The most electronegative element, fluorine, with an atomic size close to that of hydrogen, imparts unique, and often unpredictable, characteristics to the molecules containing the element. The study of fluorine-containing molecules, which began as a new area of research almost half a century ago, has become one of the most important and mature areas of science. Today, fluorine-containing molecules are prominent in all branches of chemistry, particularly in agro-, materials and medicinal chemistry. The importance of fluorine chemistry was recognized early (1963) by the American Chemical Society, with a technical division dedicated to fluorine. Indeed, to date, this is the only chemical element with a separate division. The Royal Society of Chemistry followed suit with a Fluorine Subject Group in 2001 and efforts are underway to initiate a similar group in Japan.
It is estimated that almost 20% of all pharmaceuticals on the market and 30% of agrochemicals contain at least one fluorine atom Citation[1]. The high lipophilicity of fluorine aids the biological transportation and distribution of such compounds. The modified metabolic and excretion rates of these molecules also allow longer action on the substrate or receptor of interest. In addition, the 18F isotope plays a very important role in PET.
An increasing number of publications in organic chemistry-related journals exploit the chemistry of fluoro-organic molecules. This richness is also evidenced by an increasing number of books and reviews Citation[2–6]. It has become common practice among medicinal chemists to ‘fluorine-scan’ (study the effect of fluorine substitution) before arriving at lead compounds. Two recent reviews provide deeper insights into the importance of this fascinating atom to pharmaceutical science Citation[7,8].
It highly appropriate that the first thematic issue of this exciting new journal should be dedicated to the topic of ‘Fluorine in Medicinal Chemistry’, and it is my pleasure and privilege to act as Guest Editor. This issue was conceived on the back of the considerable interest generated for a special symposium with the same title during the 19th Winter Fluorine Conference in St Petersburg Beach, FL, USA, in January 2009. It is our great pleasure to present this issue during the 19th International Symposium on Fluorine Chemistry that will be held in Jackson Hole, WY, USA, in August 2009.
In this issue
We are extremely pleased that one of the pioneers in this area, Robert Filler, has contributed the issue’s lead article entitled ‘Fluorine in medicinal chemistry: a century of progress and a 60-year retrospective of selected highlights’. I direct the reader to this article for a captivating account of past achievements and the current state of the field. One can only appreciate the growth that has occurred in this area by looking back at the monograph entitled ‘Carbon-fluorine compounds – chemistry, biochemistry and biological activities’, which was coedited by Robert Filler and Yoshiro Kobayashi back in 1982 Citation[9]. Their efforts a quarter century ago gave an impetus that led to a number of special symposia, reviews and other publications.
We have assembled a remarkable group of leaders in fluorine chemistry from around the world and their contributions for the success of this issue are much appreciated. A quick look at the topics covered will provide a hint of the wide influence of fluoro-organic chemistry: it is truly at the interface of various topics in organic, biological and medicinal chemistry, such as enantio- and stereo-selective synthesis, novel methodology development, drug development in neurochemistry, cancer research and enzyme inhibitors.
I wish all of our readers a fabulous future with fluorine!
Acknowledgements
P Veeraraghavan Ramachandran is very grateful for the interest of Iwao Ojima (State University of New York at Stony Brook, USA), Senior Editor of Future Medicinal Chemistry.
Financial & competing interests disclosure
The author has no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.
No writing assistance was utilized in the production of this manuscript.
Additional information
Funding
Bibliography
- Ojima I . Fluorine in Medicinal Chemistry and Chemical Biology. Wiley-Blackwell, Oxford, UK (2009).
- Gakh A , KirkKL. Fluorinated Heterocycles. Oxford University Press, UK (2008).
- Uneyama K . Organofluorine Chemistry. Blackwell, Oxford, UK (2006).
- Soloshonok VA , MikamiK, YamazakiT, WelchJT, HonekJ. Current Fluoroorganic Chemistry: New Synthetic Directions, Technologies, Materials, and Biological Applications. Oxford University Press, UK (2007).
- Kirsch P . Modern Fluoroorganic Chemistry: Synthesis, Reactivity, Applications. John Wiley, Sussex, UK (2004).
- Filler R , KobayashiY, YagupolskiiLM. Organofluorine in Medicinal Chemistry and Biochemical Applications. Elsevier, USA (1993).
- Muller K , FaehC, DiederichF. Fluorine in pharmaceuticals: looking beyond intuition.Science317, 1881–1886 (2007).
- Hagmann WK . The many roles of fluorine in medicinal chemistry.J. Med. Chem.51(15), 4359–4370 (2008).
- Filler R , KobayashiY. Biomedicinal Aspects of Fluorine Chemistry. Elsevier, USA (1982).