| 摘要 |
Process for the preparation of didemnine A Comprises: (a) coupling the units Z-N(Me)-O(Me)-Tyr-O- [Boc-Thr]-OH and H-Ist-Hip-Leu-Pro-OBzl. HCl in the presence of HBTU and DIEA, (b) simultaneously deprotecting the N- and C-terminal ends of the product obtained, (c) cyclizing the product from stage (b) using the coupling agent HBTU in the presence of HOBT and DIEA to produce a macrocycle with the terminal N of the Thr protected, (d) deprotecting the said group and coupling the macrocycle with Boc-(R)-NMe-Leu-OH to produce Boc- didemnine A, (e) reacting the latter product with trifluoroacetic acid to obtain didemnine A. Didemnine A has application as an antitumour, antiviral and immunosuppressive agent.
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