共查询到19条相似文献,搜索用时 375 毫秒
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本文首先用5-(3-吡啶)-2H-四唑乙酰基酰肼与芳酰基异硫氰酸盐反应制备成化合物1-[5-(3-吡啶)-2H-四唑乙酰基]-4-芳酰氨基硫脲化合物1a~j, 然后用冰醋酸回流处理1a~j得到一系列化合物5-[5-(3-吡啶)-2H-四唑亚甲基]-2-芳酰氨基-1,3,4-噻二唑2a~j . 化合物1a~b在强碱介质中首先发生降解, 然后进行环化反应 . 相似文献
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本文通过5-(α-萘)-2H-四唑-2-乙酰肼(Ⅰ)与芳酰基异硫氰酸酯缩合制得16种新的1-[5-(α-萘)-2H-四唑-2-乙酰基]-4-芳酰基胺基硫脲(Ⅱ),(Ⅲ)在碱性催化条件下环化为3-[5-(α-萘)-2H-四唑-2-亚甲基]-4-芳酰基-1,2,4-三唑啉-5-硫酮(Ⅲ),化合物的结构经元素分析,IR、~1H NMR和MS鉴定,对化合物(Ⅲ)的质谱裂解进行分析,解释了化合物(Ⅱ)的环化方向,经初步筛选,发现个别化合物对小麦胚芽生长有促进作用。 相似文献
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本文合成了1-[5-(α-萘)-2 H-四唑-2-乙酰]-4-苯基氨基硫脲5,以及由5衍生的环化产物3-[5-(α-萘)-2 H-四唑-2-甲撑]-4-苯基-1,2,4-三唑啉-5-硫酮6,2-苯胺基-5-[5-(α-萘)-2 H-四唑-2-甲撑]-1,3,4-噻二唑7及2-苯胺基-5-[5-(α-萘)-2 H-四唑-2-甲撑]-1,3,4-(口恶)二唑8。它们的结构均通过元素分析,红外光谱,核磁共振及质谱鉴定。其药理实验正在进行中。初步实验表明,5及6对小麦生长有较强的促进作用。 相似文献
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酰氨基硫脲及其相关杂环衍生物的研究II.1-[5-(α-萘)-2H-四唑-2-乙酰[-4-苯基氨基硫脲及其相关环衍生物的合成 总被引:15,自引:0,他引:15
本文合成了1-[5-(α-萘)-2-H-四唑2-乙酰]-4-苯基氨基硫脲5,以及由5衍生的环化产物3-[5-(α-萘)-2H-四唑2-甲撑]-4-苯基-1,2,4-三咪啉-5-硫酮6,2-苯胺基-5-[5-(α-萘)-2H-四唑-2-甲撑]-1,3,4-噻二唑7及2-苯胺基-5-[5-(α-萘)-2H-四唑-2-甲撑]-1,3,4-二唑8.它们的结构均通过元素分析,红外光谱,核磁共振及质谱鉴定.其药理实验正在进行中.初步实验表明,5及6对小麦生长有较强的促进作用. 相似文献
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4-(5-喹啉-3-基-四氮唑-2-基)丁胺的合成 总被引:1,自引:0,他引:1
三苯基膦钯催化3-溴喹啉完成氰化取代制得3-氰喹啉(1);1与叠氮化钠经[2+3]环加成合成了3-(2H-四氮唑-5-基)喹啉(2);2与N-(4-溴丁基)邻苯二甲酰亚胺反应制得2-[4-(5-喹啉-3-基-四氮唑-2-基)丁基]异吲哚-1,3-二酮(3);3经肼解合成了4-(5-喹啉-3-基-四氮唑-2-基)丁胺(4... 相似文献
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l-[2-(N,N-dimethyl-amino)ethyl]-1H-tetrazol-5-thiol is an important intermediate.It is widely used as cephalosporin CS derivative.This paper has developed a new synthetic pathway to give it by six steps.The experimental procedures are shown the following. 相似文献
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Regioselective alkylation of 2-alkyl-5,6,7,8-tetrahydro-3H-cycloheptimidazol-4-one (1) and 2-alkyl-3H-cycloheptimidazol-4-one (2) was investigated. 3-[2'-(1-tert-Butyl-1H-tetrazol-5-yl)biphenyl-4-ylmethyl]-2-propyl-5,6,7,8-tetrahydro-1H-cycloheptimidazol-4-one (6) was preferentially obtained under the conditions by using NaH in DMF or THF. On the other hand, 3-[2'-(1-tert-butyl-1H-tetrazol-5-yl)biphenyl-4-ylmethyl]-2-propyl-5,6,7,8-tetrahydro-3H-cycloheptimidazol-4-one (5), the synthetic intermediate compound of Pratosartan, was obtained selectively in the presence of n-Bu(4)NBr in toluene by using aqueous sodium hydroxide as a base. In this reaction, it was found that the concentration of the alkaline solution influences its regioselectivity. This selectivity was observed even for aldehyde and ester derivatives. 相似文献
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以4-氰基苯酚和2-氯丙酸乙酯(或2-氯乙酸甲酯)为起始原料进行反应,得到2-(4-(1H-四唑-5-基)苯氧基)丙酸/乙酸酯,进而发生Huisgen反应合成了一系列新型1,3,4-噁二唑类标题化合物,其结构经~1H NMR,~(13)C NMR,IR,MS及元素分析或高分辨质谱得到表征和确认.用X射线衍射测定了化合物3q的晶体结构.初步生物活性测试结果表明,含有较小体积取代基的噁二唑化合物3c和3d在200μg/mL测试浓度下对水稻KARI酶分别具有94.5%和83.1%的抑制活性.化合物3p在100μg/mL浓度下对双子叶油菜(Brassica campestris)胚根生长抑制率可达82.4%. 相似文献
