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1.
利用L-脯氨酸催化的5-氯水杨醛(1)与6-甲基-4-羟基吡喃酮(2)的缩合反应及硫酸铜催化下与1,3-二甲基-5-氨基吡唑(3)的串联反应,合成得到了10-氯-1,3-二甲基-5-(2-氧代丙基)色烯并[4,3-d]吡唑并[3,4-b]吡啶-6(3H)-酮(4)和10-氯-5-二乙氧基甲基-1,3-二甲基色烯并[4,3-d]吡唑并[3,4-b]吡啶-6(3H)-酮(5).化合物5的结构通过单晶X射线衍射法确定:晶体属于三斜晶系,空间群P-1;相对分子质量Mr=803.68;晶胞参数a=1.03160(10)nm,b=1.42900(13)nm,c=1.44268(15)nm;V=1.9448(3)nm~3;Z=2;晶胞密度Dc=1.372g/cm~3;吸收系数μ=0.228mm-1;单胞中电子的数目F(000)=840.晶体结构用直接法解出,经全矩阵最小二乘法对原子参数进行修正,最终的偏离因子为R=0.0681,w R=0.2051.在晶体结构中色烯环与吡啶环及吡唑环近似于共平面. 相似文献
2.
Dejiang Li Deqing Long Heqing Fu 《Phosphorus, sulfur, and silicon and the related elements》2013,188(9):2079-2087
In search of better bioactive compounds, a series of novel 2,6-bis[(3-aryl)-s-triazolo[3,4-b]-[1,3,4]thiadiazole-6-yl]pyridines 2 were synthesized in high yields by the cyclization of 3-aryl-4-amino-5-mercapto-1, 2, 4-triazoles 1 with 2,6-pyridine dicarboxylic acid. 2 exhibited good fungicidal activities against Cerospora beticola sacc. 相似文献
3.
Yuh-Wen Ho 《中国化学会会志》1999,46(6):955-962
Coupling the diazonium salt of 3-amino-2-cyano-4,6-dimethylthieno[2,3-b]pyridine 1 with malononitrile 2 gave 2-cyano-3-(hydrazonomalononitrile)-4,6-dimethylthieno[2,3-b]pyridine 3 which then reacted with hydrazine compounds 4a-4h to yield corresponding 2-cyano-3-(3,5-diamino-1-substituted-pyrazol-4-yl)azo-4,6-dimethylthieno[2,3-b]pyridines 5a-5h. The 2-cyano-3-(2-amino-5,7-disubstituted-pyrazolo-[1,5-a]pyrimidine-3-yl)azo-4,6-dimethylthieno[2,3-b]pyridines 7a-7f were obtained in good yield by the cyclocondensation reaction of 2-cyano-3-(3,5-diamino-pyrazol-4-yl)azo-4,6-dimethylthieno[2,3-b]pyridine 5a with the appropriate 1,3-diketones 6a-6f under acidic condition. 相似文献
4.
ZHANG Zi-Yi ZOU NingNational Laboratory of Applied Organic Chemistry Department of Chemistry Lanzhou University Lanzhou Gansu China 《中国化学》1995,13(5):448-453
In this paper , 10 novel 6-aryl-3-(5'-phenyl-2H-tetrazole-2'-methylene)-S-triazolo[3, 4-b]-1,3,4-thiadiazoles have been synthesized by the condensation of 3-(5'-phenyl-2H-tetrazole-2'-methylene)-4-amino-5-mercapto-1,2,4-triazole with various aromatic carboxylic acids in the presence of phosphorus oxychloride. The structure of these compounds was determined by elemental analysis , UV, IR, 1H NMR and MS. Their spectral properties were also discussed. 相似文献
5.
Dejiang Li Deqing Long Heqing Fu 《Phosphorus, sulfur, and silicon and the related elements》2013,188(3):519-526
1,3-bis[(3-aryl)-s-triazolo[3,4-b]-[1,3,4]thiadiazole-6-yl]benzenes 2 were synthesized in high yields by the reaction of 3-aryl 4-amino-5-mercapto-1,2,4-triazole 1 with m-phthalic acid. 相似文献
6.
A practical approach to polyfunctionally substituted 4,7-dihydropyrazolo[3,4-b]pyridine derivatives from heteroaryl hydrazine, 3-aryl-3-oxopropanenitriles and aldehydes have been described in the report. The present catalyst-free protocol involves the intermediacy of 5-aminopyrazole and α-cyanochalcone, which undergoes in situ Michael addition to afford title compounds in moderate to good yields. All the steps were conducted concomitantly to render the procedure as practical and straightforward as possible. The expeditious synthetic protocol experiment takes less than one hour and shows broad substrate scope. 相似文献
7.
