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Recent Innovations of Organo-Fluorine synthesis and pharmacokinetics

Author(s):

Omkar Kamble, Ramababu Dandela* and Sandip Shinde*  

Abstract:


The fluorinated compounds have significance in medicinal chemistry and pharmaceuticals research. The introduction of fluorine atom in the heterocyclic compounds increases biological activity, develops favourable physiochemical interaction. Combination of the heterocycles and fluorine substituent having large scope in the research work of the different drugs molecules. The compounds not only show biological activity but also show unique physical and chemical properties that open the doors of multidisciplinary research areas. Fluorine atom tolerance towards maximum functional groups, simplicity in operation, replacing hydrogen with fluorine of bioactive molecules are more efficient for the production at the commercial level. The fluorine substitution also increases the binding affinity to the targeted protein. Also, incorporation of fluorine into the drug helps to increase the polarity hence to increase the rate of drug metabolism and improves the metabolic stability. The pharmacokinetic study plays an important role in clinical research, since 1996, researcher Whitford discover that the pharmacokinetic of fluorine is depend on its pH and amount in the bone. pH of organofluoride governs the absorption, distribution and excretion of fluoride. It also increases the stability when binding with carbon atom and resulting in an increase in bioactivity. This is the main reason that around 25% of present active drugs on various diseases, including cancer, diabetes, HIV, etc. have fluorine as important content. Not only pharmacokinetic property but also the physical property of the drug can be enhanced or altered by selective insertion at the key place of the fluorine atom in the drug compound. In this report, we have summarized the interesting research article reported since 2000 for the synthesis of low fluorine substituted organic compounds for medicinal research and pharmacokinetic study of fluorine molecules in neurological diseases, cancer, and tuberculosis research.

Keywords:

Fluorine, Pharmacokinetics, Heterocyclic, Phase transfer catalyst, Organic synthesis, Nucleophilic Substitutions, Halogenations, Pharmaceuticals, Fluorination.

Affiliation:

Department of Industrial and Engineering Chemistry, Institute of Chemical Technology, Indian oil Odisha Campus, Samantpuri, Bhubaneswar, Department of Industrial and Engineering Chemistry, Institute of Chemical Technology, Indian oil Odisha Campus, Samantpuri, Bhubaneswar, Department of Industrial and Engineering Chemistry, Institute of Chemical Technology, Marathwada Campus, Ja



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