The problem of creating new effective domestic pharmacological preparations, including the development of the methods for obtaining biologically active substances in compliance with the “green chemistry” principles, are among the priority areas for the development of chemical science. The choice of an initial molecule, which carries the potential of biological activity, is the guarantor of a successful experimental search. Imidazole derivatives occupy a unique place in the medicinal chemistry. An imidazole cycle is part of the natural compounds such as histamine, biotin, some alkaloids and nucleic acids, and is a structural fragment of medicinal preparations. The goalof the present review is to analyze the publications on the chemistry of imidazole derivatives with an emphasis on the methods of obtaining biologically active and other practically useful molecules with an obligatory imidazole cycle. The objects of the study:imidazole derivatives. The examples of the routes of synthesizing imidazole derivatives, as well as the compounds of interest for the medicinal chemistry, agriculture, and other fields, which have been published in the scientific and technical literature since 2000, have been presented. Conclusion.The studies in the field of searching for new highly effective preparations among imidazole derivatives are relevant and promising. The most important stage in this search is the directed synthesis of the substances with the specified, practically useful properties. The range of new practically useful substances in the series of imidazole derivatives has been significantly expanded and replenished thanks to the modern modifications of the classical methods of their obtaining.