Abstract

The fluorinated compounds have significance in medicinal chemistry and pharmaceutical research. The introduction of fluorine atom in the heterocyclic compounds increases biological activity by favourable physiochemical interactions. The combination of heterocycles with fluorine substituents has a wide range of applications in the study of various pharmacological research. The compounds not only exhibit biological activity but have also shown unique physical and chemical characteristics features that open the new avenues for multidisciplinary research. Fluorine atom tolerance to maximal functional groups, simplicity in operation, replacing hydrogen with fluorine of bioactive molecules are more efficient for the synthesis of fluorinated compounds at the commercial level. The fluorine substitution also increases the binding affinity to the targeted protein. Furthermore, the incorporation of fluorine on the drug molecules helps in enhancing the polarity, increasing the rate of drug metabolism and improving metabolic stability. The pharmacokinetic study plays an important role in clinical research. In 1996, researcher Whitford found that the pharmacokinetics of fluorine is affected by pH and quantity in the bone study. The pH of organofluoride influences fluoride absorption, distribution, and excretion. It also increases the stability when bound to carbon atom, resulting in increased bioactivity. This is the primary reason that fluoride is a key component of around 25% of currently available active drugs for various diseases, including cancer, diabetes, HIV etc. Not only the pharmacokinetic properties but also the physical properties of the drug can be enhanced or altered by selective insertion at the key place of the fluorine atom in the drug candidate. In this report, we have studied and referred to the interesting research articles reported since 2000 for the synthesis of low fluorine substituted organic compounds for medicinal research and pharmacokinetic use, example neurological diseases, cancer, and tuberculosis research.

Keywords: Fluorine, pharmacokinetics, heterocyclic, phase transfer catalyst, organic synthesis, nucleophilic substitutions, halogenations, pharmaceuticals, fluorination.

Graphical Abstract