The copper(I)-catalyzed 1,2,3-triazole-forming reaction between azides and terminal alkynes has become the gold standard of click chemistry due to its reliability, specificity, and biocompatibility. Applications of click chemistry are increasingly found in all aspects of drug discovery; they range from lead finding through combinatorial chemistry and target-templated in vitro chemistry, to proteomics and DNA research by using bioconjugation reactions. The triazole products are more than just passive linkers; they readily associate with biological targets, through hydrogen-bonding and dipole interactions. The present review will focus mainly on the recent literature for applications of this reaction in the field of medicinal chemistry, in particular on use of the 1,2,3-triazole moiety as pharmacophore.

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Review: ca. 200 refs.

A simple and efficient methodology has been described for the selective oxidation of secondary benzylic alcohols to the corresponding ketones. In contrast, primary benzylic alcohols afforded dimethyl acetals.

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Halogen compounds Q 0090One-Step Preparation of α-Chlorostyrenes. -Friedel-Crafts-type acylation of electron-rich arenes with aliphatic acid chlorides in the presence of iron silicate as the heterogeneous catalyst results in formation of α-chlorostyrenes along with the normal Friedel-Crafts products. Aromatic ketones gives the expected diarylketones under similar conditions. -(BORATE*, H. B.; GAIKWAD, A. G.; MAUJAN, S. R.; SAWARGAVE, S. P.; KALAL, K. M.; Tetrahedron Lett. 48 (2007) 28, 4869-4872; Div. Org.