Synthetic approaches for the preparation of azolyl purine and azolyl purine nucleoside derivatives are reviewed. The title compounds are important in terms of medicinal and biological chemistry. Among others, the methodology regarding purine-azole conjugates includes SNAr reactions, cyclisation approaches on amino or hydrazinyl purines and transition metal catalyzed cross-coupling reactions. Azolyl purine derivatives are used as agonists and antagonists of adenosine receptors. They also possess useful levels of antiviral activities. Several compounds of this class exhibit fluorescent properties that can be successfully applied in biological chemistry. Also, chemical applications of azolyl purine derivatives as synthetic intermediates are discussed. The review summarizes the reported classes of purine-azole conjugates and indicates the groups of compounds yet to be synthesized.