共查询到19条相似文献,搜索用时 125 毫秒
1.
贫电子环丙烷衍生物1以精制四氢呋喃为溶剂, 与2-巯基苯骈噻唑(2)封管加热反应, 得到产物3和4. 产物3经IR, MS, 1H NMR, 13C NMR和元素分析等数据确定其结构为: (R)-β-取代-(R)-γ-(2-巯基)苯骈噻唑基-γ-对位取代苯基丁酸或(S)-β-取代-(S)-γ-(2-巯基)苯骈噻唑基-γ-对位取代苯基丁酸(3); 产物4通过IR, MS, 1H NMR, 13C NMR, 2D-NOESY谱和元素分析等数据确定其结构为: 反式-β-取代-γ-对位取代苯基-3-丁烯酸(4). 对生成产物的机理也进行了推测. 相似文献
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为了寻找高效低毒的非甾体抗炎药物, 将5-氯-2-吲哚酮与氯甲酸苯酯经酯化及水解制得1-苯氧羰基-5-氯-2-吲哚酮, 在4-N,N-二甲氨基吡啶作用下与对甲磺酰基苯甲酰氯反应, 经酸化得1-苯氧羰基-3-[羟基-(p-甲磺酰基)苯甲撑基]-5-氯-2-吲哚酮(II1), 最后与相应的胺(氨)反应, 经盐酸中和制得未见文献报道的目标化合物II2~II15, 其结构经IR, 1H NMR, MS和元素分析确证. 二甲苯致小鼠耳肿胀模型测试显示II10, II11, II15具有明显的抗炎活性; 角叉菜胶致大鼠足跖肿胀模型试验结果表明, II10, II11抗炎活性与双氯芬酸钠和替尼达普钠相当(P>0.05); 其中II11的胃肠道副作用显著小于双氯芬酸钠(P<0.05)和替尼达普钠(P<0.01). 相似文献
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分别由2-[(2Z)-3-羧基-1-氧代-2-丙烯基]氨基-2-脱氧-1,3,4,6-四-O-乙酰基-β-D-吡喃葡萄糖(1a), 2-[(2-羧基苯甲酰基)氨基]-2-脱氧-1,3,4,6-四-O-乙酰基-β-D-吡喃葡萄糖(2a)和氧化二正丁基锡反应合成了两个新化合物双-{2-[(2Z)-3-羧基-1-氧代-2-丙烯基]氨基-2-脱氧-1,3,4,6-四-O-乙酰基-β-D-吡喃葡萄糖}-二正丁基锡酯(1)和双-{2-[(2-羧基苯甲酰基)氨基]-2-脱氧-1,3,4,6-四-O-乙酰基-β-D-吡喃葡萄糖}-二正丁基锡酯(2), 并经红外光谱、核磁共振(1H, 13C NMR)、质谱初步确定了其结构. 体外抗肿瘤活性结果表明, 化合物1对人肺癌细胞株A-549和人肝癌细胞株BEL-7402的细胞毒活性显示为强效; 而对小鼠白血病细胞株P388和人白血病细胞株HL-60的细胞毒活性为弱效. 化合物2对肿瘤细胞株HL-60, A-549和BEL-7402具有强效的细胞毒活性; 而对肿瘤细胞株P388的作用则为弱效. 克隆基因分析表明化合物1和2在3.82×10-6 和 3.02×10-6 mol/L均具有造血细胞毒性. 相似文献
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N′-(取代嘧啶-2-基)-N-菊酰硫脲的合成与生物活性研究 总被引:7,自引:0,他引:7
采用活性基团拼接法, 将第一菊酸构型中的最高活性组分(+)-反式菊酸以及二氯菊酸引入到含取代嘧啶环的酰基硫脲结构中, 合成了5个未见文献报道的N′-(取代嘧啶-2-基)-N-(+)-反式菊酰硫脲衍生物(3a~3e)和3个均未见文献报道的N′-(取代嘧啶-2-基)-N-二氯菊酰硫脲(3f~3h), 结构经元素分析、IR和1H NMR得到确证. 初步的生物活性测试结果表明: 大部分化合物具有较好的杀菌活性, 有的化合物兼具除草和杀菌活性, 有的化合物兼具杀虫和杀菌活性. 相似文献
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以豆腐果苷为原料, 与盐酸羟胺缩合反应生成4-β-D-吡喃阿洛糖苷-苯甲醛肟(2), 2与次氯酸叔丁酯发生取代反应生成4-β-D-吡喃阿洛糖苷-α-氯苯甲醛肟(3); 再将3与Schiff碱通过1,3-偶极环加成生成一系列3-(4-β-D-吡喃阿洛糖苷-苯基)-4-芳基-5-芳基-1,2,4-噁二唑啉(5a~5h). 3和 5a~5h共9个化合物均未见文献报道, 其结构经1H NMR, IR和MS (HRMS)加以确认, 并对5a~5h进行了药理活性筛选. 结果表明, 部分化合物具有良好的镇静活性. 其中, 化合物5g (200, 100 mg•kg-1)和5h (200, 100 mg•kg-1)与豆腐果苷相比较具有更强的活性. 相似文献
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以(S)-2-氨基丙醇为手性源与α-溴-3-氯苯丙酮反应, (R)-2-氨基丙醇为手性源与6-甲氧基-2-(2-溴丙酰基)萘反应, 分别合成了手性纯化合物(2R,3R,5S)-3,5-二甲基-2-(3-氯苯基)-2-吗啉醇盐酸盐(4a)和(2S,3S,5R)-3,5-二甲基-2-(6-甲氧基-2-萘基)-2-吗啉醇盐酸盐(4b), 利用X射线单晶衍射仪测定了两化合物的晶体结构和两化合物的空间结构, 并初步分析两化合物空间结构, 化合物4a晶体属正交晶系, 空间群为P21212, 晶胞参数为: a=0.8718(2) nm, b=0.7883(2) nm, c=2.0247(6) nm, Z=4, V=1.3915(7) nm3, Dc=1.328 g/cm3, F(000)=584, R1=0.0399, wR2=0.0797, S=1.042. 化合物4b晶体属正交晶系, 空间群为P212121, 晶胞参数为: a=0.71035 (9) nm, b=0.77703(10) nm, c=2.9820(4) nm, Z=4, V=1.6318(4) nm3, Dc=1.318 g/cm3, F(000)=688, R1=0.0520, wR2=0.1108, S=0.994. 相似文献
