Abstract

The intramolecular cyclizations of 6-amino-5-(N-aryliminomethyl)-1,3-dimethyluracils (2) involving the N-N bond formation were effected via a hypervalent iodine oxidation using iodobenzene diacetate. This method enabled a facile synthesis of 2-aryl-5,7-dimethylpyrazolo[3,4-d]pyrirnidine-4,6(5H,7H)-diones (3) in moderate to excellent yields. The primary advantage of this N-N bond formation method is that various 2-aryl-substituted pyrazolo[3,4d]pyrimidines can be provided under mild oxidative conditions.

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