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Pyrazolo[3,4-d]pyrimidines are substances that found applications in medical practice (allopurinol) and have a number of biological activities: antimicrobial, antiinflammatory, anticancer, etc. Methods of synthesis, including both variants of pyrazole nucleus annulation by pyrimidine ring and pyrimidine nucleus by pyrazole ring, chemical and biological properties of pyrazolo[3,4-d]pyrimidine, and methods of their synthetic usage for the construction of synthetic polycyclic systems have been analyzed and generalized in the review.