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将邻羟苯基引入1,2,3-三唑结构中, 设计合成了10个1-(4-取代苯基)-4-苯基-5-取代-1,2,3-三唑类衍生物. 首先, 以对位取代的芳胺为原料, 经重氮化、叠氮化、闭环和缩合反应制得1-(4-取代苯基)-4-苯基-5-水杨醛亚胺-1,2,3-三唑类衍生物(3a~3e), 再用硼氢化钠还原制得1-(4-取代苯基)-4-苯基-5-(2-羟基苄基)氨基-1,2,3-三唑类衍生物(4a~4e). 目标化合物的结构经核磁、IR及元素分析确认. 抑菌活性测试表明, 当质量浓度为0.1 mg/L时, 除化合物3e和4e外, 所有化合物对白色念球菌的抑菌率均达95%以上, 对大肠杆菌的抑菌率达85%以上, 具有强抑菌活性, 表明该类化合物在抗菌药物开发方面有重要应用价值. 相似文献
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本文设计一条新的合成路线,以价廉的异香兰素、间苯二酚为起始原料,通过Dakin反应、乙酰化、酚羟基醚化等系列反应得到目标化合物1-(2,4二异丙基氧基苯基)乙酮(5b)和新化合物1-(2,4二异丙基氧基-5-甲氧基苯基)乙酮(5a)。通过对化合物(5a)进行条件因素探索,得出合成(5a)的最佳反应条件,并通过1H NMR、MS、熔点等技术手段对其进行结构的确认与表征。 相似文献
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以5(6)-硝基-1-(4-硝基苯基)-1,3,3-三甲基茚满为原料,Pd/C为催化剂,用氢气还原合成5(6)-氨基-1-(4-氨基苯基)-1,3,3-三甲基茚满。红外、核磁表征了产物结构;考察了反应温度、反应时间、充入氢气压力及催化剂用量四个因素,设计正交试验对还原工艺条件进行优化分析。结果表明,对粗产率的影响显著程度依次为充入H2压力、反应时间、反应温度和催化剂用量,获得了优化工艺条件,即反应温度70℃、反应时间为2 h、充入H2压力为1.5 MPa,催化剂用量为5(6)-硝基-1-(4-硝基苯基)-1,3,3-三甲基茚满的10%。 相似文献
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1,1,3,3-四(全氟己基乙基)二锡氧烷二聚体在环氧化合物开环反应中的催化作用 总被引:2,自引:0,他引:2
采用氟碳-有机溶剂两相催化体系,考察了1,1,3,3-四(全氟己基乙基)二锡氧烷二聚体(1)在环氧化合物开环反应中的催化作用.结果表明,催化剂(1)在氟碳-有机溶剂两相体系中使环氧苯乙烯和甲醇的开环反应产率高达95%,13CNMR谱表明,开环反应的区域选择性为100%.在氟碳-有机溶剂两相催化体系中以一锅法制备了3-苯基丙酸2-甲氧基-2-苯乙醇酯,收率高,方法简便,催化剂几乎可以定量回收循环使用. 相似文献
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以3,5-二甲氧基苯甲酸(1)为起始原料, 经过甲醇酯化、氢化铝锂还原、四溴化碳溴代和Wittig-Horner反应,高产率的合成了Wittig-Horner试剂(5). 化合物5与对羟基苯甲醛(6)的羟基保护产物(7)偶联得到化合物(8),后者经去甲氧基亚甲基保护和仿生氧化偶联反应成功地全合成了(E)-脱氢二聚白藜芦醇-11,11′,13,13′-四甲醚(10). 通过1H NMR、13C NMR、IR、HRMS等测试技术确定化合物10为二聚芪类化合物(E)-脱氢二聚白藜芦醇-11,11′,13,13′-四甲醚,总收率48.93%. 相似文献
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Fangming Kong Tianmin Zhu Weitao Pan Russ Tsao Thomas G. Pagano Bao Nguyen Brian Marquez 《Magnetic resonance in chemistry : MRC》2012,50(12):829-833
A contracted ring degradation product, WYE‐120318 (compound 2), was discovered during the development phase for methylnaltrexone bromide (compound 1) drug substance. The compound was isolated by high‐performance liquid chromatography fractionation, and its structure was determined by spectroscopic data analyses. WYE‐120318 is formed from methylnaltrexone through a benzyl‐benzilic acid type rearrangement reaction to yield an α‐hydroxy‐cyclopentanecarboxylic acid substructure. The proposed structure and the formation mechanism are confirmed by the synthesis of WYE‐120318 from methylnaltrexone (compound 1). A similar benzyl‐benzilic acid type rearrangement reaction can be envisioned as the biological origin of remisporine A (compound 3), a naturally occurring cyclopentadienyl compound that autocatalytically dimerizes to remisporine B (compound 4). The structure of remisporine A was deduced from its dimer 4. Coniothyione (compound 5) can be considered as the first example of a stable natural product bearing the remisporine A skeleton. However, the regiochemistry of the chlorosubstitution in the coniothyrione structure needs to be revised to compound 6 on the basis of the nuclear magnetic resonance data and biogenesis analysis. Copyright © 2012 John Wiley & Sons, Ltd. 相似文献
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合成了一个新型的双核Pt(Ⅳ)配合物{[cis-Pt(NH3)2Cl(OH)2]2(4,4'-methylenedianiline)}(NO3)2(化合物1)及相应的 15N标记化合物{[cis-Pt(15NH3)2Cl(OH)2]2(4,4'-methylenedianiline)}(NO3)2(化合物15N-1).利用1H NMR和ESMS进行了结构表征,化合物15N-1的2D[1H,15N]HSQC NMR发现,该化合物在水溶液中存在同分异构体.2D[1H,15N]HSQC NMR技术跟踪了化合物15N-1与Guanosine-5'-Monophosphate(5'-GMP)和Glutathione(GSH)的反应.结果显示,5'-GMP能在0.5 h内将化合物1还原,而GSH在6 h以后才能够部分的将化合物1还原.化合物1所表现出来的反应性能将有利于提高其治疗效果和降低毒副作用. 相似文献
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Teppei Yoshioka Md Zahangir Alam Tomonari Ogata Takamasa Nonaka Seiji Kurihara 《Liquid crystals》2004,31(9):1285-1291
Several chiral azobenzene compounds having different chiral substituents were synthesized. A cholesteric phase was induced by mixing each chiral azobenzene compound with a host non-chiral nematic liquid crystal (E44). The helical twisting power (HTP) as well as the change in HTP by trans-cis photoisomerization of the chiral azobenzene compound was dependent on the structure of the chiral substituents. A compensated nematic phase was induced by combination of E44, a chiral azobenzene compound and a non-photochromic chiral compound. Reversible switching between the compensated nematic phase and cholesteric phase was brought about by trans-cis photoisomerization of the chiral azobenzene compound in the liquid crystalline systems. An azobenzene compound substituted with a menthyl group showed the highest efficiency as the trigger for the switching; this efficiency was related to the compactness of the chiral group substituted within the azobenzene core moiety. 相似文献
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