The Rh(II)-catalyzed formal [3+2] and [3+3] cycloadditions of 1-tosyl 1,2,3-triazoles with 2H-azirines have been developed, which enable the efficient synthesis of polysubstituted 3-aminopyrroles and 1,2-dihydropyrazines, respectively. The reported [3+2] cycloaddition represents the first application of 1-sulfonyl 1,2,3-triazole as a [2C]-component in relevant cycloaddition reactions.

2-Phenyl-1-(3?,5?-dichloro-2?-benzo(b)thiophenoylamino)-4-arylidine-5-imidazolones (2a-j) were prepared from the 2-hydrazinocarbonyl-3,5-dichlorobenzo[b]thiophene 1 by the reaction with different oxazolinone which were prepared by the condensation of substituted benzaldehyde with benzoyl glycine in presence of sodium acetate and acetic anhydride. Reaction of 1 with different aromatic isothiocya...

Substituted 1, 2, 4- Triazoles have shown multiple biological activities such as anti-inflammatory, anti fungal, etc. 5-mercapto triazoles were prepared from the potassium dithiocarbazinates. These triazoles were used for preparation of different derivatives by two different schemes. In the first scheme the Mannich bases were prepared from 5- marcapto-s triazole Quinazolines. The 5-Marcato-s-Tr...

In this paper we present the room temperature synthesis of a novel serie of 1,4-disubstituted-1,2,3-triazoles 4a-l by employing the (3+2) cycloaddition reaction of pyrimidinones containing alkyne functions with different model azides in the presence of copper sulphate and sodium ascorbate. To obtain the final triazoles, we also synthesized the major precursors 6-amino-5-cyano-1,4-disubstituted-...

The reactivity of 2-benzyl-1,2,3-triazole in palladium-catalyzed direct arylation was studied. reaction conditions for the selective synthesis 2-benzyl-4-aryl-1,2,3-triazoles moderate to high yields using phosphine-free Pd(OAc)2 catalyst and inexpensive KOAc base have been found. Then, from these 4-aryl-1,2,3-triazoles, C?H bond functionalization C5-position allowed corresponding 4,5-diarylated...

Objective(s) Inhibitors of p38 MAP kinase are considered as suitable target in the treatment of inflammatory diseases such as rheumatoid arthritis and bowel inflammatory diseases. The development of 5-alkylthio-1-aryl-2-(4-pyridinyl) triazoles as inhibitors of p38 MAP kinase is described. These are analogues of 4- pyridinyl imidazole p38 MAP kinase inhibitor reported by Merck Research Laborator...

Electron deficient azides are challenging substrates in CuAAC reactions. Particularly, when N-carbonyl azides are applied the formation of N-carbonyl triazoles has not yet been observed. We report herein the first example of this class of reaction, with a copper-based system that efficiently enables the synthesis of N-carbamoyl 1,2,3-triazoles by [3+2] cycloaddition of N-carbamoyl azides and al...

The feasibility of trapping the vinyl copper intermediate generated in situ from azide-[3 + 2] cycloadditions and viability of employing these triazoles as unique templates for ring-closing metathesis are described here; this work effectively combines the two powerful reactions for the first time to construct various de novo fused and bridged triazoles that are otherwise not trivial to synthesize.

1,2,3-Triazoles are an important class of heterocycles, which display very large spectrum of biological activities and are widely used as pharmaceuticals and agrochemicals. Compounds containing 1,2,3-triazoles have also found industrial applications as corrosion inhibitors, lubricants, dyes, and photostabilizers. As such, the development of new and more general methods for their preparation is ...