3-Alkyl-5-phenyl-3H-[1,2,3]triazolo[4,5-d]pyrimidin-7(6H)-ones were prepared by nitrosative cyclization of the appropriate 5,6-diamino-2-phenylpyrimidin-4(3H)-ones with nitrous acid and were subjected to regioselective alkylation with several alkylating agents in aprotic solvent at different temperature. Simultaneous 6-N- and 7-O-alkylation were observed and the regioselectivity varied remarkably with size and shape of the alkylating agents as well as with the reaction temperature. Similarly, N- and O-alkylation as well as selectivity was also observed in the case of 2-phenyl-9-propyl-9H-purin-6(1H)-one. Some of the synthesized compounds showed moderate antiviral and antitumor activities.

中文翻译：

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3-烷基-5-苯基-3 H- [1,2,3]三唑并[4,5 - d ]嘧啶-7（6 H）-ones和2-苯基-的合成及区域选择性N-和O-烷基化9-丙基-9 H-嘌呤-6（1 H）-1具有抗病毒和抗肿瘤活性的评估

通过对合适的5,6-二氨基-2亚硝基环化制备3-烷基-5-苯基-3 H- [1,2,3]三唑并[4,5- d ]嘧啶-7（6 H）-一。 -亚苯基嘧啶-4（3 H）-亚硝酸，并在非质子溶剂中与几种烷基化剂在不同温度下进行区域选择性烷基化。观察到同时的6-N-和7-O-烷基化，区域选择性随烷基化剂的大小和形状以及反应温度而显着变化。类似地，在2-苯基-9-丙基-9 H-嘌呤-6（1 H）-一。一些合成的化合物显示出中等的抗病毒和抗肿瘤活性。