni; Riccardo Rondanin; Roberto de Castiglione; Pierfrancesco Bravo; Matteo Zanda

Publisher
Elsevier Science
Year
1998
Tongue
French
Weight
555 KB
Volume
54
Category
Article
ISSN
0040-4020

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✦ Synopsis

AIImraet The ~ of two ~ mimetics of RGD, ct-Tfm-Arg-Gly-Asp-Phe-NHz 9 anti ct-Tfm-Arg431y-Asp-NH-(CH2h-C6Hs 13, is desmb~ The precursor of ct-Tfin-omithine was obtained in two s~ steps from 2-N-C~-2-T[m-hexkncdiaO_ " __'d_-l-all~-! ester and introduced into the peptide chain by tz-catboxy-group activation via oxazolon¢. The int~oductio~a of the guanidi~ residue led to the final l~des as mixtures of the two tliastetetm~m. Configuratiomlly Irate ~ were obtained in good yields by RP-HPLC.

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