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为寻找高效低毒的含三氟甲基取代的喹唑啉类新型抗肿瘤活性化合物,以2-硝基-5-氯苯甲酸为原料,通过水解、还原、偶联、环合、三氟甲基加成消除等反应,合成了14个2-芳基-4-三氟甲基喹唑啉衍生物,并通过1H NMR、13C NMR、19F NMR等进行了结构确证。采用MTT法评价了目标化合物对PC3(前列腺癌细胞)、LNCaP(前列腺癌细胞)、K562(人慢性髓系白血病细胞)、HeLa(宫颈癌细胞)和A549(人肺癌细胞)等肿瘤细胞株的生长抑制活性。结果显示,在5μmol/L浓度下,部分目标化合物对上述5种肿瘤细胞均具有较好的生长抑制活性,其中,化合物8c、13e对LNCaP细胞的IC50(半数抑制浓度)分别为2.9和1.9μmol/L,值得进一步深入研究。 相似文献
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N. V. Kovganko Zh. N. Kashkan Yu. G. Chernov S. K. Ananich S. N. Sokolov V. L. Survilo 《Chemistry of Natural Compounds》2003,39(5):411-437
Literature data published in 1998-2002 on the chemical synthesis of ecdysteroids and their structural analogs were reviewed. 相似文献
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《Journal of heterocyclic chemistry》2017,54(2):1572-1577
The synthesis of new derivatives of 6,7‐dibromoquinoline‐5,8‐dione and 6,7‐dichloroquinoline‐5,8‐dione via palladium/Sphos‐mediated Suzuki–Miyaura cross‐coupling reaction is reported. The 6,7‐dibromoquinoline‐5,8‐dione and 6,7‐dichloroquinoline‐5,8‐dione intermediates were prepared in a three‐step reaction from 8‐hydroxyquinoline. The palladium‐catalyzed reactions of 6,7‐dibromoquinoline‐5,8‐dione and 6,7‐dichloroquinoline‐5,8‐dione with a variety of aryl boronic acids provide coupled compounds in high yields. The arylation of 6,7‐dibromoquinoline‐5,8‐dione and 6,7‐dichloroquinoline‐5,8‐dione with 4‐bromophenyl boronic acid supplied 6,6′‐(1,4‐phenylene)bis(7‐bromoquinoline‐5,8‐dione) and (4‐(6‐(4‐(6‐chloro‐5,8‐dihydroquinolin‐7‐yl)phenyl)‐5,8‐dihydroquinolin‐7‐yl)phenyl)boronic acid respectively, in addition to the expected coupled compounds in moderate yields. Also, Pd(0)/PPh3 allowed the 7‐chloro‐6‐(4‐nitrophenyl)quinoline‐5,8‐dione and 7‐chloro‐6‐phenylquinoline‐5,8‐dione to be synthesized via Heck reaction. The yields of the synthesized target molecules depend largely on the reaction conditions and the type of ligands employed. Structural assignments of the synthesized compounds were established by spectra and analytical data. 相似文献
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1-芳酰基-4-取代吡唑甲酰基氨基硫脲和环化产物的合成及生物活性 总被引:28,自引:0,他引:28
利用1-苯基-3-甲基-5-氯-4-吡唑甲酰基异硫氰酸酯(Ⅰ)与芳酰肼(Ⅱ)的加成反应合成了系列新的酰胺基硫脲衍生物(Ⅲ),并将Ⅲ在酸性条件下进行环化反应得到2-取代吡唑甲酰基氨基-5-芳基-1,3,4-噻二唑(Ⅳ).生物活性测定结果表明部分化合物Ⅲ和Ⅳ具有较好的除草活性. 相似文献
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Four-component, one-pot condensation of dimedon, thiophene-2-carbaldehyde, ammonium acetate, and numerous acetophenones yielded novel 2-aryl-4-thionylquinoline derivatives. The structures were characterized by 1H NMR, 13C NMR, IR, and elemental analysis. 相似文献
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以喹啉(1)和取代苯肼(2a~2d)为原料,K2S2O8为引发剂,TBAB为相转移催化剂,乙腈为溶剂,经自由基反应合成了4个2-苯基喹啉化合物(3a~3d, 3d为新化合物),其结构经1H NMR, 13C NMR和HR-ESI-MS表征。以3a的合成为模板反应,研究了引发剂,溶剂和反应温度对3收率的影响。结果表明:在最佳反应条件(1 1.0 mmol, 2 1.2 eq., K2S2O8 2.0 eq., TBAB 0.2 eq.,于室温反应4 h)下,3a~3d收率54%~72%。 相似文献
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1-苯氧基乙酰基-4-(邻硝基苯甲酰基)氨基硫脲及其相关杂环化合物的合成研究 总被引:7,自引:0,他引:7
芳氧基乙酸及其衍生物对植物有很强的生理活性,广泛用作除莠剂和植物生长调节剂[1,2].1,4-二酰基取代的氨基硫脲及其杂环衍生物亦有多种生物活性[3].若将上述两类具有生物活性的基团聚集于同一分子中,实现其活性叠加,同时改变取代基,有望获得具有更高生物活性的物质.基于此,我们在以前工作[4]的基础上,以PEG-400为催化剂,在固-液相转移条件下,用邻硝基苯甲酰氯与硫氰酸铵反应,首先制得邻硝基苯甲酰基异硫氰酸酯(Ⅰ),不经分离,Ⅰ直接与芳氧基乙酰肼加成得到了1-芳氧基乙酰基-4-(邻硝基苯甲酰基… 相似文献
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LI Yu-Linga b WANG Xiang-Shan a b ZENG Zhao-Sena LOU Xiu-Liana SHI Da-Qinga b TU Shu-Jianga b 《有机化学》2005,(11)
在KF/Al2O3催化下,α,β-不饱和腈或α,β-不饱和羧酸酯和7-甲氧基-1,2,3,4-四氢-2-萘酮反应,生成了一系列4-芳基-9,10-二氢萘并[2,1-b]-4H-吡喃衍生物.产物的结构通过红外光谱和核磁共振氢谱进行表征,并通过X单晶衍射分析进一步证实产物的结构. 相似文献
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Anne Brennführer Helfried Neumann Dr. Matthias Beller Prof. Dr. 《Angewandte Chemie (International ed. in English)》2009,48(23):4114-4133
A CO group richer : (Hetero)arenes are vital intermediates in the manufacture of agrochemicals, dyes, pharmaceuticals, and other industrial products. In the past decades transition‐metal‐catalyzed coupling reactions of aryl halides with all types of nucleophiles have been developed. This Review summarizes recent work in the area of palladium‐catalyzed carbonylation reactions of aryl halides and related compounds (see scheme).
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A series of novel 3-cyano- and related 3-substituted phthalmidines have been synthesized from acyclic precursors, some of which were isolated. 相似文献
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钯络合物能催化许多反应,在有机合成中有着广泛的应用。钯催化下的反应,产率高,选择性好,反应条件温和。本文介绍了近年来该类反应在有机合成中的一些应用。 相似文献