共查询到19条相似文献,搜索用时 50 毫秒
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为了寻找高效低毒的抗肿瘤候选化合物, 以去氢骆驼蓬碱为原料, 对β-咔啉环的2-,7-和9-位3个结构位点进行了结构改造, 合成了11个去氢骆驼蓬碱衍生物, 化合物的结构经核磁共振、 红外光谱、 质谱及元素分析确证. 采用四甲基偶氮唑盐(MTT)法初步测试了目标化合物体外抗肿瘤(Bel-7402, 786-0, BGC-823, A375, 769-P和MCF7)活性, 结果表明化合物4a, 4b, 8a和8b具有显著的体外抗肿瘤活性. 相似文献
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以柚皮苷为原料,经酸催化水解、O-甲基化或O-异戊烯基化反应、碱催化的开环反应合成了天然查尔酮卡瓦胡椒素A(1)和查尔酮异戊烯基醚衍生物2;然后以查尔酮1和2为底物,分别通过Mannich反应对其3'位进行了胺甲基化修饰,合成了14个未见文献报道的新型查尔酮Mannich碱衍生物3~16.所合成化合物的结构已由核磁共振谱、红外光谱和质谱所证实,并对所合成的查尔酮及其Mannich碱衍生物进行了乙酰胆碱酯酶(AChE)抑制活性测试,结果发现查尔酮Mannich碱衍生物3~5,9具有良好的AChE抑制活性. 相似文献
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以丹皮酚和对氯苯甲醛为起始原料,通过Claisen-Schmidt反应得到2-羟基-4-甲氧基-4′-氯查尔酮(3),再经过Mannich反应得到10个查尔酮曼尼希碱衍生物(4a~4e, 5a~5e)。目标化合物结构均经高分辨质谱、核磁共振氢谱、碳谱进行确证。采用MTT法测试了所合成化合物对人肺癌细胞A549、人肝癌细胞HepG2的体外抗增殖活性。结果表明,目标化合物对肿瘤细胞A549、HepG2均具有较强的细胞增值抑制作用,且明显优于阳性对照药5-氟尿嘧啶。 相似文献
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对羟基桂皮酸甲酯和阿魏酸甲酯分别在氧化银催化下发生自由基仿生氧化偶联反应,合成得苯并二氢呋喃环结构化合物1,1经甲基化反应得2.1和2分别在无水碳酸钾、10%氢氧化钠水溶液等不同的碱性条件下进行反应,获得了11个苯并二氢呋喃环开环产物,即8—5′新木脂素类化合物3a~9b,实现了由苯并二氢呋喃新木脂素向8—5′新木脂素的转变,也为合成芪类化合物提供了一种新方法.C-8位上的吸电子基团如酯基的影响使苯并二氢呋喃环易在碱性条件下开环形成8-5′新木脂素类化合物.所合成化合物的结构由MS,IR,^1H NMR和^13C NMR进行了表征. 相似文献
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采用量子化学从头算MP2方法在6-31G(d)基组水平上系统地研究了过氧仲丁基自由基内三个不同碳位上的氢原子向O—O基的端O转移的过渡态结构, 讨论了这些氢转移反应过程中相关化学键的变化, 并在此基础上进一步研究了氢转移产物解离的过渡态结构. 结果表明具有四元环、五元环、六元环结构的三个氢转移过渡态对应的氢转移反应位垒分别是195.86, 176.43, 122.49 kJ•mol-1; 相应的氢转移产物进一步解离的反应位垒分别是3.53, 126.23, 154.2 kJ•mol-1, 对应的最终产物分别为HO自由基和丁酮, HO2自由基和丁烯, HOOCHCH3和乙烯. 相似文献
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芳香胺参加的Mannich反应——3-芳氨基-3-苯基-1-(4-溴苯基)丙酮的合成 总被引:2,自引:0,他引:2
文献报道过芳香胺与苯甲醛生成的Schiff碱可在少量相应的芳香胺盐酸盐或浓盐酸催化下制备Mannich碱(Ⅰ),所用的Schiff碱系事先合成,且产率较低(15-68.9%)。本文报导用4-溴苯乙酮、苯甲醛和芳香胺在少量浓盐酸催化下能直接发生Mannich反应, 相似文献
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2-Arylaminomethyl-1-tetralone and 2-arylaminomethyl-6 (or 7)-methyl (or me thoxy) -1 - tetralone were synthesized by the Mannich reaction which was carried out directly on the condensation product of arylamine with formaldehyde or arylamine-HC1 and 1-tetralone derivatives in ethanol-HCl solution. Twenty-five compounds were obtained in high yields. 相似文献
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本文综述了用酮作为酸性组分合成Mannich碱的最近进展。内容包括:β-脂氨基酮、β-芳氨基酮的合成和分子内Mannich反应。 相似文献
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Li Yuan MOU Zi Yun LIN Li Ya ZHU* Xiao Tian LIANG Institute of Materia Medica Chinese Academy of Medical Sciencesand Peking Union Medical College Beijing Center for Biophysical Science Engineering University of Alabama at Birmingham 《中国化学快报》2001,(6)
Mannich reaction is widely used for the synthesis of many kinds of compounds1. In the synthesis of the derivatives of styryl ketonic Mannich bases, a one-pot method is used, in which ketone, secondary-amine hydrochloride, paraformaldehyde are refluxed together in alcohol2,3. In most cases the normal Mannich product MA is obtained. But when certain amine is used as the reactant, a side-product IM, instead of MA is obtained. MS and 1HNMR data indicate that compound IM is a new type of Man… 相似文献
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Jakub Iwanejko Elżbieta Wojaczyńska Justyna Trynda Magdalena Maciejewska Joanna Wietrzyk Andrzej Kochel Jacek Wojaczyński 《Tetrahedron》2017,73(16):2276-2282
Tests of antiproliferative activity of Mannich adducts of aromatic nucleophiles and a chiral bicyclic imine revealed a di-tert-butylphenol derivative as a promising compound for further exploration. To study the influence of substitution pattern and a configuration of stereogenic centers on the inhibition of cancer cell growth, a series of Mannich bases were obtained with a good to high diastereoselectivity from the reaction of the imine and three isomeric di-tert-butylphenols. Six new enantiopure adducts were isolated and fully characterized. Selected derivatives were shown to exhibit an interesting antiproliferative activity comparable to cisplatin. 相似文献
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TheoreticalStudiesontheMechanismofMannichReactionInvolvingIminiumSaltasPotentialMannichReagent(1)——UseAcetaldehydeasPseudo┐ac... 相似文献
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Jiao Wang~a Ying Zhong~ 《中国化学快报》2008,19(4):387-389
Five new C-8 Mannich base derivatives of irisolidone 2a-2e were synthesized and their nitric oxide(NO)production inhibitory activity was evaluated.Compounds 2a,2b,2c and 2e displayed stronger activities in vitro than the parent compound irisolidone. 相似文献
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An aminophenol ligand, N,N,N'-tri(2-hydroxy-5-methylbenzyl)-l,2-ethanediamine, was prepared through the Marmich reaction, and structurally characterized by NMR, IR, MS and single-crystal X-ray diffract... 相似文献