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新型手性咪唑鎓环番的合成及对氨基酸的对映选择性识别 总被引:2,自引:0,他引:2
以L-氨基酸为手性源, 合成了一系列新型手性咪唑鎓环番, 并进行了结构表征. 在碱性条件下, L氨基酸和乙二醛、甲醛缩合生成了(S)-2-(1-咪唑)羧酸钠, 转化为甲酯后与乙二胺进行胺解反应制得开链手性咪唑二酰胺, 然后与二溴化合物在高稀淡技术和无水条件下进行季铵化关环反应, 再进行阴离子交换制得目标分子(4~6). 以手性咪唑鎓环番为主体分子, 研究了对氨基酸及其衍生物的对映选择性识别作用. 相似文献
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本文选用南开牌D61、D72离子交换树脂催化多元醇和单羧酸的酯化反应,成功地合成了12种多元醇的单羧酸酯。在不同的反应条件下,酯的产率均超过90%。 相似文献
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The Claisen-Schmidt condensation of 1-(triphenylmethyl)-2-imidazolecarboxaldehyde with acetophenones yielded 1-aryl-3-[1-(triphenylmethyl)-2-imidazolyl]propen-1-ones 7 . Selective catalytic hydrogenation over platinum of 7 furnished 1-aryl-3-(2-imidazolyl)-1-propanones 8 . An alternate synthesis of 8 started with sodium borohydride reduction of 7 to give allylic alcohols, 1-aryl-3-[1-(triphenylmethyl)-2-imidazolyl]-2-propen-1-ols 10 , which were rearranged by hot aqueous sodium to 8 . Acid hydrolysis of 8 provided the title compounds and triphenylmethanol. 相似文献
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Richard Tomko C. G. Overberger 《Journal of polymer science. Part A, Polymer chemistry》1985,23(2):265-277
Some ω-(1-imidazolyl) and ω-[4(5)-imidazolyl]alkanoic acids were synthesized and grafted onto poly(vinylamine) with an amide bond. These water-soluble grafts were used to study the kinetics of the esterolysis of activated phenyl esters. The 1-substituted imidazoles were prepared by the reaction of the sodium salt of imidazole with the ethyl ω-bromoalkanoates. The 4(5)-substituted imidazoles were prepared from urocanic acid or 4(5)-hydroxymethylimidazole. The ω-(1-imidazolyl)alkanoic acids were grafted onto poly(vinylamine) via their acyl–guanidine derivatives; the 3-[4(5)-imidazolyl]propanoic acid was grafted with a water-soluble carbodiimide. 相似文献
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以(2R)-3-[(3S,4R)-1-(叔丁基二甲基硅氧基)乙基]-4-乙酰氧基氮杂环丁-2-酮为母体,2-溴乙(丙)酸酯或2-溴丙酰胺为亲核试剂,通过Reformatsky反应合成了一系列新型的1-β-碳氢霉烯类抗生素中间体——3-{(2R)-2-[(3S,4R)-1-(叔丁基二甲基硅氧基)乙基]氮杂环丁-2-酮-4-基}乙(丙)酸酯(3a~3d)和3-{(2R)-2-[(3S,4R)-1-(叔丁基二甲基硅氧基)乙基]氮杂环丁-2-酮-4-基}-N,N-二取代丙酰胺(3e,3i和3k),其结构经1H NMR和13C NMR表征,其中3a~3e和3i未见文献报道。 相似文献
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利用Kröhnke方法,以芳基乙酮为原料一锅法简洁地合成了6-芳基-6'-溴-2,2'-联吡啶2b~2d。 通过(R)-3-(4,4,5,5-四甲基-1,3,2-二噁唑硼烷基)-2,2'-乙氧基-1,1'-联萘((R)-1)与6-溴-2,2'-联吡啶及其衍生物2a~2d的Suzuki偶联, 合成了4种手性6-[3-((R)-2,2'-二乙氧基-1,1'-联萘)基]-2,2'-联吡啶(R)-3a~3d。 将配体(R)-3a~3d应用于苯乙酮的不对称氢转移反应中,配体(R)-3a给出92%的转化率和4%的对映体过量(ee)值。 相似文献
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基于抗菌氟喹诺酮的作用靶拓扑异构酶与哺乳动物的相似性,为寻找由抗菌活性到抗肿瘤活性转化的有效修饰方法,用噁二唑杂环作为诺氟沙星(1)的羧基电子等排体得中间体,1-乙基-6-氟-7-(哌嗪-1-基)-3-(5-巯基-1,3,4-噁二唑-2-基)-喹啉-4(1H)-酮(3),化合物3与氯甲基噁二唑(4a~4e)进行S-醚化得双噁二唑甲硫醚(5a~5e),再进一步甲基化和季铵化得相应的N-甲基双噁二唑甲硫醚(6a~6e)和N,N-二甲基双噁二唑甲硫醚碘化物(7a~7e)。 双噁二唑甲硫醚目标物的结构经元素分析、1H NMR、MS技术确证。 采用MTT法评价了目标化合物对体外培养人肝癌细胞株Hep-3B生长的抑制活性。 结果表明,15个目标化合物的抑制活性均显著高于对照化合物1的抑制活性,其季铵盐的IC50值低于25.0 μmol/L,显示出潜在的抗癌活性。 相似文献
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M. Q. Zhang A. Haemers D. Vanden Berghe S. R. Pattyn W. Bollaert I. Levshin 《Journal of heterocyclic chemistry》1991,28(3):673-683
A series of 7-(2-substituted-4-thiazolyl and thiazolidinyl)-1-ethyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acids and their 6-fluoro analogues were synthesized. The Hantzsch method was used for the preparation of the thiazolylquinolones. The thiazolidinylquinolones were synthesized by quaternization of the corresponding thiazolyl analogues, followed by reduction of the obtained thiazolium salts with sodium borohydride in aqueous solution. Antibacterial activity was tested in vitro. Most of the compounds were inactive against Gram-negative bacteria but some of them showed however good activity against Gram-positive bacteria and mycobacteria. This activity pattern is rarely found among the quinolone antibacterials. 相似文献
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以糠醛为原料,经氧化、醚化和重结晶制得5-甲氧基-3,4-二溴-2(5H)-呋喃酮(4); 4与哌嗪经Michael加成消除反应制得5-甲氧基-4-哌嗪基-3-溴-2(5H)-呋喃酮(5); 5与取代磺酰氯经磺酰化反应合成了7 个新型的含哌嗪-磺酰胺的2(5H)-呋喃酮类化合物(7a~7g),其结构经1H NMR, 13C NMR, IR和HR-MS表征。初步的生物活性研究(MTT法)表明,7a~7g均能显著抑制人宫颈癌Hela细胞的增殖,其中5-甲氧基-4-(对乙酰氨基苯磺酰基-哌嗪基)-3-溴-2(5H)-呋喃酮(7f)的抑制活性最佳,其IC50为0.03 μM(24 h)。 相似文献