N. D. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, Leninsky Prospect 47, 119991 Moscow, Russia.
Int J Mol Sci. 2023 Feb 2;24(3):2937. doi: 10.3390/ijms24032937.
Piperidines are among the most important synthetic fragments for designing drugs and play a significant role in the pharmaceutical industry. Their derivatives are present in more than twenty classes of pharmaceuticals, as well as alkaloids. The current review summarizes recent scientific literature on intra- and intermolecular reactions leading to the formation of various piperidine derivatives: substituted piperidines, spiropiperidines, condensed piperidines, and piperidinones. Moreover, the pharmaceutical applications of synthetic and natural piperidines were covered, as well as the latest scientific advances in the discovery and biological evaluation of potential drugs containing piperidine moiety. This review is designed to help both novice researchers taking their first steps in this field and experienced scientists looking for suitable substrates for the synthesis of biologically active piperidines.
哌啶是设计药物最重要的合成片段之一,在制药工业中起着重要作用。它们的衍生物存在于二十多类药物以及生物碱中。本综述总结了近年来关于导致各种哌啶衍生物形成的分子内和分子间反应的最新科学文献:取代的哌啶、螺哌啶、稠合的哌啶和哌啶酮。此外,还涵盖了合成和天然哌啶的药物应用,以及发现和生物评价含哌啶部分的潜在药物的最新科学进展。本综述旨在帮助刚涉足该领域的新手研究人员和寻找合成生物活性哌啶合适底物的经验丰富的科学家。