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N-烷基/芳基-N'-(4-芳基噻唑-2-基)-N"-糖基胍的合成及生物活性研究 总被引:4,自引:1,他引:3
2,3,4,6-四-O-乙酰基-β-D-吡喃葡萄糖基异硫氰酸酯(1)与2-氨基-4-取代苯基噻唑(2a~2b)反应, 生成糖基硫脲衍生物3a~3b, 再在伯胺存在下经氯化汞脱硫, 得到一系列新的N-烷基/芳基-N'-(4-芳基噻唑-2-基)-N"-糖基胍类化合物(4a~4e, 5a~5e). 所有新化合物的结构均经IR, 1H NMR, MS谱和元素分析证实, 所得产物均为β-构型. 生物活性测试结果表明, 化合物4b和5d对HIV-1 PR表现出了较高的抑制活性. 相似文献
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Navabeh Nami Masoumeh Hosseinzadeh Ehteram Rahimi 《Phosphorus, sulfur, and silicon and the related elements》2013,188(10):2438-2442
The reaction of 4-oxo-2-(2-oxo-1,2-dihydroindol-3-ylidene)hydrazone-1,3-thiazin-6-methyl carboxylate 2 with hydrazine hydrate in methanol gave 4-oxo-2-(2-oxo-1,2-dihydroindol-3-ylidene)hydrazone-1,3-thiazin-6-carbonylhydrazine 3. Furthermore, the reaction of 3 with carbon disulfide and then hydrazine hydrate afforded 3-[6-(4-amino-5-thioxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)-4-oxo-1,3-thiazin-2-yl] hydrazone-1,3-dihydroindol-2-one 5. the latest reacted with DMAD to give {6-hydroxy-3-[4-oxo-2-(2-oxo-1,2-dihydroindol-3-ylidene)hydrazone-1,3-thiazin-6yl]-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazin-7-ylidene}methoxycarbonylmethylene 6. 相似文献
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Adri van den Hoogenband Jack A.J. den Hartog Jos H.M. Lange Jan Willem Terpstra 《Tetrahedron letters》2004,45(46):8535-8537
A novel efficient synthetic route to the pharmaceutical key intermediate N-(piperidin-4-yl)-1,3-dihydroindol-2-one is described. The key step involves a high-yielding intramolecular palladium-catalyzed amination reaction using Buchwald’s X-Phos ligand under mild reaction conditions. 相似文献
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Fatma A. El-Samahy Nabila M. Ibrahim 《Phosphorus, sulfur, and silicon and the related elements》2016,191(1):59-64
In this study use was made of the Wittig carbonyl olefination reaction and stereo-identification of the resulting alkenes. Condensation of 2-chloroquinoline-3-carbaldehyde with some selected stabilized phosphonium ylides yielded a mixture of the corresponding E and Z olefins in each case. On the other hand reaction of 2-oxoquinoline-3-carbaldehyde with the selected ylides afforded the respective olefins only in one of the possible stereoisomers. The reaction of 2-chloroquinoline-3-carbaldehyde with