ABSTRACT
Fluorine-containing molecules are of particular interest in the elds of biomedicine, agriculture, and material sciences.1 Over the past decade, with the progress of uorine chemistry research and in-depth understanding of uorine atoms and uorine substituent groups,2 drug discovery scientists are continuing to utilize uorinated molecules as therapeutic agents (Scheme 9.1).3 The latest statistics show that the current global annual sales of uorine-containing drugs at about US$40 billion; among 200 of the world’s top-selling drugs, uorinated drugs accounted for 29, having total sales of $32 billion.4 It is estimated that 25%–30% of new drug development programs are based on the uorine chemical raw material. Fluorine remains an important element in blocking metabolic activity, altering chemical properties and has been used as a functional group. According to the literature, about 15%–20% of the new drug candidate compounds contain a uorine atom or a triuoromethyl group. Based on our statistics,5 a total of 163 listed uorinated drugs will have been approved by the FDA by the end of 2013, indicating that other than the chlorine atom, the uorine atom is the second most utilized halogen atom selected by pharmaceutical chemists.6 Drug research which utilizes structure-activity relationship (SAR) methodology in tuning molecules as potential drugs coupled with the ready availability of uorinated intermediates has provided a huge boost in drug discovery.
