265657-43-0Relevant academic research and scientific papers
Synthesis of some 7H-s-triazolo[3,4-b]-1,3,4-thiadiazine derivatives
Dong, Heng-Shan
, p. 541 - 545 (2000)
The cyclization of 1-amino-2-mercapto-5-[5-methyl-1-(4-methylphenyl)-1,2,3-triazol-4-yl]-l,3,4- triazole with various α-haloketone in absolute ethanol yields 7H-3-[5-methyl-1-(4-methylphenyl)-l,2,3-triazol-4-yl]-6-substituted-s- triazolo[3,4-b]-1,3,4-thiadiazines and their structures are established by elemental analysis, MS, IR and 1H NMR spectral data.
Primary discovery of 1-aryl-5-substituted-1H-1,2,3-triazole-4-carboxamides as promising antimicrobial agents
Finiuk, Nataliya,Klyuchivska, Olha,Manko, Nazar,Matiychuk, Vasyl,Obushak, Mykola,Pokhodylo, Nazariy,Stoika, Rostyslav
, (2021/08/05)
Three series of novel 1H-1,2,3-triazole-4-carboxamides: 1-aryl-5-alkyl/aryl-1H-1,2,3-triazole-4-carboxamides, 1-aryl-5-amino-1H-1,2,3-triazole-4-carboxamides and 1,2,3-triazolo[1,5-a]quinazoline-3-carboxamides were synthesized via base-mediated click azide reactions. Compounds were evaluated for their antimicrobial activities against primary pathogens: Gram-positive and Gram-negative bacterial strains Escherichia coli, Klebsiella pneumonia, Acinetobacter baumannii, Pseudomonas aeruginosa, Staphylococcus aureus, as well as fungal strain Cryptococcus neoformans var. grubii and Candida albicans. Compounds exhibiting moderate to good activities were selected for SAR analysis. Several 5-methyl-1H-1,2,3-triazole-4-carboxamides 4d, 4l, 4r, showed potent antibacterial effect against S. aureus. On the contrary, 5-amino-1H-1,2,3-triazole-4-carboxamide 8b and [1,2,3]triazolo[1,5-a]quinazoline-3-carboxamide 9a were active against pathogenic yeast C. albicans. Thus, compound 4l under 1 μM demonstrated 50% growth inhibition against S. aureus. At the same concentration, the compound 9a killed approx. 40% of C. albicans cells. In general, these compounds demonstrated selective action and no significant impact on the viability of human keratinocytes of HaCaT line.
An integrated high-throughput strategy enables the discovery of multifunctional ionic liquids for sustainable chemical processes
Zhu, Anlian,Li, Lingjun,Zhang, Chi,Shen, Yutan,Tang, Mingjie,Bai, Lili,Du, Chunyan,Zhang, Suojiang,Wang, Jianji
supporting information, p. 307 - 313 (2019/01/28)
Development of new chemical processes with simplified reaction systems and work-up procedures is a challenging task. Although ionic liquids are a class of potential multifunctional compounds to simplify traditional chemical processes, their rational design is difficult due to complex interactions. In this work, a proof-of-concept strategy has been proposed to achieve an integration of high-throughput preparation of ionic liquids and in situ screening of their reaction-promoting performance in 96-well plates. The integrated approach then enables a facile identification of optimal ionic liquids from a 400-ionic liquid candidate pool to act as the solvent, the catalyst and the separating assistant, simultaneously, for carbonyl-azide cycloaddition reactions. Merits of the ionic liquids-based processes have been demonstrated not only in the convenient and efficient synthesis of 1,2,3-triazolyl compounds but also in the discovery of a new reaction for the chemical post-modification of free peptides.