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O. A. Shemyakina A. G. Mal’kina A. I. Albanov B. A. Trofimov 《Chemistry of Heterocyclic Compounds》2011,47(4):464-469
Using the example of the reaction of tetrazole with 4-hydroxy-4-methyl-2-pentynonitrile, conditions were found under which
(Z)-4-hydroxy-4-methyl-3-(1H-tetrazol-1-yl)2-pentenonitrile was formed by regio- and stereoselective addition at atom N(1) of
tetrazole (yield 85%, selectivity 95%). 相似文献
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Three novel naphthoquinone-based heterocyclic pigments, 2-methyl-3-[(1-methyl-1H-imidazol-2-yl)thio-1,4-naphthalenedione, (4-methyl-4H-1,2,4-triazol-3-yl)thio-1,4-naphthalenedione, and (1-methyl-1H-tetrazol-5-yl)thio]-1,4-naphthalenedione, are synthesized, and their optical properties in both solution and solid states are investigated. Depending on the heteroarylthio ring in the pigment, variation in optical properties is observed, e.g. characteristic colours for each pigment in the solution and solid states. The achiral pigment containing the 1-methyl-1H-tetrazol-5-yl ring exhibits a chiral space group and a CD signal in the solid state. 相似文献
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Three hydroxylated metabolites of 2-propyl-3-[2'-(1H-tetrazol-5-yl)biphenyl-4-ylmethyl]-5,6,7,8-tetrahydro-3H-cycloheptimidazol-4-one (Pratosartan), which is a selective angiotensin II receptor antagonist, were synthesized in confirmation of their structures and in studies of their pharmacological properties. An MTPA ester of the human main metabolite was identified with the synthesized compound by comparing (1)H-NMR spectra, MS spectra, and HPLC retention time. The structure of the human main metabolite was confirmed to be (S)-(-)-2-(1-hydroxypropyl)-3-[2'-(1H-tetrazol-5-yl)biphenyl-4-ylmethyl]-5,6,7,8-tetrahydro-3H-cycloheptimidazol-4-one ((S)-(-)-1). Also, the rat main metabolites were confirmed to be 8-hydroxylated compound (2) and 5-hydroxylated compound (3). These metabolites showed lower antagonistic activity than that of the parent compound. 相似文献
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《Journal of Saudi Chemical Society》2014,18(5):513-519
One pot synthesis and characterization of new 5-[2′-(1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-4,5,6,7-tetrahydro-thieno[3,2-c]pyridines (3a–k) using amides (2a–k) were reported. The prepared 5-[2′-(1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-4,5,6,7-tetrahydro-thieno[3,2-c]pyridine (3a) is a bioisostere of 4′-(6,7-dihydro-4H-thieno [3,2-c]pyridin-5-ylmethyl)-biphenyl-2-carboxylic acid (1), having good in vivo antithrombotic activity compared with Clopidogrel. The new tetrazole derivatives (3a–k) were screened for their in vitro activity as platelet aggregation inhibitors. 相似文献
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钌配合物[Ru(bpy)2(PNT)]2+的合成、表征及与DNA相互作用研究 总被引:3,自引:1,他引:2
以cis-Ru(bpy)2Cl2·2H2O与PNT为原料合成钌(Ⅱ)多吡啶配合物[Ru(bpy)2(PNT)]2+(bpy=2,2’-联吡啶, PNT=2-[4’-(5-四唑基)苯基]咪唑-[4,5-f][1,10]邻菲咯啉), 通过元素分析、质谱和核磁共振波谱对该化合物进行了结构表征. 利用紫外-可见吸收光谱、荧光光谱、热变性和黏度实验研究了配合物与CT-DNA的相互作用, 实验结果表明, 该配合物以部分插入模式与DNA结合. 相似文献