In order to study the influence of the length of the amino acid chain of N,N-phthaloyl-amino acid amides as analogues of the former anticonvulsant taltrimide on the seizure-antagonizing activity glycine, beta-alanine and gamma-aminobutyric acid (GABA) derivatives were synthesized. The corresponding taurine derivatives were also included. Generally, the glycine-derived amides showed a higher act...

The decomposition of 5-benzhydryl-1H-tetrazole in an N-methyl-2-pyrrolidone/acetic acid/water mixture was investigated under a variety of high-temperature reaction conditions. Employing a sealed Pyrex glass vial and batch microwave conditions at 240 °C, the tetrazole is comparatively stable and complete decomposition to diphenylmethane requires more than 8 h. Similar kinetic data were obtained ...

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.

This research included synthesizing a series of heterocyclic compounds where the compound 2-chloroacetohydrazide was synthesized from ethyl chloroethanoate with Hydrazine hydrate 95%. The reaction carried out in cold condition. 2-(pyrimidin-2-ylamino)acetohydrazide prepared by A1 2-amino pyrimidine absolute ethanol using Potassium hydroxide (KOH); then 2-(pyrimidin-2-ylamino) acetohydrazide dif...

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...

A 405 nm light-activatable terthiophene-based tetrazole was designed that reacts with a fumarate dipolarophile with the second-order rate constant k2 exceeding 10(3) M(-1) s(-1). The utility of this laser-activatable tetrazole in imaging microtubules in a spatiotemporally controlled manner in live cells was demonstrated.

The synthesis of 3-amino-1-nitroguanidine (3-ANQ) and 5-hydrazino tetrazole (5-HT) derivatives as new energetic materials are described. Reaction of 3-ANQ with triethyl orthoformate leads to the formation of 3-nitramino triazole while no reaction was observed whit 5-HT. Addition of NaN3 to a mixture of 3-ANQ and triethyl orthoformate, afforded 1-nitroguanidyl tetrazole in excelle...

A tetrazole ring is often used in drug discovery as a replacement for the carboxylic acid group. Previous work indicates that compounds containing a tetrazole moiety show asymmetric permeability in Caco-2 cells characteristic of an efflux transporter substrate. The aim of this study is to determine which transporters are responsible for polarization of transport of tetrazole-containing compound...