3-芳亚甲基联氨羰基-5-(对位取代苯基)-吡唑衍生物的 合成、结构和生物活性

以4-取代苯乙酮及草酸二乙酯为起始原料, 设计合成了20个新的3-芳亚甲基联氨羰基-5-(对位取代苯基)-吡唑衍生物, 产率较高. 所合成的化合物经元素分析, IR, 1H NMR对其结构进行了表征, 化合物4b, 4h还通过X-ray单晶衍射进一步确证了其结构. 初步生物活性实验结果表明, 所合成的化合物对绿豆发芽过程有着较好的生长调节作用.     

金催化选择性氧化共轭炔基炔酰胺合成4-羰基丁-2-炔酰胺（英文）

通过金催化选择性氧化1,3-共轭炔基炔酰胺,为4-羰基丁-2-炔酰胺化合物的合成提供了一种新的方法.这种含有活化的不饱和炔烃的1,4-双羰基化合物是有机化学中一种重要的合成子.利用该金催化氧化方法,可以高度选择性地对共轭炔烃的1,4-位进行氧化得到2-炔-4-羰基丁酰胺化合物,而不是生成较为常见的1,2-双羰基化合物.在该选择性氧化的条件下,可以以较高的收率得到一系列4-羰基丁-2-炔酰胺化合物.     

α -重氮-β -二羰基化合物在有机合成中的应用

叙述了α-重氮-β-二羰基化合物的制备,详细讨论了它们作为合成子在有机合成中的应用。     

3-羟基-6-腙及6-羰基-3-腙胆甾烷的合成及抗肿瘤活性评估

以胆甾醇为原料,通过不同的合成方法,制备得到8个新的具有3-羟基-6-腙及3个6-羰基-3-腙结构的胆甾烷腙衍生物,所有合成化合物都通过了IR,NMR及HRMS的结构表征.另外,采用人肝癌细胞(Bel-7404)及胃癌细胞(SGC-7901)对合成化合物的抗肿瘤活性进行了研究,结果表明所合成的3-羟基-6-腙胆甾烷衍生物对所测试的肿瘤细胞株表现出明显的生长增殖抑制活性,本研究结果为甾体抗肿瘤药物的合成研究提供了有用的参考.     

几种新型的耐高温耐水解的聚苯基-1,2,4-三嗪

由对苯二酰胺腙和五种不同的芳族四酮分别进行缩聚反应,可以合成五种新的聚苯-1,2,4-三嗪,对它们进行了表征。η_(比粘)介于1.39—2.16分升/克范围内。这些高聚物可以浇铸成韧性的薄膜,涂制成漆包线,具有良好的耐温性、耐水解性、耐溶剂性、电绝缘性及力学性能等。     

噻吩并[2,3-b]吡啶类化合物的合成及生物活性

用邻氨基噻吩腈与不同结构的二羰基化合物反应,合成了新的多取代噻吩并吡啶类衍生物4-氨基-5-取代羰基噻吩并[2,3-b]吡啶-6-酮。用元素分析、红外光谱、核磁共振氢谱和质谱等测试技术对所合成化合物的结构进行了表征。初步生物活性测试表明,该类化合物有较好的杀菌活性和一定的除草活性。     

(4-甲基-1,3-二噻烷-2-亚甲基)-1,7-二芳基-1,6-二烯-3,5-二酮的合成

从2,4-戊二酮和1,2,3-三溴丙烷出发合成了一类新的α-羰基二硫缩烯酮类化合物,并以其为底物合成了(4-甲基-1,3-二噻烷-2-亚甲基)-1,7-二芳基-1,6-二烯-3,5-二酮类化合物,通过IR和1H NMR方法对其进行了表征.     

可见光诱导的醇的选择性氧化

在蓝光照射的无金属、 无添加剂的绿色温和条件下, 以2-氯蒽醌为光催化剂, 空气/氧气为氧化剂, 高选择性地将芳族与杂芳族取代的伯醇和仲醇转化为相应的羰基化合物. 实验结果表明, 该催化剂具有较宽的底物适用范围, 为苄基位含氧化合物的合成提供了一条经济、 环保和可持续的新路径, 具有潜在的应用前景.     