acetylmethylenetriphenylphosphorane produced the respective olefine together with acridin-3-ol. Heating of (E) and/or (Z)-methyl 3-(2-chloroquinolin-3-yl)acrylate with hydrazine hydrate yielded the corresponding propan-1-ol derivative. Dechlorination of (E)-ethyl 3-(2-chloroquinolin-3-yl)acrylate and/or (E)-4-(2-chloroquinolin-3-yl)but-3-en-2-one was effected upon treatment with morpholine or piperidine in absolute ethanol to give the respective enone derivatives. 相似文献
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The quasi-antiaromatic 2H-indol-2-one ring system is readily generated by treating a 3-hydroxy-substituted 1,3-dihydroindol-2-one with a Lewis acid. Stepwise addition of various pi-nucleophiles to the highly reactive 2H-indol-2-one system occurs smoothly to afford substituted oxindoles. The cyclization was also carried out in an intramolecular fashion to give spiro-substituted oxindoles in good yield. 相似文献
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A. B. Dobrynin P. I. Gryaznov O. E. Naumova I. A. Litvinov V. A. Alfonsov 《Journal of Structural Chemistry》2008,49(5):917-921
An X-ray study of (3Z)-(±)-4-(2′-hydroxypropyl)amino-and (3Z)-4-(2′-hydroxyethyl)amino-pent-3-en-2-ones is reported. The bond lengths inside the H ring are equalized due to the classical N-H...O hydrogen bond between the carbonyl oxygen and the amino group. In the 4-(2′-hydroxyethyl)amino-pent-3-en-2-one crystal, due to the classical N-H...O bonds, infinite zigzag chains are formed along the 0b axis and arranged into a layered structure due to the weak C-H...O interactions. In (±)-4-(2′-hydroxypropyl)aminopent-3-en-2-one crystal, however, centrosymmetric dimers are formed, which are then linked by weak C-H...O intermolecular interactions to form a layered structure along the a0b plane. 相似文献
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Victor I. Dyachenko Aleksandr S. Peregudov Nikolai D. Chkanikov 《Journal of fluorine chemistry》2007,128(7):868-878
The strategy of searching for highly electrophilic agents in a class of chemically inert compounds - methylenequinone imines - was developed and successfully performed. The first representative of such electrophiles - N-acyl-α-methoxycarbonyl-α-trifluoromethyl-p-methylenequinone imine 6 - was synthesized. Its reactions with N-, O- and C-nucleophiles were investigated that gave various derivatives of α-trifluoromethyl-α-amino(oxy) acids as well as ß,ß,ß-trifluoropropionic acids. 3-Chloro-3-trifluoro-1,3-dihydroindol-2-ones were first obtained and their reactions with nucleophiles were studied with 1-aza-3-trifluoroindene-2-ones being formed as intermediates. 相似文献
