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盐酸伐昔洛韦有关物质的合成 被引量:1

Synthesis of Related Substances of Valaciclovir Hydrochloride
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摘要 为了控制抗病毒药盐酸伐昔洛韦产品质量,分别合成了欧洲药典7.0版收载的两个有关物质:以氢化钠为碱,在乙二醇二丁醚中用N-Cbz伐昔洛韦分别与碘甲烷和碘乙烷反应生成N-甲基-N-Cbz伐昔洛韦和N-乙基-N-Cbz伐昔洛韦,随后在钯炭催化下氢解脱保护制得N-甲基伐昔洛韦(2)和N-乙基伐昔洛韦(3)。该方法是立体位阻较大的N-Cbz氨基酸衍生物的N-烷基化反应的改进方法。 To perform the quality control of antiviral agent valaciclovir hydrochloride, two related substances recorded in EP 7.0, N-methylvalaciclovir and N-ethylvalaciclovir, were synthesized from N-Cbzvalaciclovir by N-alkylation with methyliodide and ethyliodide respectively to give N-Cbz-N-methylvalaciclovir or N-Cbz-N- ethylvalaciclovir, which were subjected to deprotection catalyzed by Pd/C. It is an improved method for the N-alkylation of sterically hindered N-Cbzamino acid derivatives.
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2012年第12期974-976,共3页 Chinese Journal of Pharmaceuticals
关键词 伐昔洛韦 抗病毒药 有关物质 合成 valaciclovir antiviral agent related substance synthesis
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