Yuh-Wen Ho 《中国化学会会志》1999,46(1):91-96
The reaction of 3-amino-4,6-dimethyl-2-thieno[2,3-b]pyridine carbohydrazide ( 1 ) with appropriate chalcones 2a-2d in the presence of acid catalyst produced the corresponding 3-amino-2-[(3,5-disubstituted-pyrazolin-1-yl)carbonyl]-4,6-dimethylthieno[2,3-b]pyridines 3a-3d . 3-Amino-2-[(3-substituted-pyrazolin-1-yl)carbonyl]-4,6-dimethylthieno[2,3-b]pyridines 7a, 7b were also obtained by the cyclization reaction of carbohydrazide 1 with Mannich base derivatives 6a, 6b under basic condition. 相似文献
8.
A one-pot,three-component condensation reaction of an aldehyde,benzoyl acetonitrile(3-oxo-3-phenylpropane nitrile) and 6- amino-1,3-dimethylpyrimidine-2,4(1H,3H)-dione or 3-methyl-1-phenyl-1H-pyrazol-5-amine in water to give fused pyrido[2,3- d]pyrimidines and pyrazolo[3,4-b]pyridines in high yields without any catalyst,is described. 相似文献
9.
AbdElAziz A. Nayl Hamada Mohamed Ibrahim Kamal M. Dawood Wael A. A. Arafa Ahmed I. Abd-Elhamid Ismail M. Ahmed Mohamed A. Abdelgawad Hazim M. Ali Ibrahim Hotan Alsohaimi Ashraf A. Aly Stefan Brse Asmaa Kamal Mourad 《Molecules (Basel, Switzerland)》2022,27(19)
An appropriate and efficient Q-tube-assisted ammonium acetate-mediated protocol for the assembly of the hitherto unreported 5-arylazopyrazolo[3,4-b]pyridines was demonstrated. This methodology comprises the cyclocondensation reaction of 5-amino-2-phenyl-4H-pyrazol-3-one with an assortment of arylhydrazonals in an NH4OAc/AcOH buffer solution operating a Q-tube reactor. This versatile protocol exhibited several outstanding merits: easy work-up, mild conditions, scalability, broad substrate scope, safety (the Q-tube kit is simply for pressing and sealing), and a high atom economy. Consequently, performing such reactions under elevated pressures and utilizing the Q-tube reactor seemed preferable for achieving the required products in comparison to the conventional conditions. Diverse spectroscopic methods and X-ray single-crystal techniques were applied to confirm the proposed structure of the targeted compounds. 相似文献
10.
Andrey V. Khramchikhin Mariya A. Skrylnikova Iana L. Esaulkova Ekaterina O. Sinegubova Vladimir V. Zarubaev Maxim A. Gureev Aleksandra M. Puzyk Vladimir A. Ostrovskii 《Molecules (Basel, Switzerland)》2022,27(22)
This study of the interaction system of binucleophilic 3-substituted 4-amino-4H-1,2,4-triazole-5-thiols and 3-phenyl-2-propynal made it possible to develop a new approach to synthesis of such isomeric classes as 7-benzylidene-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazine and 8-phenyl-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazepine. Among the 20 compounds studied in vitro against influenza A/Puerto Rico/8/34 (H1N1) virus, half of them demonstrated selectivity index (SI) of 10 or higher and one of them (4-((3-phenylprop-2-yn-1-yl)amino)-4H-1,2,4-triazole-3-thiol) possessed the highest (SI > 300). Docking results and values showed that the preferred interactant for our ligands was M2 proton channel of the influenza A virus. Protein-ligand interactions modeling showed that the aliphatic moiety of ligands could negatively regulate target activity level. 相似文献
11.
3—吡唑基—6—取代均三唑并[3,4—6]—1,3,4—噻二唑的合成及生物活性 总被引:3,自引:2,他引:3
以1-甲基-3-乙基(4-氯)-5-哟唑甲作原料,经两步得到4-氨基-3-(1-甲基-3-乙基(4-氯)-5-吡唑基)-1,2,4-三唑-5-硫酮(3),3再与取代酸反应,得到一系列3(1-甲基-3-,乙基(-4-氯)-5-吡唑基)-6-取代均三并「3,4-b」-1,3,4-噻二唑(4,5,6),元素分析、HNMR、IR和MS确定了它们的结构,初步生侧结果表明,3具有植物生长调节活性,4b、4d、 相似文献
12.
13.
Fifteen novel pyrazolo[3,4-b]-pyrido[4,3-d]-pyrimidine-4-ones (7a–o) were designed and have been successfully synthesized via tandem aza-Wittig and annulation reactions of the corresponding iminophosphorances 5, phenylisocyanate, and substituted phenols in 60–77% isolated yields. Their structures were clearly verified by infrared (IR), 1H NMR, electron impact–mass spectrometry (EI-MS), and elemental analysis. The results of a preliminary bioassay indicated that some compounds possess inhibition activities against the root of Brassica napus (rape) and Echinochloa crusgalli (barnyard grass) at a dosage of 100 mg/L and 10 mg/L. 相似文献
14.
