Title:Recent Innovations of Organo-fluorine Synthesis and Pharmacokinetics
Volume: 25
Issue: 21
Author(s): Omkar Kamble, Ramababu Dandela*Sandip Shinde*
Affiliation:
- Department of Industrial and Engineering Chemistry, Institute of Chemical Technology, Indian Oil Odisha Campus, Samantpuri, Bhubaneswar,India
- Department of Industrial and Engineering Chemistry, Institute of Chemical Technology, Marathwada Campus, Jalna,India
Keywords:
Fluorine, pharmacokinetics, heterocyclic, phase transfer catalyst, organic synthesis, nucleophilic substitutions, halogenations,
pharmaceuticals, fluorination.
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.