publication . Article . 2015

Recent advances in fluorination techniques and their anticipated impact on drug metabolism and toxicity

Cormac D. Murphy; Graham Sandford;
Open Access English
  • Published: 02 Mar 2015
  • Publisher: Taylor and Francis
  • Country: Ireland
Abstract
Introduction: Fluorine’s unique physicochemical properties make it a key element for incorporation into pharmacologically active compounds. Its presence in a drug can alter a number of characteristics that affect ADME-Tox, which has prompted efforts at improving synthetic fluorination procedures. Areas covered: This review describes the influence of fluorine on attributes such as potency, lipophilicity, metabolic stability and bioavailablility and how the effects observed are related to the physicochemical characteristics of the element. Examples of more recently used larger scale synthetic methods for introduction of fluorine into drug leads are detailed and th...
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free text keywords: Biotransformation, Fluorinating reagent, Organofluorine, Synthesis, Metabolic stability, Bond formation, Organic chemistry, Chemistry, Biochemical engineering, Drug production, Drug metabolism, Drug, media_common.quotation_subject, media_common
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