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Iodo-1,2,3-triazoles are of considerable interest for chemical and biomedical applications. However, current synthetic methods for preparing iodo-1,2,3-triazoles cannot easily be applied to the direct modification of bioactive molecules in water. Through the combination of water-compatible oxidative iodination and the copper-catalyzed alkyne-azide cycloaddition reaction, a novel copper-catalyzed aqueous multicomponent synthetic method for the preparation of 5-iodo-1,2,3-triazoles has been developed. The method is highly effective and selective for substrates including biologically relevant compounds with nucleoside, sugar, and amino acid moieties. Based on this aqueous tandem reaction, a direct single-step multicomponent dual modification of peptide is developed from readily available starting materials. Furthermore, the method could also be applied to concise and fast multicomponent radioactive 125 I labeling from an aqueous solution of commercially available sodium 125 iodide as a starting material.

Within a complex biological sample, the in situ sequential detection of multiple molecules without any interference is greatly desirable. Dual-functional nanoparticles are constructed, with the enzyme-based core-shell structures, for the in situ sequential detection of ATP and H2 O2 within the same biological system.

In a search for new probes to detect β-amyloid plaques in the brain of patients with Alzheimer′s disease, the radioiodinated quinoxaline derivative (I) is found to show specific labeling of Aβ plaques.

Wittig reaction of bithiophenecarbaldehydes (I) with triphenyl phosphonium ylides (II) yields the target styrylbithiophene derivatives (III).