Abstract In support of a research program aimed at discovering purine-related anticancer drug candidates, a method for the 14 C-labeling of pyrazolopyrimidines utilizing the readily available labeled starting material, sodium [14 C] formate, has been developed with a good overall yield. This new method was proven to be general in the preparation of other related [4.3. 0] heterocycles containing N, O, and S atoms. A concise synthesis of a model ...