| 摘要 |
FIELD: chemical technology, antiviral preparations. SUBSTANCE: invention relates to synthesis of acyclic guanosine analogues showing antiviral activity, in part, to the preparation aciclovir, [9-(2'-hydroxyethoxymethyl)-guanine] . Method involves combined processes of acetylguanines synthesis in a single reactor and their alkylation with 2-oxa-1,4-butandiol diacetate or dioxolan under conditions of acid catalysis followed by deacetylation of an intermediate substituted guanine with alkaline agent excess and regioselective formation of the end product and its isolation by crystallization. High yield of pure product (80-95%) is provided by precise control of narrow temperature intervals, barometric and time parameters of process and catalysts used. Guanine, guanosine and their acetates can be used as the parent raw. Important aspect of process - simultaneous synthesis of ribofuranose tetraacetates. Invention describes principle scheme of aciclovir synthesis and its derivatives and six typical examples. Synthesized preparation is used in medicine as an effective antiherpes agent. EFFECT: improved method of synthesis. 20 cl, 1 dwge
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