Abstract

A convenient method has been proposed for the preparation of new derivatives of adamantine-based drugs, such as memantine and rimantadine. The synthesis was performed by functionalization of amino-group of memantine and rimantadine by ipso-substitution of cyano-group at C⁵ position of 1,2,4-triazine scaffold with the corresponding aminoadamantane moieties with subsequent aza-Diels–Alder transformation of 1,2,4-triazine cycle into pyridine one in some cases.

中文翻译：

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作为有前途的候选药物的新型美金刚和金刚乙胺衍生物的合成

摘要

提出了一种制备金刚烷类药物新衍生物（例如美金刚和金刚乙胺）的简便方法。该合成是通过用相应的氨基金刚烷部分对1,2,4-三嗪支架的C ^{5位置上的氰基进行}原位取代，对美金刚和金刚乙胺的氨基进行官能化，随后进行 1 的氮杂-Diels-Alder 转化。 ,2,4-三嗪在某些情况下循环成吡啶一。