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以3,3-二甲基-1-(1H-1,2,4-三唑基)-2-丁酮肟为原料,经醚化、肼解及腙化3步反应得到(E)-N'-(取代苯亚甲基)-2-[(Z)-3,3-二甲基-1-(1H-1,2,4-三唑-1-基)丁基-2-亚甲氨氧基]乙酰肼(3a~3u),化合物3与二乙酸碘苯(IBD)反应,合成了21个(Z)-3,3-二甲基-1-(1H-1,2,4-三唑-1-基)-2-丁酮肟-(5-芳基-1,3,4-噁二唑-2-基)甲基醚(4a~4u),化合物4的化学结构经核磁共振谱、高分辨质谱和元素分析确证.采用单晶X射线衍射仪测定了化合物4c的晶体结构.抑菌活性测试结果表明,在500 mg/L浓度下,化合物4k,4f,4j和4n对纹枯病菌的防效率分别为70.9%,60.2%,60.0%和60.6%;在25 mg/L浓度下,化合物4b,4c,4d和4e对菌核病菌的抑制率为71.8%~76.9%. 相似文献
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Alexander Y. Simonov Evgeny E. BykovSergey A. Lakatosh Yury N. LuzikovAlexander M. Korolev Marina I. ReznikovaMaria N. Preobrazhenskaya 《Tetrahedron》2014
15, 16, and 17-Membered lactones based on the bis-3,4(indol-1-yl)maleimide framework were obtained using intramolecular esterification reaction starting from 3-(1-ω-carboxyalkyl-2,3-dihydroindol-1-yl)-4-(1-ω-hydroxyalkyl-2,3-dihydroindol-1-yl)-maleimides. 3,4-Dibromo-maleimide, ω-(2,3-dihydroindol-3-yl)alkanoic acids, and ω-(2,3-dihydroindol-3-yl)alkanoles were used as starting compounds. Substitution of Br for the substituted indolines followed by the intramolecular cyclization of O-silylated hydroxyl acids derivatives led to macrolactones that incorporated 4-(dihydroindol-1-yl)-3-(indol-1-yl)maleimide moieties. Indoline nuclei in these compounds were dehydrogenated by DDQ in refluxing toluene to give 15, 16 or 17-membered lactones 3-[(ω-3-carboxyalkylindol-1-yl)-4-(ω-hydroxyalkylindol-1-yl)maleimides. Quantum chemical calculations showed that the formation of macrolactones of smaller size (13-membered) corresponds to the higher Gibbs energy ΔG# and correlates with the absence of the target reaction product. 相似文献
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Ali Ramazani Bagher Mohammadi Nader Noshiranzadeh Abbas Azizian 《Phosphorus, sulfur, and silicon and the related elements》2013,188(8):1717-1719
Protonation of the highly reactive 1:1 intermediates produced in the reaction between tributylphosphine and dimethyl acetylenedicarboxylate by 3-hydroxy-2-methyl-4 H -pyran-4-one leads to vinyltributylphosphonium salts, which undergo an addition-elimination reaction in CH 2 Cl 2 at room temperature to produce dimethyl 2-[(2-methyl-4-oxo-4 H -pyran-3-yl)oxy]-2-butenedioate (1:1 mixtures of E and Z isomers) in fairly good yields. 相似文献