| 摘要 |
<p>Novel compounds which are N- and 0-acylates of pyrazofurin are described herein. A novel process for the preparation of the mono-N1-acylates comprises reacting pyrazofurin with an acylating agent under non-basic conditions in an organic solvent. The mono-N1-acylate so formed is further acylated under weak basic conditions to provide a tetra-acylated or penta-acylated pyrazofurin derivative, depending upon the duration of reaction. Mild solvolysis of either a tetra-acylate or a penta-acylate provides a tri-acylated pyrazofurin derivative. In the presence of a strong base, the mono-N1-acylate is further acylated to provide different tetra-acylates or pentaacylates of pyrazofurin, again depending upon the duration of reaction. Pyrazofurin acylates are useful as antiviral, antipsoriatic, antitumor and antifungal agents, as well as intermediates for new C-nucleosides.</p> |
