14064-62-1Relevant articles and documents
Design, synthesis and evaluation of 5-substituted 1-H-tetrazoles as potent anticonvulsant agents
Liao, Ai-Mei,Wang, Tiantian,Cai, Bangrong,Jin, Yi,Cheon, Seunghoon,Chun, Chang Ju,Wang, Zengtao
, p. 435 - 443 (2017/04/13)
Abstract: A series of 5-substituted 1-H-tetrazoles were designed and synthesized as potent anticonvulsant agents. Their preliminary anticonvulsant activities were evaluated using maximal electroshock and subcutaneous pentylenetetrazole (scPTZ) seizure tests. Neurotoxicity was determined using rotarod test. The results indicated that the compound 2j in scPTZ model exhibited the ED50 values of 83.3?mg/kg, superior to the standard drug ethosuximide with the maximum activity. In addition, compound 2k showed the most potent activity in MES model with ED50 value of 9.6?mg/kg and TD50 value of 189.5?mg/kg after intraperitoneal injection in mice, and displayed a high protective index (TD50/ED50) of 19.7 compared to reference antiepileptic drugs. Graphical Abstract: [Figure not available: see fulltext.]
An efficient and economical synthesis of 5-substituted 1 H -tetrazoles via Pb(II) salt catalyzed [3+2] cycloaddition of nitriles and sodium azide
Kant, Rama,Singh, Vishal,Agarwal, Alka
, p. 305 - 312 (2016/04/20)
A simple, mild and efficient method is developed for the synthesis of 5-substituted 1H-tetrazoles. Out of three used Pb(II) catalysts, lead chloride (PbCl2) has been found to be an efficient catalyst for [3+2] cycloaddition of NaN3 with aromatic and aliphatic nitriles to afford 5-substituted 1H-tetrazoles. The catalyst is reusable up to four cycles with consistent activity. The cost effectiveness and easy availability of the catalyst, simple methodology, excellent yield and easy work-up are the additional advantages.
OSU-6: A highly efficient, metal-free, heterogeneous catalyst for the click synthesis of 5-benzyl and 5-aryl-1H-tetrazoles
Nammalwar, Baskar,Muddala, Nagendra Prasad,Pitchimani, Rajasekar,Bunce, Richard A.
, p. 22757 - 22766 (2016/01/25)
OSU-6, an MCM-41 type hexagonal mesoporous silica with mild Br?nsted acid properties, has been used as an efficient, metal-free, heterogeneous catalyst for the click synthesis of 5-benzyl and 5-aryl-1H-tetrazoles from nitriles in DMF at 90 °C. This catalyst offers advantages including ease of operation, milder conditions, high yields, and reusability. Studies are presented that demonstrate the robust nature of the catalyst under the optimized reaction conditions. OSU-6 promotes the 1,3-dipolar addition of azides to nitriles without significant degradation or clogging of the nanoporous structure. The catalyst can be reused up to five times without a significant reduction in yield, and it does not require treatment with acid between reactions.