Design, synthesis and anticancer activity evaluation of aziridine-1,2,3-triazole hybrid derivatives
Dong, Hong-Ru,Wu, Jian-Guo
, p. 109 - 112 (2018/04/25)
New 1-aryl-4-[(aziridine-1-yl)diarylmethyl]-5-methyl-1H-1,2,3-triazole derivatives 7a-i were synthesized by a one-pot reaction of diaryl-(1-aryl-5-methyl-1H-1,2,3-triazol-4-yl)methanols 6a-i derived from 1-aryl-5-methyl-1H-1,2,3-triazole-4-carboxylic acid
Regiospecific synthesis of 1,4,5-trisubstituted 1,2,3-triazoles via enolate-azide cycloaddition between 1,3-dicarbonyl compounds and aryl azides
Nelson, Ronald,Kesternich, Víctor,Pérez-Fehrmann, Marcia,Jaldin, Sally,Marcourt, Laurence,Christen, Philippe
, p. 453 - 457 (2016/08/13)
A cycloaddition reaction at room temperature between aryl azides and 1,3-dicarbonyl compounds in the presence of potassium carbonate in dimethylsulphoxide yielded 10 4-ethoxycarbonyl-1-aryl-5-methyl-1H-1,2,3-triazoles and seven other closely-related compounds. The 1,2,3-triazoles, nine of which are new, were obtained in good to high yields and only the 1,4-regioisomers were formed.
Efficient TMG catalyzed synthesis of 1,2,3-triazoles
Ahmadi, Fereshteh,Tisseh, Zeinab Noroozi,Dabiri, Minoo,Bazgir, Ayoob
, p. 1086 - 1090 (2013/12/04)
A practical and efficient method for the synthesis of 1,2,3-triazoles via the cycloaddition reaction of azides and CH-acids in the presence of 1,1,3,3-tetramethylguanidine (TMG) in ethanol at 30 C has been reported. The simple experimental procedure, shor
The synthesis and crystal structure of new bis(3-chlorophenyl)-[5-methyl-1- (4-methylphenyl)-1,2,3-triazol-4-yl]-methanol
Dong, Heng-Shan,Huo, Guo-Yong
scheme or table, p. 28 - 31 (2009/06/06)
The title compound bis(3-chlorophenyl)-[5-methyl-1-(4-methylphenyl)-1,2,3- triazol-4-yl]-methanol 8 has been synthesized and established by H NMR, IR and MS spectra and X-ray diffraction crystallography. Compound 8, C 23H29Cl2N3O, Mr = 424.31, crystallizes in the monoclinic space group P21/c with unit cell parameters a = 14.5402(6) A, b = 12.5888(5) A, c = 11.6510(5) A, α = 90°, β = 100.183°(2), γ = 90°, V = 2099.05(15) A3, Dx = 1.343 mg m-3 and Z = 4. The final R was 0.0514. The molecular conformation and packing is stabilized by interactions of intermolecular O1-H1...;N3′.
Synthesis of 3-[5-methyl-1-(4-methylphenyl)-1,2,3-triazol-4-yl]-6- substituted-s-triazolo[3,4-b]-1,3,4-thiadiazoles
Dong, Heng-Shan,Quan, Bin,Luo, Jin-Dong
, p. 1953 - 1956 (2007/10/03)
Several 3-[5-methyl-1-(4-methylphenyl)-1,2,3-triazol-4-yl]-6-substituted-1,3, 4-triazolo[3,4-b]-1,3,4-thiadiazoles have been synthesized and their structures established by elemental analysis and spectral data.
Synthesis of 3-[5-methyl-1-(4 -methylphenyl)-1,2,3-triazol-4 -yl]-6-aryl/heteroaryl-substituted-s-triazolo-[3,4-b] -1,3,4-thiadiazoles
Dong,Wei,Wang,Quan
, p. 81 - 88 (2007/10/03)
Several 3-[5-methyl-1-(4-methylphenyl)-1,2,3-triazol-4-yl]-6 -substituted-1,3,4-triazolo[3,4-b]-1,3,4-thiadiazoles have been synthesized and the structures of these compounds were established by elemental analysis. MS, IR, and 1H NMR spectral data.
Synthesis of 3-[5-methyl -1 -(4-methylphenyl)-1,2,3-triazol-4-yl]-6-substituted-s-triazolo[3,4-b]-1,3,4- thiadiazoles
Dong, Heng-Shan
, p. 343 - 346 (2007/10/03)
Several 3-[5-methy1-l-(4-methylphenyl)-l,2,3-triazol-4-yl]-6-substituted-l)3,4- triazolo[3,4-b]-l,3,4-thiadiazoles have been synthesized and the structures of these compounds were established by elemental analysis, MS, IR and 1H NMR spectral data.