3-甲基-4-乙氧基(二乙氨基)羰基-1H-吡唑衍生物的合成 及其生物活性

以乙酰乙酸乙酯的二硫缩醛为原料,分别合成了1-磺酰基-3-甲基-4-乙氧基(二乙氨基)羰基-5-甲硫(甲磺酰)基-1H-吡唑和1-甲酰基-3-甲基-4-乙氧基羰基-5-甲硫基1H-吡唑。元素分析、1^HNMR证实了它们的结构,部分化合物经过MS和IR的证实。初步的生测结果表明部分化合物对芦笋茎枯病和番茄早疫病具有较好的效果。     

α-羰基一硫代半缩醛与脂肪族脲反应合成2, 4-咪唑啉二酮衍生物

利用α-羰基一硫代半缩醛与脂肪基取代脲反应合成了六个新的咪唑啉二酮类衍生物。并用IR,NMR,MS和元素分析进行测定,最后用X四圆衍射仪确定了它们的结构。     

Design,stereoselective synthesis and computational calculations of novel hybrid compounds via Pauson-Khand reactions

A series of novel chiral hybrid compounds between benzofuran and bicyclic cyclopentenone and also benzothiophene and bicyclic cyclopentenone have been designed and synthesized. Chiral enynes derived from enantiomerically enriched homoallyl and homopropargyl alcohols were converted into bicyclic cyclopentenone structures by intramolecular Pauson-Khand reactions. This strategy provides a facile access to various bicyclic cyclopentenones substituted with benzofuran or benzothiophene ring systems in good yields. In addition to the experimental work, the ground state geometries of the hybrid compounds were optimized using Density Functional Theory applications at the B3LYP/6-31G(d,p) level in order to obtain information about the 3D geometries and electronic structure.     

An Efficient Solid Acid Promoted Synthesis of Quinoxaline Derivatives at Room Temperature

Quinoxaline derivatives have been synthesized in a very short time with excellent yields by the condensation of 1,2-diamines with aliphatic or aromatic 1,2-dicarbonyl compounds or benzilmonoxime in the presence of silica sulfuric acid as a very inexpensive solid acid catalyst at room temperature. The recovery and reuse of the catalyst are also satisfactory.     

苯并异噻唑啉酮类化合物的合成与活性研究

通过烷基醇与固体三光气(BTC)反应后加入1,2-苯并异噻唑啉-2(3H)-酮(BIT)继续反应的“一锅法”制备了8种未见文献报道的2-(苯并异噻唑啉-3-酮-2-基)甲酸酯类化合物.化合物结构经IR、1HNMR和元素分析确认,并且对枯草芽孢杆菌、金黄色葡萄球菌、嗜水单细胞菌和大肠杆菌进行了初步抑菌活性实验,实验结果表...     

KF/Al2O3催化下芳醛和4-羟基喹啉-2-酮的反应研究

以芳醛和4-羟基喹啉-2-酮为原料, 在KF/Al₂O₃催化下以乙醇为溶剂, 在80 ℃合成了一系列新的双(4-羟基-2-氧代喹啉-3-基)-芳基甲烷衍生物, 反应条件温和, 产率较高, 并通过IR, ¹H NMR和元素分析确证产物的结构.     

ACC对羰基化合物、含苄基化合物及稠环芳烃中活泼碳氢键的选择性氧化

前文曾报道了几种以铵盐或氯化铵为配体与三氧化铬所形成的配合物(CH_3)_3NHCrO_3Cl、(CH_3)_2NH_2CrO_3Cl、CH_3NH_3CrO_3Cl和NH_4CrO_3CI。它们都是高效、温和的醇和肟类选择性氧化剂。其中,NH_4CrO_3Cl(ACC)是最廉价的,具有制备简单、性质稳定、选     

Synthesis of novel scaffolds based on thiazole or triazolothiadiazine linked to benzofuran or benzo[d]thiazole moieties as new hybrid molecules

Abstract

A synthesis of novel hybrid molecules containing thiazole or bis(thiazoles) each bearing benzofuran and/or benzo[d]thiazole moieties by the reaction of the appropriate thioamide derivatives with the corresponding bis-bromoacetyl derivatives is reported. Mono- and bis(triazolothiadiazine) derivatives based on benzofuran or benzo[d]thiazole moieties were also synthesized in good yields by the reaction of the appropriate bis(bromoacetyl) derivatives with each of 4-amino-5-mercapto-1,2,4-triazoles and their corresponding bis-derivatives.     

