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Purine nucleosides have significant importance and pivotal effects in medicinal chemistry. As part of our program of research on the synthesis of purine analogs and other antimetabolites. We have previously reported several new approaches for the synthesis of mercaptopurine analogs and their thioglycosides, these ring systems are interesting because they are purine analogs and as such they have useful properties as antimetabolites in purine biochemical reactions. The aim of this book was to address the use of recent reported purine nucleosides in drug discovery and development. Following the enormous developments in the novel synthetic strategies of the purine nucleosides, we surveyed the most recent and up-to-date synthetic approaches of the purine nucleosides that reflect its comprehensive importance in the different fields. Consequently, the new insights of a broad array of novel compounds have been demonstrated. The biological evaluation of the novel synthesized compounds were emphasized. Their synthetic procedures were also elaborated.