2,5-二[4-(2-芳基乙烯基)苯基]噁二唑的合成及发光特征

二乙烯联苯及其衍生物是一种可发射蓝光的小分子空穴型有机发光材料, 通过Wittig-Horner反应, 将电子传输型噁二唑环“嵌入”其中, 设计合成了6个2,5-二[4-(2-芳基乙烯基)苯基]-1,3,4-噁二唑化合物. 经光谱分析和元素分析等方法确认了它们的化学结构. IR和UV-vis分析数据表明标题化合物分子结构中的C＝C双键均为反式结构特征. 研究结果表明: 2,5-二[4-(2-对二甲氨基苯基乙烯基)苯基]-1,3,4-噁二唑具有良好的蓝色发光性能; 取代基对标题化合物的UV-vis吸收光谱和发光特性的影响显着.     

Stereoselective Synthesis of （E）-α-Aryltellurenylvinyl-stannanes and Their Application in the Synthesis of Stereodefined Trisubstituted Alkenes

(E)-α-Aryltellurenylvinylstannanes have been synthesized stereoselectively via the hydrozirconation of alkynylstannanes, followed by the reactions with aryltellurenyl iodides. (E)-α-Aryltellurenylvinylstannanes can undergo sequential cross coupling reactions with both electrophiles and nucleophiles in the presence of transition metal complexes to form two carbon-carbon bonds in the same olefinic carbon leading to trisubstituted alkenes stereoselectively.     

Synthesis and electrochemical properties of 2,6-bis（6-aryl-[1,2,4]- triazolo[3,4-b][1,3,4]-thiadiazole-3-yl）pyridines

By the condensation of 2,6-bis（4-amino-5-mercapto-[1,2,4]-triazoles-2）pyridine with aromatic acid in the presence of phosphorus oxychloride. Compounds of 2,6-bis（6-aryl-[1,2,4]-triazolo[3,4-b][1,3,4]-thiadiazole-3-yl）pyridines were synthesized. Their structures were confirmed by IR, ^1H NMR spectroscopies and elemental analysis. Their electrochemical behavior and cyclic voltammogram also were be studied. The results showed that they have high ionization potentials and good affinity.     

L-脯氨酸催化下甲基酮和1-芳基-2,2,2-三氟乙酮的不对称Aldol反应

Direct asymmetric aldol addition of methyl ketones to 2,2,2-trifluoro-1-phenylethanone and its ring-substituted derivatives was achieved using L-proline as a chiral promoter. Various optically active β-trifluoromethyl-β-hydroxy ketones were obtained in almost quantitative yields with moderate enantioselectivities up to 64 % ee.     

芳基三氮烯4-位取代基对抗癌活性影响的构象分析

传统的药物设计和新药开发主要是依靠随机筛选,这种方法误差大,且需要费大量时间和经费,其结果也经常不能达到预期的设想。即使是一个国际性的大制药集团,每年平均要合成上万个化合物才能从中筛选出一个可以成为商品的新药。这种状况迫使我们去寻找一条新的打破常规的途径研究新药。近年来,随着计算机图形系统的广泛应用,对药物构效关系的研究得到了卓有成效的发展,取得了一些成功的例子。如抗菌抗癌琥珀酰-L脯氨酸就是计算化学与分子图形技术相结合的成果,目前已投放市场。     

One-pot synthesis of N-aryl propargylamine from aromatic boronic acid,aqueous ammonia,and propargyl bromide under microwave-assisted conditions

A facile,one-pot synthesis of N-aryl propargylamine from aromatic boronic acid,aqueous ammonia,and propargyl bromide has been achieved under microwave-assisted conditions.The reactions can be smoothly completed within a total 10 min through a two-step procedure,including copper-catalyzed coupling of aromatic boronic acids with aqueous ammonia and following propargylation by propargyl bromide.     

镍催化环丁酮肟酯与芳基锌试剂的Negishi偶联反应

发展了一种镍催化环丁酮肟酯和芳基锌试剂之间Negishi偶联的方法.镍既作为亚胺自由基的引发剂,也作为芳基锌试剂与烷基自由基偶联反应的催化剂在反应中起作用.本方法可避免使用剧毒的氰化物,且具有很广的底物适应性和官能团兼容性,因此可能是一种具有潜在吸引力的高效合成烷基腈类化合物的新策略.初步的机理研究显示,该反应极可能经历自由基历程.     

双核芳基Os(Ⅱ)配合物的合成及诱导肿瘤铁死亡机制

本文报道了一种双核锇Os(Ⅱ)配合物[Os （η⁶-bip）（1，3-bib） Cl]₂Cl₂（bib-Os），其中η⁶-bip=η⁶-联苯，1，3-bib=1，3-二（1H-咪唑-1-基）苯。并通过¹H NMR和ESI-MS进行基础表征。配合物bib-Os具有良好的脂溶性，易在细胞中积累。配合物bib-Os对人卵巢癌A2780细胞表现出高效的抗增殖活性，可产生活性氧（ROS）并诱导线粒体损伤。脂质过氧化物（LPO）积累、谷胱甘肽（GSH）消耗和谷胱甘肽过氧化物酶4（GPX4）下调表明，配合物bib-Os诱导A2780细胞死亡的主要机制是铁死亡，bib-Os是第一例诱导肿瘤细胞铁死亡的Os金属配合物。     

Room-Temperature Bismuth-Catalyzed Bis-arylation of Carbonyl Compounds with Aryl Ethers and Phenols

Using Bi2（SO4）3 as the catalyst and TMSCl as the additive, a wide variety of aldehydes, ketones, and acetals were smoothly condensed with aryl ethers at room temperature to provide the corresponding diarylmethanes and triarylmethanes selectively in good to excellent yields.