| 摘要 |
<p>The tetrapeptide S-Bz-N-Tos-Cys-Tyr-Ile-Ser-OMe and the corresponding azide (where Bz = benzyl and Tos = tosyl) is prepared by reacting a reactive functional derivative of CBO-IleOH (CBO = carbobenzoxy) with HSerO-Alkyl or -O-Aralkyl to give the ester of CBO-Ile-SerOH, reacting this with catalytically activated H2, condensing it with S-Bz-N-Tos-Cys-TyrOH in the presence of carbodiimide to give SBz-N-Tos-Cys-Tyr-Ile-SerOH ester, e.g. methyl ester, reacting this with NH2NH2 to give the hydrazide then reacting this with HNO2; or by reacting a functional derivative of CBO-IleOH with an N2-protected serine hydrazide, treating the CBO-Ile-Ser-NHNH2-N2 derivative with activated H2, condensing the product with S-Bz-N-Tos-Cys-TyrOH in the presence of carbodiimide to give SB2-N-Tos-Cys-Tyr-Ile-SerNHNH2-N2 derivative and converting this into the free hydrazide by acid solvolysis before reaction with HNO2.</p> |
