合成抗病毒药物更昔洛韦的高效一步法工艺

IF 1.7 4区 化学 Q3 CHEMISTRY, MULTIDISCIPLINARY
Vilas Sudrik, Dnyaneshwar Karpe, Vrushali Jadhav, Shamrao Lawande
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引用次数: 0

摘要

杂环嘌呤衍生物抗病毒药物更昔洛韦的一种新的区域选择性单锅合成方法,首先在碘(5%)存在下用乙酸酐处理鸟嘌呤,得到二乙酰鸟嘌呤中间体、在催化酸性 Amberlite IR-120 的存在下,中间体与 AMDP 发生原位 N-烷基化反应,得到 N-烷基化中间体,最后脱乙酰基得到纯的区域选择性更昔洛韦,该产品具有商业可行性且环保。图解摘要 我们开发了抗病毒药物更昔洛韦的一步法合成。首先,鸟嘌呤经乙酸酐和碘处理生成二乙酰鸟嘌呤 3。然后,该中间体在酸性 Amberlite IR-120 的存在下与 AMDP 反应,得到化合物 5。最后,去乙酰化得到更昔洛韦 1,这是一种商业上可行且环保的工艺。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Efficient one-pot process for synthesis of antiviral drug Ganciclovir

Efficient one-pot process for synthesis of antiviral drug Ganciclovir

A regioselective novel one-pot synthesis of heterocyclic purine derivative antiviral agent Ganciclovir in which initially guanine is treated with acetic anhydride in the presence of iodine (5%) to get diacetyl guanine intermediate, which undergoes in situ N-alkylation with AMDP in presence of catalytic acidic Amberlite IR-120 to get N-alkylated intermediate and finally deacetylation to get pure regioselective Ganciclovir, which is commercially viable and eco-friendly.

Graphical abstract

We developed one-pot synthesis of antiviral drug Ganciclovir. Initially, Guanine is treated with acetic anhydride and iodine to yield diacetyl guanine 3. This intermediate then reacted with AMDP in the presence of acidic Amberlite IR-120 to obtain compound 5. Finally, deacetylation yields Ganciclovir 1, a commercially viable and eco-friendly process.

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来源期刊
Journal of Chemical Sciences
Journal of Chemical Sciences CHEMISTRY, MULTIDISCIPLINARY-
CiteScore
3.10
自引率
5.90%
发文量
107
审稿时长
1 months
期刊介绍: Journal of Chemical Sciences is a monthly journal published by the Indian Academy of Sciences. It formed part of the original Proceedings of the Indian Academy of Sciences – Part A, started by the Nobel Laureate Prof C V Raman in 1934, that was split in 1978 into three separate journals. It was renamed as Journal of Chemical Sciences in 2004. The journal publishes original research articles and rapid communications, covering all areas of chemical sciences. A significant feature of the journal is its special issues, brought out from time to time, devoted to conference symposia/proceedings in frontier areas of the subject, held not only in India but also in other countries.
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