Development of a new improved and efficient process suitable for the large-scale production of Irbesartan has been described. The key steps are tetrazole formation from secondary amide for the preparation of the key intermediate 1-Benzyl-5-(4'-bromomethyl-biphenyl-2-yl)-1H-tetrazole (9), N-alkylation and debenzylation.

Eleven oxytocin analogues substituted in position 4, 5 or 9 by tetrazole analogues of amino acids were prepared using solid-phase peptide synthesis method and tested for rat uterotonic in vitro and pressor activities, as well as for their affinity to human oxytocin receptor. The tetrazolic group has been used as a bioisosteric substitution of carboxylic, ester or amide groups in structure-activ...

A new activator for the coupling of phosphoramidites to the 5'-hydroxyl group during oligonucleotide synthesis is introduced. The observed time to complete coupling is twice as fast with 4, 5-dicyanoimidazole (DCI) as the activator, compared with 1 H -tetrazole. The effectiveness of DCI is thought to be based on its nucleophilicity. DCI is soluble in acetonitrile up to 1.1 M at room temperature...

Driven by an interest in the impact of para-substituent calix[4]arenes on metal complexation and structural chemistry, studies p-cyclohexylcalix[4]arene (L) have been carried out. The 1:1 dichloromethane dimethylformamide solvates were found to be isostructural, different typical bilayer structure often observed for p-t-butylcalix[4]arene solvates. methanol solvate, contrast, does form a bilaye...

Recently there has been increased interest in high nitrogen content “green” energetic materials which are designed to produce relatively non-toxic decomposition products as part of a push to decrease the environmental impact of energetic materials through all phases of their existence. With the use of a T-Jump/Time-of-Flight Mass Spectrometer (T-Jump/TOFMS) capable of high heating rates (up to ...

An improved procedure is described for the efficient and high-yield (76-91%) synthesis of nucleoside diphosphate sugars from the readily available nucleoside 5'-monophosphomorpholidate and sugar 1-phosphate in the presence of 1H-tetrazole. Comparative kinetic investigations by means of (31)P NMR spectroscopy with different additives (1,2,4-triazole, acetic acid, N-hydroxysuccinimide, 4-(dimethy...

A zeolite-like microporous tetrazole-based metal-organic framework (MOF) with 24 nuclear zinc cages was synthesized and characterized. It exhibits high CO(2) adsorption capacity up to 35.6 wt % (8.09 mmol/g) and excellent CO(2)/CH(4) selectivity at 273 K/1 bar, being among the highest values known to date. Theoretical calculations based on simulated annealing techniques and periodic DFT reveale...

Three novel tetrazole-based frustrated magnets, namely, Co3(OH)2(3-ptz)2(SO4)(H2O)4 (1), Co2(OH)(tzba)(H2O)4 (2) and [Co(OH)(tta)] (3) (3-ptz = 5-(3-pyridyl) tetrazole, H2tzba = 4-(1H-tetrazol-5-yl) benzoic acid, Htta = 1H-tetrazole) were hydrothermal synthesized and magnetically characterized. Compound 1 is a 2D (4,4) layered structure assembled by sulfate capped triangular [Co3(μ3-OH)(μ3-SO4)...