Chiral bioactive fluoroorganic compounds

During the past decade, there has been an increased emphasis on new approaches to chiral compoimds and asymmetric syntheses. This focus has been particularly pronounced in medicinal chemistry, where a specific enantiomer or diastereomer often exhibits enhanced therapeutic potency compared with the racemate. Organofluorine compounds have played a significant role in these advances. An earlier report emphasized a range of methods for the synthesis of chiral bioactive fluoroorganic compounds (1). Since the intent of this paper is to provide an overview which captures the scope and flavor of these recent developments, it seems quite appropriate to briefly cite the fascinating range of research studies of the other contributors to this book. 

Tetr 34 3 (1978) (Introduction of Fluorine into Organic Molecules Why and How) 47 5329 (1991) (The Combination of Hydrogen Fluoride with Organic Bases as Fluorination Agents) 49 9385 (1993) (Synthesis of Chiral and Bioactive Fluoroorganic Compounds)... 

For reviews see. (a) Welch, J. T. (1987) Tetrahedron report number 221 Advances in the preparation of biologically active organofluorine compounds. Tetrahedron, 43, 3123-3197. (b) Resnati, G. (1993) Synthesis of chiral and bioactive fluoroorganic compounds, Tetrahedron, 49, 9385-9445. (c) Soloshonok, V. A. (ed.) (1999) Enantiocontrolled Synthesis of Fluoroorganic Compounds Stereochemical Challenges and Biomedicinal Targets, John Wiley Sons, Ltd, Chichester, UK. (d) Rosen, T. C., Yoshida, S., Kirk, K. L. and Haufe, G. (2004) Fluorinated phenylcyclopropylamines as inhibitors of monoamine oxidases. ChemBioChem., 5, 1033-1043. 

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