The rearrangement reaction of 2-benzothiazolylthioacetyl hydrazide 1 with potassium hydroxide and carbon disulfide in ethanol to produce s-triazolo [3,4-b] benzothiazole-3-thiol 3 was described. 3 also can be obtained from 2-benzothiazolylhydazine 2 and the two methods for getting 3 were compared. Mannich reaction of compounds 3 was reported too. 相似文献
15.
由化合物3-(4'-吡啶基)/苯基4氨基-5-巯基-1,2,4-三唑与芳香酸在三氯氧磷作用下脱水、闭环得到3-(4'-吡啶基)/苯基-6-芳基-1,2,4-三唑并[3,4-b]-1,3,4-噻二唑类新型化合物,产率为42%~72%。该化合物具有较大的共轭平面,其结构经红外光谱、核磁共振氢谱、元素分析测试技术确证。电化学测试的工作窗口为-1.4~1.0V.负向扫描,循环伏安图中显示标题化合物均有还原峰,还原起始电位为-0.35~-0.95V.借鉴有机材料能带表征的方法,结合其紫外-可见光谱计算出了被测化合物的电子亲和势、电离势、带隙等电化学参数。结果表明,与常用的有机电子传输材料PBD相比,标舾化合物具有较高的电子亲和势(3.79~4.39ev)和电离势(6.95~7.84eV),较高的电子亲和势有利于电子的传输。 相似文献
16.
将5-取代吡唑-3-甲酸乙酯1位甲基化,经水解反应得到3种中间体1-甲基-5-取代1H-吡唑-3-甲酸(2a~2c);以不同取代的羧酸为原料经一系列反应合成6种中间体3-取代4-氨基-5-巯基-1,2,4-均三唑(3a~3f);将中间体(2a~2c)和(3a~3f)在三氯氧磷条件下反应,合成出18种1,2,4-三唑并[3,4-b]-1,3,4-噻二唑类化合物(4a~4r),均未见文献报道。 通过IR、1H NMR、13C NMR和元素分析表征了化合物结构。 初步的生物活性测试结果显示,所合成的化合物均表现出不同程度的生长素活性和抑菌活性。 并选取抑菌活性较好的两个化合物进行抗菌药物最低抑菌浓度(MIC)的测定。 相似文献
17.
E. A. Kaigorodova A. A. Osipova L. D. Konyushkin G. D. Krapivin 《Russian Chemical Bulletin》2004,53(4):853-859
Reactions of 2,5-dimethoxytetrahydrofuran with 3-aminothieno[2,3-b]pyridines afford a number of substituted 3-(1H-pyrrol-1-yl)thieno[2,3-b]pyridines. The possibility of the reaction and the yield of the product are determined by the character of a substituent in position 2 of thieno[2,3-b]pyridine. The Curtius rearrangement of 2-acylazido-3(1H-pyrrol-1-yl)thieno[2,3-b]pyridines yields 4,5-dihydropyrido[3",2":4,5]thieno[2,3-e]pyrrolo[1,2-a]pyrazin-4-ones. The molecular and crystal structures of ethyl 4-methoxymethyl-6-methyl-3-(1H-pyrrol-1-yl)thieno[2,3-b]pyridine-2-carboxylate were determined by X-ray diffraction analysis. 相似文献
18.
A multicomponent, catalyst-free reaction for the synthesis of fused 6-amino-3-methyl-4-aryl-1H-pyrazolo [3,4-b] pyridine-5-carbonitrile from 3-amino-5-methylpyrazole, malononitrile, and substituted aldehydes under ultrasound irradiation in short reaction times (8–10 min) with good yields (85–98%) is reported.
19.
合成了18个含有1H-1,2,4-三唑的咪唑[2,1-b]-1,3,4-噻二唑以及S-三唑[3,4-b]-1,3,4-噻二唑的稠杂环衍生物,经元素分析及谱学表征,探讨2,5,6-三取代咪唑[2,1-b]-1,3,4-噻二唑的可能生成机制.对大肠杆菌、绿脓杆菌、枯草杆菌等初步抑菌试验证明,多数化合物表现了较好的抑菌活性. 相似文献
20.
取代苯甲醛与4-氨基-5-(3,4,5-三甲氧基苯基)-1,2,4-三唑-3-硫酮(2)缩合生成5-(3,4,5-三甲氧基苯基)-4-取代苯基亚胺基-1,2,4-三唑-3-硫酮(3),再烷基加成化为新型5,6-2H-1,2,4-三唑[3,4-b][1,3,4]噻二嗪衍生物4.化合物结构经1HNMR 13C NMR,IR以及元素分析确认.采用噻唑兰(MTT)比色法进行化合物抑制人体前列腺癌细胞(PC3)体外活性测试,结果表明所合成的化合物具有不同程度的抑制PC3活性,其中化合物4a在10μmol·L-1浓度下对PC3的抑制率为75.9%. 相似文献