CAS: 10444-89-0; 2-Amino-5-Trifluoromethyl-1,3,4-Thiadiazole

该化合物是一种杂环化合物,其特点是,在五人环结构中存在由两个氮原子和一个硫原子组成的三环环,与矿群相邻的碳相连的三氟甲基组(CF3)对其化学特性有重大影响,增强了其亲脂性和潜在生物活动;该化合物一般在室温下是固体,在极地有机溶剂中表现出中等溶解性;其独特的结构使其能够参与各种化学反应,使其在制药和农用化学等领域引起兴趣;该矿组的存在表明氢联结的潜力,可能影响其再活性以及与其他分子的相互作用;此外,三氟甲基组可产生独特的电子特性,使其在医药化学和材料科学中的潜在应用成为研究对象;由于氟化合物的存在,应观测安全性和处理预防措施,因为氟,它可能构成健康风险.

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25306-15-4 108-33-8 312524-33-7

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合成工艺路线路线简述

    📜2-(2,2,2-Trifluoroethylidene)Hydrazine-1-Carboximidothioic Acid置于iron(III) Chloride体系中,化学反应生成2-氨基-5-三氟甲基-1,3,4-噻二唑
    参考文献:新型短效催眠药hie-124的噻二唑[3,2-A ] [1,3]二氮杂analogue类似物的合成,生物学评价和分子建模研究
    标题:新型短效催眠药hie-124的噻二唑[3,2-A ] [1,3]二氮杂analogue类似物的合成,生物学评价和分子建模研究
    摘要:合成了一系列新的6,7-二氢-[1,3,4]噻二唑[3,2-A ] [1,3]二氮杂analogue类似物,并对其进行了生物学评估.与硫喷妥钠(6)相比,化合物gs-62(33)表现出强大的体内短效催眠活性,其起效时间,睡眠时间和治疗指数分别为6.4+/-0.2,94.8+/-5.3分钟,6.62 .维持剂量为6时,化合物33没有显示出任何急性耐受的迹象.同时33增强了6的体内催眠作用等摩尔量(0.06 Mmol)的组合分别显示起效和持续时间分别为7.5+/-1.3,62.5+/-5.9分钟.这种组合允许使用较低剂量的两种药物,以避免不良的副作用.对接研究揭示了非常好的相互作用和与gaba A受体的bdz结合位点的结合,尤其是与arg87,Arg149和thr151氨基酸残基的结合.
    Doi:10.1016/j.Ejmech.2016.08.038

    专利信息


    专利号:US-4412079-A
    优先权日:1968-03-13
    标题:Thiadiazole compounds and methods of using said compounds in agriculture
    发明人:CEBALO TONY; WALDE ROBERT A
    权利人:AIR PROD & CHEM
    摘要:Novel thiadiazole compounds are disclosed which contain in the 5 position, C-linked moieties which are either acyclic hydrocarbon radicals or halogenated acyclic hydrocarbon radicals (in which case each halogen is independently selected from F, Cl and Br). These novel compounds also contain an exocyclic nitrogen in the 2 position, and some of them contain the exocyclic substituent: wherein R3 is a lower acyclic hydrocarbon radical and R4 is either H or a lower acyclic hydrocarbon radical. Synthesis of these compounds is disclosed, including synthesis of those which exhibit isomerism and/or tautomerism. Various of these compounds have various agricultural utilities (e.g. as herbicides, insecticides, acaricides and fungicides), each of them having at least one such biological utility. Methods of using these compounds in phytotoxic fungicidal, acaricidal and insecticidal applications are disclosed.

    专利号:US-6743811-B2
    优先权日:1999-07-28
    标 题:Oxazalidinone compounds and methods of preparation and use thereof
    发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; GADWOOD ROBERT C
    权利人:UPJOHN CO
    摘要:Oxazolidinones and methods for their synthesis are provided. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. Oxazolidinones as disclosed herein can be readily synthesized and used in a variety of applications including use as antimicrobial agents. In one embodiment, a variety of thioamidomethyloxazolidinones and methods for their synthesis and use are provided.

    专利号:US-6531470-B1
    优先权日:1998-01-23
    标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation
    发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC
    权利人:UPJOHN CO
    摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.

    专利号:US-6562844-B2
    优先权日:1998-01-23
    标 题:Oxazolidinone combinatorial libraries, compositions and methods of preparation
    发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC
    权利人:UPJOHN CO
    摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.

    专利号:US-7002020-B1
    优先权日:1998-01-23
    标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation
    发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V
    权利人:UPJOHN CO
    摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.

    专利号:US-8318928-B2
    优先权日:2008-12-15
    标题 :Fused imidazole carboxamides as TRPV3 modulators
    发明人:CHAUDHARI SACHIN SUNDARLAL; ABRAHAM THOMAS; KADAM ASHOK BHAUSAHEB; DHONE SACHIN VASANTRAO; KADAM SURESH MAHADEV; KHAIRATKAR-JOSHI NEELIMA; KATTIGE VIDYA GANAPATI
    权利人:CHAUDHARI SACHIN SUNDARLAL; ABRAHAM THOMAS; KADAM ASHOK BHAUSAHEB; DHONE SACHIN VASANTRAO; KADAM SURESH MAHADEV; KHAIRATKAR-JOSHI NEELIMA; KATTIGE VIDYA GANAPATI; GLENMARK PHARMACEUTICALS SA
    摘要:The present invention provides transient receptor potential vanilloid (TRPV) modulators of formula (I). In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPV3. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPV3.

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    合成参考文献


    摘要:Collier, S. J., Science of Synthesis, (2004) 13, 403.
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