ChemInform Abstract: The Acylation of 4‐Amino‐4,5‐dihydro‐1H‐1,2,4‐triazol‐5‐ones.

Abstract

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Preparation, GIAO NMR Calculations and Acidic Properties of Some Novel 4,5-dihydro-1H-1,2,4-triazol-5-one Derivatives with Their Antioxidant Activities

“…In this study, the structures of six new 3-alkyl(aryl)-4-( p -nitrobenzoylamino)-4,5-dihydro-1 H -1,2,4- triazol-5-ones ( 2a–f ) synthesized from the reactions of compounds 1a–f with p -nitrobenzoyl chloride were identified by using elemental analyses and IR, 1 H-NMR, 13 C-NMR and UV spectral data, and these obtained spectral values were seen as compatible with literature [2,4,7–14]. The newly synthesized compounds 2a–f were titrated potentiometrically with TBAH in four non-aqueous solvents such as acetone, isopropyl alcohol, tert -butyl alcohol and N,N -dimethylformamide of relative dielectric permittivity 20.6, 19.4, 12.0 and 36.7, respectively.…”

“…1,2,4-Triazole and 4,5-dihydro-1 H -1,2,4-triazol-5-one derivatives are reported to show a broad spectrum of biological activities [1–6], and several papers have devoted with the synthesis of acyl derivatives of 4,5-dihydro-1 H -1,2,4-triazol-5-one derivatives [2,4,7–12]. In addition, it is known that 1,2,4-triazole and 4,5-dihydro-1 H -1,2,4-triazol-5-one rings have weak acidic properties, so that some 1,2,4-triazole and 4,5-dihydro-1 H -1,2,4-triazol-5-one derivatives were titrated potentiometrically with tetrabutylammonium hydroxide in non-aqueous solvents, and the p K a values of the compounds were determined [2,13,14].…”

Synthesis and pancreatic lipase inhibitory activities of some 1,2,4‐triazol‐5(3)‐one derivatives

“…[9][10] Additionally, a number of marketed drugs containing 1,2,4-triazole ring such as anastrozole and letrozole (to treat breast cancer); fluconazole, itraconazole, and vorozole (to treat fungal infections); ribavirin (to treat respiratory syncytial virus); etoperidone and nefazodone (to treat depression); and rizatriptan (to treat migraine headaches) have been used in clinic. [11][12][13][14][15][16][17] On the other hand, 1,2,4-triazole-5(3)-ones are azoleclass compounds that are generally obtained either by reactions of ester etoxycarbonyl hydrazones with ammonia and derivatives or by ring closure of semicarbazides in the basic medium. [18,19] The chemistry of these compounds studied in detail by Ikizler and coworkers were reported to be good nucleophiles in most reactions.…”

“…On the other hand, 1,2,4‐triazole‐5(3)‐ones are azole‐class compounds that are generally obtained either by reactions of ester etoxycarbonyl hydrazones with ammonia and derivatives or by ring closure of semicarbazides in the basic medium. [ 18,19 ] The chemistry of these compounds studied in detail by Ikizler and coworkers were reported to be good nucleophiles in most reactions. [ 20 ] Because of these properties, some 4‐arylidenamino and 4‐acylamino derivatives have been synthesized via nucleophilic attack of amino nitrogen at position 4 on the 1,2,4‐triazol‐5‐one ring.…”

“…[ 20 ] Because of these properties, some 4‐arylidenamino and 4‐acylamino derivatives have been synthesized via nucleophilic attack of amino nitrogen at position 4 on the 1,2,4‐triazol‐5‐one ring. [ 18,20–24 ] In addition, N‐ethyl acetate derivatives were obtained via nucleophilic attack of N‐1 on the 1,2,4‐triazol‐5‐one ring. Synthesized ethyl acetate derivatives were used as the starting material in the synthesis of a lot of heterocyclic compounds that have various biological properties.…”