水溶性C60-β丙氨酸衍生物清除超氧阴离子自由基O-·2及对小鼠胸腺细胞生长影响的研究

合成具有特殊生物活性的富勒烯衍生物及其生物活性的研究是近年来十分活跃的研究领域.许多实验显示C 60衍生物在抗爱滋病毒、神经保护、抗菌、 DNA切割和光动力学治疗等方面具有良好的应用前景[1]. 其中C 60衍生物对自由基的清除显得十分重要[2].     

一锅法合成开链片螺素-吡咯异喹啉羧酸乙酯

片螺素(Lamellarins)是一类从海洋软体动物中提取的具有良好生物活性的吡咯类生物碱.自1985年,Faulkner等首次从前腮亚纲软体动物中提取出片螺素A-D[1]后,国内外便开始对各类片螺素及其衍生物的全合成进行研究,至今相关合成报道络绎不绝[2][3].与此同时多种开链片螺素也是一类具有特殊生物活性的吡咯类生物碱,由于目前还未有关其提取的报道,因此对其进行合成具有重要意义.     

乙酰基吡嗪的合成及应用研究进展

乙酰基吡嗪是一类重要的有机合成中间体,由于它具有良好的生物活性和反应活性,近年来在有机合成中引起了人们的广泛关注.因此,对乙酰基吡嗪的合成、反应和应用方面的研究进行了概括和总结.     

过渡金属脒配合物的合成与应用研究进展

脒及其衍生物是一类具有广泛而良好生物活性的有机物,也是重要的有机合成中间体.脒作为一类良好的配体,具有多种成键类型,所生成的脒过渡会属配合物也具有很多特殊性质与重要用途.本文主要综述了脒配合物合成方法的进展及其性能与应用.其中腈胺加成"一锅"法制备脒配合物的有效性和方便性.不但可以利用过渡金属诱导有机腈与胺耦合成眯,而...     

右旋肌醇甲醚唑类核苷类似物的合成

糖基部分中氧原子被亚甲基代替的碳环核苷是核苷类药物发展的一个重要方向.这类化合物表现出了比较宽的生物活性谱,特别是作为抗肿瘤[1]和抗病毒[2]药物的开发具有良好的前景.     

叔烯酰胺的催化不对称串联反应快速合成吲哚里西丁生物碱类似物

正吲哚里西丁类生物碱的结构复杂多变,手性中心多,具有良好的抗癌、抗病毒等生物活性,但由于其毒性等原因很少直接用于临床.高效、高选择性地合成吲哚里西丁类生物碱衍生物及其类似物具有重要的意义.其合成目前主要是通过贵金属的不对称催化氢化来实现,很少通过催化不对称串联反应合成的报道来完成.近年来,清华大学化学系王梅祥课题组致力于开发稳定叔烯酰胺的反应及其在天然产物和生物活性分子合成中的应用.最近,他们成功     

2-芳基苯并[b]呋喃衍生物的生物活性与合成策略

2-芳基苯并呋喃是一类广泛存在于植物中的化合物,具有良好的抗病毒、抗肿瘤、抗真菌、抗氧化等生物活性,一直以来都引起人们的广泛关注.综述了近年来2-芳基苯并呋喃类化合物的研究进展,重点介绍其生物活性和合成方法,尤其是苯并呋喃环的构建方法.     

α-氰基丙烯酸酯及其衍生物的合成与农药生物活性研究进展

丙烯酸酯是一类具有良好生物活性的化合物, 由于它作用机制新颖、环境友好, 故其分子设计和合成及生物活性成为目前农药创制的热点之一, 按其在农药应用方面的不同活性作用进行分类, 综述了丙烯酸酯及其类似物的合成、生物活性与除草活性方面构效关系的研究进展.     

瑶药野葛花化学成分抑菌活性的追踪研究

采自广东连南的野葛花,属于峨嵋葛类(Pueraria omeiensis),是传统的瑶药之一,对其化学成分及药理活性的研究至今未见报道.我们通过建立体外动物实验模型,把化学分离与生物活性结合起来,以期筛选出具有良好生物活性的有效成分.     

松香树脂酸及其衍生物的生物活性研究进展

松香树脂酸是一种重要的天然可再生资源,具有独特的化学结构和多个手性中心,表现出广泛的生物活性,在医药及农药等领域有着重要的用途.本文按照松香树脂酸衍生合成的特点,对松香树脂酸及其衍生物的生物活性研究进展进行了综述,并对松香树脂酸及其衍生物的生物活性研究前景进行了展望.     

