17 Results Found

The Ugi-azide MCR (UA) is one of the most efficient methods for the synthesis of 1,5-disubstituted-1H-tetrazoles (1,5-DS-T). Complex drug-like scaffolds incorporating tetrazoles have demonstrated a wide range of therapeutic benefits such as anti-infl...

A series of five novel bis-1,5-disubstituted-1H-tetrazoles (bis-1,5-DS-1H-T) were quickly prepared by a catalyst-free Ugi-azide repetitive process from easily accessible starting materials in excellent yields, either at room temperature (88%–95%) or...

A series of ten 1,5-disubstituted-1H-tetrazoles (1,5-DS-T) were synthesized via Ugi-azide isocyanide-based multicomponent reactions (IMCR) in low to good yields (30–85%), using propargyl amine or 2-azidobenzaldehyde as a component, and using ul...

The anticarcinogenic potential of a series of 1,5-disubstituted tetrazole-1,2,3-triazole hybrids (T-THs) was evaluated in the breast cancer (BC)-derived cell lines MCF-7 (ER+, PR+, and HER2−), CAMA-1 (ER+, PR+/−, and HER2−), SKBR-3...

A high-order multicomponent reaction involving a six-component reaction to obtain the novel linked 1,5-disubstituted tetrazole-1,2,3-triazole hybrids in low to moderate yield is described. This one-pot reaction is carried out under a cascade process...

A serie of 2-tetrazolylmethyl-2,3,4,9-tetrahydro-1H-β-carbolines were synthesized via a one pot Ugi-azide/Pictet–Spengler process under mild ultrasound-assisted conditions. The products containing two privileged heterocyclic frameworks: 1,5-disubstit...

1,5-disubstituted tetrazoles (1,5-Ds-T) are heterocyclic bioisosteres of the cis-amide bond, commonly found in bioactive compounds, pharmaceuticals, and functional materials. Chromones are privileged scaffolds widely present in natural products that...

The ongoing study is a Ugi-azide four-component reaction for the synthesis of 1,5-disubstituted tetrazole(1,5-DST), which involves an aldehyde, different amines, isocyanides, and as azide’s source the Trimethylsilylazide (TMSN3), in water as solvent...

Tetrazoles have been widely studied for their biological properties. An efficient route for large-scale synthesis of 1,5-disubstituted tetrazoles (1,5-DTs) is presented. The strategy exploits a reductive approach to synthetize a cyclic chiral imine s...

Bioisosteres of amide bonds such as 4,5-disubstituted-1,2,3-triazoles (4,5-DS-1,2,3-Ts) and 1,5-disubstituted tetrazoles (1,5-DST) are present in compounds with important biological activities like those that are antineoplastic, antibacterial, antifu...

A straightforward and reliable method for the regioselective synthesis of steroidal 1,4-disubstituted triazoles and 1,5-disubstituted tetrazoles via copper(I)-catalyzed cycloadditions is reported. Heterocycle moieties were efficiently introduced onto...

1,4- and 1,5-disubstituted tetrazoles possess enriched structures and versatile chemistry, representing a challenge for chemists. In the present work, we unravel the fragmentation patterns of a chemically diverse range of 5-allyloxy-1-aryl-tetrazoles...

A serie of novel 3-tetrazolylmethyl-4H-chromen-4-ones were synthesized via Ugi-azide reaction under mild ultrasound-assisted conditions (room temperature, EtOH, 10% mol ZnO nanoparticles). The products containing two privileged heterocyclic framework...

An eco-friendly methodology for the synthesis of novel Schiff base analogs of Raltegravir, an Integrase inhibitor drug is described. Pertinence of these imine derivatives is related to Medicinal Chemistry to develop new anti-VIH compounds. To our kno...

An efficient synthesis of alkyne-3-tetrazolyl-tetrazolo[1,5-a] quinolones via a one-pot isocyanide-based multicomponent reaction (IMCR) process: I-MCR Ugi-azide/SNAr/ring-chain azido tautomerization was performed under eco-friendly conditions. We rep...

An efficient one-pot synthesis of carborane-containing high-energy compounds was developed via the exploration of carbon–halogen bond functionalization strategies in commercially available 2,4,6-trichloro-1,3,5-triazine. The synthetic pathway f...

The non-estrogenic 2,5-disubstituted tetrazole core-bearing bisphenol structures (TbB) are being researched as emerging structural congeners of Bisphenol A, an established industrial endocrine disruptor. However, there is no understanding of TbB&rsqu...