Fluorine in MedicinalChemistry and ChemicalBiologyEdited by Iwao Ojima.

Wiley, Hoboken 2009, 640 pp., hardcover$ 219.99.—ISBN 978-1-4051-6720-8

The field of fluo-rine incorporationinto organic com-pounds in drugdiscovery as wellas for exploratoryresearch in chemi-cal biology ismoving rapidly.With the availabil-ity of many newsynthetic reagentsand methods for the ready incorporationof fluorine or F-containing groups, manynew structure- or property-based con-cepts have been explored in recentyears. Iwao Ojima is to be commendedon a successful effort in bringing togeth-er many authors from diverse applicationfields in chemical biology and medicinalchemistry to put together a refreshingand comprehensive update of this im-portant field.

The book starts with an overview ofkey aspects of the physicochemical andstructural properties of fluorine-contain-ing organic compounds, their intermo-lecular interactions, and applications inMRS and PET imaging. This introductorychapter provides an insightful appetizerfor the remaining book, which is struc-tured into three sections on diverse con-

cepts and applications of fluorine incor-poration in medicinal chemistry (6 chap-ters), on advances in synthetic method-ologies (7 chapters, including one on theincorporation of 18F for radiopharmacolo-gy), and on applications of fluorinatedamino acids and peptides in chemicalbiology and pharmacology (5 chapters).

Each chapter is succinct and wellwritten, displaying modern F-organicchemistry in the context of pharmaceuti-cally interesting applications, touchingdiverse aspects of properties and phar-macology, structure and conformation,spectroscopy, and synthetic challenges,as well as medical and diagnostic appli-cations. In this way, the editor has suc-ceeded in putting together a appealingreview of diverse F-organic chemistry,triggering interest by concepts and ap-plications, rather than just assembling adry encyclopedic list of methods andcompounds.

This book is not intended for thosewho want to look up some specific re-agents or conditions for incorporating F-containing groups in a systematic com-pendium of reagents and reactions.Rather this book serves as an excellenteye opener for all those who know (ordo not yet know) about the importanceof F-organic chemistry and would like toget a stimulating and enjoyable updateor refresher on modern methods andapplications in the diverse fields of F-or-ganic medicinal or biological chemistry.

For the more systematically orientedreader, the book offers two appendicesin which all F-containing drugs forhuman and veterinary use are listed to-

gether with their drug names, systematicnames, structural formulae, therapeuticuses, mode of application, CAS-numberfor quick reference, and drug sponsor orcommercial producer(s). One little deficitin these two lists is the fact that theycontain only compounds for use in theUS (as approved by the FDA), ratherthan more generally in the world, partic-ularly in Europe. Thus, quite a number ofdrugs that have been in use in Europe(but not the US) cannot be found. Thus,the reader finds some 140 compoundsfor human use and some 40 compoundsfor veterinary applications, whereasthere appear to be over 210 drugs suc-cessfully launched for human use world-wide. However, this book does notintend to give a comprehensive list of allF-containing drugs, and the list of US-available drugs is perfectly suited to pro-vide a good overall impression of bothrecurrent and less common F-containingstructural motifs. Random checks onsome 10 % of all compounds listed indi-cate that the authors did a careful job inwriting clean structures with correct ste-reochemistry.

In summary, this is an excellent bookon modern F-organic chemistry and di-verse applications in drug discovery andbiological chemistry; it is highly recom-mended for anyone wishing to get acompetent update on the current stateof the art in this important and rapidlymoving field.

Klaus M�llerHoffmann–La Roche, Basel (Switzerland)DOI: 10.1002/cbic.200900409

2114 www.chembiochem.org � 2009 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim ChemBioChem 2009, 10, 2111 – 2114