Multicomponent reactions (MCRs) are not only a powerful tool for drug discovery, they also represent an excellent methodology for synthesis rationalization. Here we wish to illustrate the potential of MCRs in the production of generic drugs by synthesizing, in racemic form, the antiplatelet agent clopidogrel and the nonsteroidal antiandrogen bicalutamide, using Ugi, Petasis and Passerini reactions.
During the last decades, multicomponent chemistry has gained much attention in pharmaceutical research, especially in the context of lead finding and optimization. Here, in particular, the main advantages of multicomponent reactions (MCRs) like ease of automation and high diversity generation were utilized. In consequence of these beneficial properties, a plethora of new MCRs combined with appropriate classical reaction sequences have been published, the accessible chemical space was extended steadily. In the meantime, the desired high diversity became a challenge itself, because by now the systematic use of this huge and unmanageable space for drug discovery was limited by the lack of suitable computational tools. Therefore, this article provides an insight for the rational use of this enormous chemical space in drug discovery and generic drug synthesis. In this context, a short overview of the applied chemo informatics, necessary for the virtual screening of the biggest available chemical space, is given. Furthermore, some examples for recently developed multicomponent sequences are presented.
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