Investigation of nitrogen‐rich energetic polymers based on alkylbridged bis‐(1‐methyl‐tetrazolylhydrazines)

Nitrogen‐rich energetic polymers were synthesized by the polyaddition reaction of 1,2‐bis(5‐monomethylhydrazinyl‐1H‐tetrazolyl)ethane ( 1a ), 1‐methyl‐1,2‐bis(5‐monomethylhydrazinyl‐1H‐tetrazolyl)ethane ( 1b ), and 1,4‐bis(5‐mono‐methylhydrazinyl‐1H‐tetrazolyl)butane ( 1c ) with hexamethylene diisocyanate. The experiments showed that neither a polymerization from solution or bulk was possible. Therefore, a new method for the polymerization of tetrazolyl hydrazines had to be developed. The formed polymers were characterized by vibrational spectroscopy (IR) and elemental analysis. The energetic properties were investigated by bomb calorimetric measurements along with calculations using the EXPLO5 software. The thermal stability was investigated by DSC measurements. The properties render the polymers into promising compounds regarding an application as energetic binder. © 2009 Wiley Periodicals, Inc. J Polym Sci Part A: Polym Chem 48: 122–127, 2010     

Cascade synthesis of benzofuran derivatives via laccase oxidation-Michael addition

The cascade synthesis of benzofuran derivatives was conducted from the reaction of catechols and 1,3-dicarbonyl compounds via oxidation-Michael addition in the presence of laccase and Sc(OTf)₃/SDS. This reaction was carried out under air at room temperature in aqueous medium, and provided benzofuran products in moderate to good yields. In addition, this reaction system showed recyclability.     

Arylpyrazole as selective anti-enterococci; synthesis and biological evaluation of novel derivatives for their antimicrobial efficacy

Exploring the structure–activity relationships (SAR) of a new set of phenylpyrazoles unveiled a potential anti-enterococcus lead compound 12 . The benzofuran moiety linked to the phenylpyrazole 12 was 32 times better than vancomycin against Enterococcus faecalis ATCC 51299. Besides, compound 12 is expected to have an excellent oral bioavailability according to the in silico studies. Of SAR analysis, we found that the benzofuran side chain was essential for the activity. Changing the benzofuran with either benzothiophene, phenyl, pyridinyl, tolyl, or naphthyl reduces/nullifies the pharmacological action. Besides the anti-enterococcal activity, derivatives 4 and 6 can be used to develop new broad-spectrum antibiotics as they exhibited activity against the wild-type highly virulent Escherichia coli isolate. Moreover, compound 13 was proved to show antifungal activity (MIC = 4 μg/ml) against the Candida albicans SS5314 (wild type). Finally, the in silico analysis showed that those compounds have good profiles regarding the absorption, distribution, metabolism, and excretion studies, drug-likeness and pharmacokinetics properties.     

Recent Advances in the Cycloaddition Reactions of 2‐Benzylidene‐1‐benzofuran‐3‐ones,and Their Sulfur,Nitrogen and Methylene Analogues

Benzothiophene, benzofuran, indole, and indene derivatives are privileged heterocyclic motifs. These are present in a wide range of bioactive natural products and pharmaceutical drugs and are the subject of materials science research. However, the construction of benzothiophene, benzofuran, indole, and indene frameworks have been long‐standing challenges to organic chemists. In this review, we classify the derivatives of four structures synthesized from 2‐benzylidene‐1‐benzofuran‐3‐one and their analogues in terms of their ring size (from three‐ to ten‐membered) and type (fused or spiro), as well as summarizing the developments of this field. Finally, we discuss the ring opening and 1,4‐addition reactions.