新型苯并咪唑衍生物的合成

以苯甲醛甘油缩醛和对甲基苯甲醛甘油缩醛为原料,采用次氯酸钠催化氧化法,制得2-芳基-4-羧基-1,3-二氧戊环中间体;中间体分别与邻苯二胺或N-甲基邻苯二胺反应,合成了4种新型苯并咪唑衍生物(3a~3d),收率为78.0%~80.5%,其结构经UV, ¹H NMR, ¹³C NMR, IR和HR-MS(ESI)表征。      

Fluoro-containing Heterocycles: VI. New Derivatives of 1,3,4-Thiadiazino[6,5,4-i,j]quinoline

A series of new tricyclic fluoroquinolones was prepared by replacing fluorine atoms in derivatives of 2-R-8-Y-7-oxo-9,10-difluoro-7H-1,3,4-thiadiazino[6,5,4-i,j]quinoline-6-carboxylic acids. In acids and esters containing a hydrogen atom in position 8 occurred replacement of F¹⁰ by amine rests, and in compounds with a fluorine in position 8 was substituted either F⁸or F¹⁰ and F⁸depending on the amine character.     

苯并咪唑衍生物的合成改进

利用空气作氧化剂, 无需任何催化剂, 以甲醇作溶剂, 芳香醛与邻苯二胺反应一步合成苯并咪唑衍生物, 产率均超过69%, 产物的结构通过元素分析、红外光谱和核磁共振氢谱确证, 该方法具有操作简单、反应条件温和、环境友好的优点.     

新型苯并咪唑衍生物的合成及其生物活性

以香草醛为原料,经2步反应制得中间体--2-(4-羟基-3-甲氧基苯基)-1-氢-苯并咪唑(3); 3分别与取代苯甲酰氯,取代苯乙酰氯和取代苯磺酰氯反应,合成了13个新型的苯并咪唑衍生物(7a~7g, 8a, 8d, 8g, 9a, 9d和9g),其结构经¹H NMR, IR和HR-ESI-MS表征。分别用菌丝生长速率法和曹坳程法测试了7~9的抑菌活性和除草活性。结果表明：c=100 mg·L^-1时,7~9对番茄灰霉病菌,油菜菌核病菌和稻瘟病菌的抑制率分别为13.79%~65.38%, 13.88%~63.78%和34.22%~58.79%; c=300 mg·L^-1时,7g对稗草和反枝苋的芽长抑制率分别为40.20%和80.84%。     

二醋酸碘苯促进苯并咪唑类化合物的合成

二醋酸碘苯促进下, 由邻苯二胺或4-甲基邻苯二胺与各种芳醛通过一步反应合成了13种苯并咪唑类化合物, 反应时间3～5 min, 反应产率83%～98%, 用核磁共振、红外光谱、质谱和元素分析对产物的结构进行了表征. 该合成方法具有底物适用范围广、反应条件温和、反应速度快、反应产率高的优点. 根据实验结果对该反应提出了可能的反应机理.     

2种苯并咪唑衍生物在微波作用下的固相合成

2种苯并咪唑衍生物在微波作用下的固相合成;固相合成;微波辐射;苯并咪唑衍生物     

二茂铁磺酰基苯并咪唑衍生物的合成、表征及晶体结构

以苯并咪唑为原料，经硝化、二茂铁磺酰化，合成了六种未见报道的二茂铁磺酰基硝基苯并咪唑衍生物，其结构经元素分析、质谱、核磁共振确证。由于苯并咪唑的互变异构，经二茂铁磺酰化后，产生两个异构体，通过X射线衍射，测定了异构体的晶体结构。     

苯并咪唑类化合物一步法合成及表征

采用对甲氧基苯甲醛、对羟基苯甲醛和邻苯二胺直接关环合成了1-(对甲氧基苄基)-2-(对甲氧基苯基)-苯并咪唑、1-(对羟基苄基)-2-(对羟基苯基)-苯并咪唑化合物.通过元素分析、IR、核磁分析对它们进行了表征,并培养了1-(对甲氧基苄基)-2-(对甲氧基苯基)-苯并咪唑化合物晶体.该晶体经X射线衍射确定为正交晶系,空间群Pna2(1),a=2.0194(7)nm,b=1.5657(4)nm,c=0.5498(1)nm,α=90°,β=90°,γ=90°,V=1.7383(8)nm3,Z=4,Mr=344.40,Dc=1.316g/cm3,μ=0.85 cm-1,F(000)=728.     

