CHIRAL, FLUORINE-CONTAINING PHARMACEUTICALS(Review)

• Datum: 2025
• Автори та афіліації: Jianlin Han — Jiangsu Co-Innovation Center of Efficient Processing and Utilization of Forest Resources, College of Chemical Engineering, Nanjing Forestry University, Nanjing 210037, China; Alicja Wzorek — Institute of Chemistry, Jan Kochanowski University in Kielce, Uniwersytecka 7, 25-406 Kielce, Poland; Gagan Dhawan — School of Allied Medical Sciences, Delhi Skill and Entrepreneurship University, Dwarka, New Delhi-110077, India; Wei Zhang — Department of Chemistry, University of Massachusetts Boston, Boston MA 02125, Unites States;; Alexander Sorochinsky — Department of Fine Organic Synthesis, V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry, The National Academy of Sciences of Ukraine, 1 Murmanska str., Kyiv 02094, Ukraine; Daniel Baecker — Department of Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy, Freie Universität Berlin, Königin-Luise-Straße 2+4, 14195 Berlin, Germany; Taizo Ono — National Institute of Advanced Industrial Science and Technology, 463-8560, Nagoya, Japan; Karel Klika — Molecular Structure Analysis, German Cancer Research Center (DKFZ), ImNeuenheimer Feld 280, 69120 Heidelberg, Germany; Vadim Soloshonok — University of Basque Country
• Ключові слова: keywords
• Hauptverfasser: Han, Jianlin, Wzorek, Alicja, Dhawan, Gagan, Zhang, Wei, Sorochinsky, Alexander, Baecker, Daniel, Ono, Taizo, Klika, Karel, Soloshonok, Vadim
• Format: Artikel
• Sprache: Englisch
• Veröffentlicht: V.I.Vernadsky Institute of General and Inorganic Chemistry 2025
• Online Zugang: https://ucj.org.ua/index.php/journal/article/view/710
• Назва журналу: Ukrainian Chemistry Journal

Fluorine is a key element in drug design due to its ability to enhance metabolic stability, binding affinity, and bioavailability. Fluorine’s properties lead to more stable drugs with longer half-lives, reducing dosing frequency and improving patient compliance. Its small size and high electronegativity also improve binding affinity, resulting in more effective treatments with lower doses. For example, fluorine increases a compound’s ability to cross cell memb­ranes. This article highlights advancements in chiral, fluorine-containing pharmaceuticals introduced over the past five years, focusing on their synthesis, therapeutic benefits, mechanisms of action, and the impact of fluorine on efficacy and safety. Chiral molecules, essential in drug development, exist in two enantiomeric forms with distinct biological activities. Synthesizing chiral, fluorine-containing drugs involves techniques like asymmetric synthesis to produce pure enantiomers, resulting in drugs with increased potency, selectivity, and reduced side effects. Understanding their mechanisms of action provides valuable insights into efficacy and safety. Reviewing recently FDA-approved chiral drugs offers insights into fluorine chemistry in drug development and future therapeutic innovations. Recent FDA approvals highlight the significance of chiral, fluorine-containing drugs in various therapeutic areas, enabling targeted and effective treatments. Analyzing these approvals reveals trends shaping drug development’s future. The article also addresses the need for more research into self-disproportionation of enantiomers (SDE) in chiral, fluorinated compounds and concerns about excessive fluorine levels. SDE can affect pharmaceutical product purity. Research into SDE in fluorinated compounds ensures drug quality. Additionally, fluorine’s widespread use raises environmental and health concerns, necessitating studies on long-term effects and mitigation strategies.