Xanthine and its derivatives are considered a pharmacologically potential moiety that manifests immense biological activities. Owing to this much diversity in the biological field, this scaffold has fascinated the attention of many researchers around the globe to scrutinize its basic structure chemically as well as biologically. In recent years, xanthine derivatives have been used therapeutically in different pathological conditions due to their presence in day-to-day life. Herein, we review the recent progress in the synthesis of xanthine and its derivatives. Some of the widely used synthetic strategies such as (a) Traube's synthesis, (b) one-pot synthesis, (c) xanthine-anneleated synthesis, and (d) miscellaneous synthesis were compiled in this review paper. The results obtained from this review paper highlight the significance of various xanthine derivatives as possible leads to the development of new drugs. The data compiled in this review paper could help the medicinal chemist in designing new active compounds from the modification of the already existing compounds in the search for novel drug leads. This report concludes that the various synthetic procedures exemplified in this review paper may serve as a support system for the designing of new molecules with a xanthine scaffold. Thus, we hope that this molecule may serve as the prototype in order to find out more active xanthine derivatives.
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