A method for the preparation of novel pyrimido[1,2-a][1,3,5]triazin-6-one derivatives functionalized in positions 2, 4, and 7 of the ring was developed. Diversity in the derivatization of the pyrimido[1,2-a][1,3,5]triazin-6-one scaffold was successfully achieved by the introduction of substituents into positions 2 and 7 via two complementary approaches for the synthesis of key intermediates viz. pyrimidinylguanidines. Variations in position 4 of the pyrimido[1,2-a][1,3,5]triazine ring were made available by the regioselective introduction of various substituents via the triazine ring closure with corresponding aldehydes. The scope of the method was illustrated by the preparation of a library of 66 pyrimido[1,2-a][1,3,5]triazin-6-ones, which was demonstrated to be a source for new selective anticancer agents. Tautomeric preferences and anticancer properties were also explored for the prepared compounds.

中文翻译：

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有效合成2,4,7-三取代的嘧啶[1,2- a ] [1,3,5]三嗪-6-酮

开发了一种制备在环的2、4和7位官能化的新型嘧啶并[1,2- a ] [1,3,5]三嗪-6-衍生物的方法。嘧啶并[1,2- a ] [1,3,5]三嗪-6-一个骨架的衍生化多样性是通过两种互补方法将取代基引入位置2和7来合成关键中间体而成功实现的即 嘧啶基胍。嘧啶并[1,2- a ] [1,3,5]三嗪环第4位的变化可通过以下方法实现：三嗪与相应的醛一起闭环。该方法的范围通过制备66个嘧啶并[1,2- a ] [1,3,5] triazin-6- one的文库进行了说明，事实证明该文库是新的选择性抗癌药的来源。还研究了所制备化合物的互变异构偏好性和抗癌特性。