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.

Fluconazole based novel mimics containing 1,5-disubstituted 1,2,3-triazoles were synthesized by using Ru catalysed 1,3 dipolar cycloaddition. All the newly synthesized compounds and pure enantiomers were more potent than fluconazole against Candida albicans. Docking of 9A and 9B showed different conformation in the active site of Cyp51 of Candida albicans. The more active compounds 2 and 2A did not exhibit any toxicity up to 3.12 mg mL À1 against mammalian cell line L929.

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Ao ne-pot procedure fort he synthesis of 1,4-disubstituted 1,2,3-triazoles by at hree-component reactiono f allyl or benzyl halides, sodiuma zide, and terminal alkynes over an eutral alumina-supported copper iodide catalyst has been developed. The products were isolated by simple filtration followed by washing of the catalystw ith acetone. The products were obtained in almost pure form in up to 98 % yield (TON 495). The catalystc an be recycled for more than eight subsequent reactions. The halides are directly converted into triazoles via in situ formation of azides and thus han-dling of hazardousa zides can be avoided. The broad scope of this protocol is shown by the synthesis of av ariety of diverselys ubstituted 1,2,3-triazoles and also two-component azide-alkyne click reaction. The key features of this procedure are the use of water as as olvent, recyclability of the catalystu pt oe ight runs without appreciable loss of activity, and high yields of products.T he catalysth as been fully characterized by FTIR, solid-state NMR and EDX spectroscopy, ESEM, TGA, and XRD.[a] S.

The sp3 C–H alkylation of 9H-fluorene using alcohol and a Ru catalyst via the borrowing hydrogen concept has been described. This reaction was catalyzed by the [Ru­(p-cymene)­Cl2]2 complex (3 mol %) and exhibited a broad reaction scope with different alcohols, allowing primary and secondary alcohols to be employed as nonhazardous and greener alkylating agents with the formation of environmentally benign water as a byproduct. A variety of 9H-fluorene underwent selective and exclusive mono-C9-alkylation with primary alcohols in good to excellent isolated yield (26 examples, 50–92% yield), whereas this reaction with secondary alcohols in the absence of any external oxidants furnished the tetrasubstituted alkene as the major product. Furthermore, a base-mediated C–H hydroxylation of the synthesized 9H-fluorene derivatives afforded 9H-hydroxy-functionalized quaternary fluorene derivatives in excellent yield.