新型苯并咪唑取代的丙烯腈衍生物的催化合成

从邻苯二胺出发,合成了2-腈甲基苯并咪唑,对2-腈甲基苯并咪唑与醛的Knoevenagel缩合反应催化剂进行了优选,研究表明,吗啡啉/乙酸是催化2-腈甲基苯并咪唑与芳香醛Knoevenagel缩合反应的良好催化剂;在吗啡啉/乙酸催化下,合成了新型的双苯并咪唑丙烯腈衍生物和3-吲哚-2-苯并咪唑丙烯腈衍生物;将2-腈甲基苯并咪唑经过碱性水解,酯化,得到苯并咪唑乙酸乙酯,后者经过次序Knoevenagel缩合/分子内酯交换高产率地得到了新型的苯并咪唑取代的香豆素衍生物。     

Fluoro-containing Heterocycles: V. Cyclization of 3-Azolylamino-2-polyfluorobenzoylacrylates

The heating of ethyl 3-azolylamino-2-polyfluorobenzoylacrylates in acetonitrile in the presence of KF gave rise to derivatives of 1-azolyl-substituted quinolones or azolo[1,5-a]pyrimidines.     

Synthesis and Characterization of Some New Benzimidazole Derivatives

Synthesis of nine new benzimidazole derivatives was reported. The products were identified by ¹H NMR, mass spectroscopy, and infrared spectroscopy.     

Synthesis and Crystal Structure of Ferrocenesulfonyl Benzimidazole Derivatives

Ferrocene derivatives have attracted much attention over the past two decades in many fields due to their diversebiological activities. [1,2] As a part of a continuing investigation into these compounds, we report here six novel com pounds and the crystal structure of 2a. The synthetic routes of the novel compounds are shown in Scheme 1.     

A Facile Synthesis of Novel Benzofuranyl Benzimidazole Derivatives

In this article, we report a facile route for the synthesis of novel benzofuranyl benzimidazole derivatives. The methodology involves the Sonagashira reaction of 2‐(3‐iodo‐4‐methoxyphenyl)‐1H‐benzimidazole ( 3 ) with variety of terminal alkynes to have novel benzimidazole alkynyl derivatives followed by iodo‐cyclisation to give novel iodo benzofuranyl benzimidazole derivatives. The resulting iodo benzofuranyl benzimidazoles were functionalized further via palladium mediated carbon–carbon bond formation for molecular diversity generating novel heterocyclic compounds.     

新型苯并咪唑衍生物的合成及其抗凝血活性

以3-［(3-氨基-4-甲基氨基苯甲酰)吡啶-2-基氨基］丙酸乙酯为原料,与4-氰基-3-氟苯取代基乙酸经环化反应制得3-【【2-｛［(4-氰基-3-氟苯取代基）甲基］-1-甲基-1-H-苯并咪唑-5-基｝羰基】吡啶-2-基】氨基丙酸乙酯（3a, 3e）; 3经水解和酰胺化反应制得3-【【【2-｛［(4-氰基-3-氟苯基)取代基］甲基｝-1-甲基-1H-苯并咪唑-5-基】羰基】吡啶-2-基氨基】丙酰取代胺基（6a~6h）;6与乙酰氧肟酸经环合反应合成了8个新型的苯并咪唑衍生物（7a~7h）,其结构经1H NMR和HR-ESI-MS表征。抗凝血活性结果表明： 7a和7c的抗凝血活性最好,其aPTT值分别为(83.1±4.2) s和(80.7±2.9) s,优于阳性对照药达比加群酯(75.3±2.1)s。     

Zeolite‐Catalyzed Environmentally Friendly Synthesis of Benzimidazole Derivatives

A simple and environmentally friendly synthesis of substituted benzimidazoles was developed using a small‐pore‐size zeolite. The similar reaction was not applicable to the preparation of 2‐substituted imidazolines.     

苯并咪唑与苯并异噁唑桥连衍生物的合成及其生物活性

以3-[(3-氨基-4-甲基氨基苯甲酰)吡啶-2-基氨基]丙酸乙酯为起始原料,经环合、水解、酰胺化等反应合成了5个新型的达比加群酯衍生物（5a~5e）,其结构经¹H NMR、 IR和HR MS(ESI)表征。并对5a~5e进行了凝血活酶抑制活性（IC₅₀）及生物利用度(F)测试。结果表明：化合物5c的抗凝血活酶活性(IC₅₀)和生物利用度(F)最好,分别为1.4±0.1（nM）和6.9%。     

新型苯并咪唑取代的丙烯腈及丙烯酸酯衍生物的催化合成

从邻苯二胺出发,合成了2-氰甲基苯并咪唑,在优选出的催化剂吗啡啉/乙酸催化下,合成了新型的双苯并咪唑丙烯腈衍生物和3-吲哚-2-苯并咪唑丙烯腈衍生物;将2-氰甲基苯并咪唑经过碱性水解、酯化,得到苯并咪唑乙酸乙酯,后者经过Knoevenagel缩合/分子内酯交换接续反应高产率地得到了新型的苯并咪唑取代的香豆素衍生物。     

Organocatalyzed One-Pot Synthesis of Substituted 1,5-Benzodiazepine and Benzimidazole Derivatives

An efficient synthesis of some heterocycles is described by condensation between o-phenylenediamine and 1,3-dicarbonyl compounds catalyzed by L-proline. The reaction is carried out either at room temperature or reflux depending on the substrates.