The nitrile imine-mediated tetrazole–ene cycloaddition is a widely used class of photoligation. Optimizing the reaction outcome requires detailed knowledge tetrazole photoactivation profile, which can only partially be ascertained from absorption spectroscopy, or otherwise involves laborious monitoring in solution. Photodissociation action spectroscopy (PDAS) combines advantages optical and mas...

An efficient synthesis of the angiotensin-II inhibitor valsartan (Diovan®) is presented. Directed ortho-metalation of 5-phenyl-1-trityl-1H-tetrazole (6) and its Negishi coupling with aryl bromide 5 are the key steps of the synthesis. This method overcomes many of the drawbacks associated with previously reported syntheses.

reaction of 5-phenyl tetrazole with ethyl chloroacetate to form ethyl (5-phenyl-1h-tetrazol-1-yl) acetate (1). compound 1 react with hydrazine hydrate in ethanol yield 2-(5-phenyl-1h-tetrazol-1-yl) acetohydrazide (2). the condensation of (2) with various aldehydes yield the corresponding substituted n'-[-arylidene]-2-(5-phenyl-1h-tetrazol-1-yl) acetohydrazide (3a- j). the compounds obtaine...

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)...

To evaluate the possibility of introducing azole nucleosides as building blocks for metal-mediated base pairs in artificial oligonucleotides, imidazole nucleoside, 1,2,4-triazole nucleoside and tetrazole nucleoside have been synthesized and characterized. The X-ray crystal structures of p-toluoyl-protected 1,2,4-triazole and tetrazole nucleosides are reported. Contrary to the situation primaril...

PURPOSE In the present study in vivo analgesic activity of some previously synthesized 1,2,4-triazole derivatives containing pyrazole, tetrazole, isoxazole and pyrimidine ring have been evaluated. METHODS Acetic acid induced writhing method and Hot plate method has been described to study analgesic activity of some 1,2,4-triazole derivatives containing pyrazole, tetrazole, isoxazole and pyrim...

The title compound, PNU-97018 [systemic name: 2-butyl-3,6,7,8,9,11-hexahydro-6,9-dimethyl-3-([2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl)-6,9-ethano-4H-imidazo[4,5-d]-pyridazino[1,2-a]pyridazin-4-one] is a newly developed angiotensin II receptor antagonist. The compound and its methanolate and ethanolate were characterized by X-ray crystallography and thermal analysis. The methanolate and...

(S)-2-(4-Chlorobenzoyl)-1,2,3,4-tetrahydrobenzo[e]pyrazino[1,2-a][1,4]diazepine-6,12(11H, 12aH)-dione was obtained in a three-step, one-pot synthesis, starting from optically pure (S)-2-piperazine carboxylic acid dihydrochloride. Selective acylation of the β-nitrogen atom followed by condensation with isatoic anhydride and cyclization with HATU/DIPEA to a seven-member benzodiazepine ring, led t...

Treatment of primary or secondary alcohols with 1-phenyl-1(H)-tetrazole-5-thiol and [Me(2)NCHSEt](+) BF(4)(-) leads directly and cleanly to 1-phenyl-1(H)-tetrazol-5-yl sulfides.

Energetic ionic salts of azotetrazolate (AT), iminobis(5-tetrazolate) (IBT) and 5, 5'-bis(tetrazole) (BT) were synthesized; 1-methyl-4-aminotriazolium azotetrazolate has a layered structure and exhibits a heat of formation of +4360 kJ kg(-1).