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Drug Design Strategies, Modes of Action, Synthesis and Industrial Challenges Behind Trifluoromethylated New Chemical Entities
Medicinal plants have been an inspiration source for developing new chemical entities,providing diverse chemical structures and modes of action for medicinal chemistry strategies.
Modern medicinal chemistry approaches promote functional group changes to improve NCE’sbiological activity. Incorporating the trifluoromethyl (-CF3) group into organic compounds iscrucial in modern drug design. It may affect the compound's lipophilicity, solubility, stability,molecular conformation, and pKa, changes that may lead to the discovery of new medicinesto treat diseases of our times. For this reason, this chemical transformation is currently ahot topic in the organic chemistry field. Chemists are competing to develop better methodsto carry out this transformation efficiently, less hazardously, and cost-effectively. The highnumber of annual scientific publications on trifluoromethylation evidences the competition.
This review profi les 21 trifluoromethylated New Chemical Entities (NCE) selected in December2020 from the GlobalData database, mainly in late stages of clinical trials (Phase II and III)or already in the commercial phase, containing one or two -CF3 groups in para or metapositions of benzene, or a pyridine ring. Synthetic approaches, therapeutic applications, andmanufacturing industrial challenges are provided.