Advances in the Synthesis of Ring-Fused Benzimidazoles and Imidazobenzimidazoles

This review article provides a perspective on the synthesis of alicyclic and heterocyclic ring-fused benzimidazoles, imidazo[4,5-f]benzimidazoles, and imidazo[5,4-f]benzimidazoles. These heterocycles have a plethora of biological activities with the iminoquinone and quinone derivatives displaying potent bioreductive antitumor activity. Synthesis is categorized according to the cyclization reaction and mechanisms are detailed. Nitrobenzene reduction, cyclization of aryl amidines, lactams and isothiocyanates are described. Protocols include condensation, cross-dehydrogenative coupling with transition metal catalysis, annulation onto benzimidazole, often using CuI-catalysis, and radical cyclization with homolytic aromatic substitution. Many oxidative transformations are under metal-free conditions, including using thermal, photochemical, and electrochemical methods. Syntheses of diazole analogues of mitomycin C derivatives are described. Traditional oxidations of o-(cycloamino)anilines using peroxides in acid via the t-amino effect remain popular.     

Pyrimido[1,2-a]benzimidazoles: synthesis and perspective of their pharmacological use

Chemistry of Heterocyclic Compounds - The review presents data on the synthesis as well as studies of biological activity of new derivatives of pyrimido[1,2-a]benzimidazoles published over the last...     

阻燃剂苯并咪唑的微波合成研究进展

苯并咪唑类化合物广泛应用于医药、农药等领域,也在阻燃剂中具有重要应用.因此,利用微波辅助方法快速、高效地合成苯并咪唑类化合物已成为近年来的研究热点,本文对此进行了综述,并从经济与规模化制备苯并咪唑等方面进行了展望.     

Conversion of sterically hindered diacylated 1,2-phenylenediamines into 2-substituted benzimidazoles

A series of bulky 2-substituted benzimidazoles was designed in order to find new leads for several biological targets. Formation by cyclodehydration from their monoacylated counterparts was shown to be strongly dependent upon the nature of the acyl group. In the case of a dicyclohexylmethyl group, cyclization was only observed in a p-toluenesulfonic acid/toluene mixture from the symmetrical diacylated precursor. Analysis of the mechanism was begun starting from mixed diacylated derivatives.     

Chiral benzimidazoles and their applications in stereodiscrimination processes

Chiral aspects of benzimidazoles have been over-shadowed for a long time due to the large number of reports on benzimidazoles in the medical field in numerous categories of therapeutic agents. The vigorous research activity in chiral applications of benzimidazole derivatives started after bifunctional benzimidazoles made their appearance especially in the last 2–3 decades. Thus, chiral benzimidazoles form a comparatively young branch of chiral chemistry. The presence of pyridine and pyrrole type of nitrogens along with the fused benzene ring confer on this class of molecules, special properties including useful nucleophilicity, hydrogen bonding ability and a rigid backbone, all of which play decisive roles in proven chiral applications. The present review aims to cover the synthetic routes to access chiral benzimidazoles and their applications in a plethora of chiral fields including enantioselective organocatalysis, metal-based catalysis, asymmetric transformations involving benzimidazole-N-heterocyclic carbenes, kinetic resolution, benzimidazole-based macrocyclic hosts in chiral supramolecular chemistry and other miscellaneous chiral applications.     

Imidazolium chloride-catalyzed synthesis of benzimidazoles and 2-substituted benzimidazoles from o-phenylenediamines and DMF derivatives

A facile, general, and economical synthesis of diversely functionalized benzimidazoles and 2-substituted benzimidazoles has been realized via the imidazolium chloride-catalyzed cyclization of o-phenylenediamines with DMF derivatives. This protocol shows a broad substrate scope for aliphatic, aromatic, and heteroaromatic amides. A series of benzimidazoles and 2-substituted benzimidazoles have been obtained in moderate to excellent yields.     

某些1-酰基苯并咪唑及1-酰基咪唑衍生物的合成

2-取代的苯氧甲基苯并咪唑、咪唑分别与酰氯在缚酸剂存在下反应,制备了24个新的1-酰基2-苯氧甲基苯并咪唑及1-苯氧乙酰咪唑衍生物.后者容易吸水,转变成相应的铵盐.所制得的化合物中某些经小麦垂直生长法测定表现出一定的促进或抑制生长活性.     

低价钛促进的苯并咪唑并[1,2-c]喹唑啉衍生物的合成

利用低价钛试剂促进的2-邻硝基苯基苯并咪唑与原甲酸酯或丙酮或固体光气的反应, 合成了一系列苯并咪唑并[1,2-c]喹唑啉衍生物, 化合物的结构经IR, 1H NMR, MS和元素分析确定, 化合物4c的结构经单晶X射线衍射分析进一步确证. 该方法具有原料易得、操作简便和产率高等优点.     

N-(酰基二茂铁)苯并咪唑类化合物的合成和表征

将二茂铁磺酰氯或二茂铁甲酰氯和1H-苯并咪唑衍生物反应,合成了12个未见文献报道的N-(酰基二茂铁)苯并咪唑类化合物,用IR、1HNMR、元素分析和MS对其结构进行了表征。结果表明,含有活泼氢的苯并咪唑衍生物能与二茂铁酰氯生成相应的N-(酰基二茂铁)苯并咪唑衍生物,并有较好的收率。     

Studies in the field of sulfanilides

2-(N-Arylsulfonyl-N-phenylaminoethyl)benzimidazoles and some of their derivatives have been synthesized.