杯[4]芳烃硫脲基席夫碱衍生物的合成

对叔丁基杯[4]芳烃-1,3-二醛基衍生物与苯基氨基硫脲反应,高产率地合成了含硫脲基席夫碱单元的新型杯[4]芳烃衍生物,其结构经1H NMR,IR和ESI-MS表征。     

对羟基苯甲醛磷酸酯席夫碱衍生物的合成及其抗抑郁活性

以对羟基苯甲醛为起始原料,经醚化和酯化反应制得中间体4-（2-羟乙氧基）苯甲醛磷酸二甲酯（2）; 2分别与伯胺经缩合反应合成了4个对羟基苯甲醛磷酸酯席夫碱衍生物（4a~4d）,其结构经¹H NMR, ¹³C NMR, IR和ESI-MS确证。采用应急模型对4a~4d进行抗抑郁活性研究。初步结果表明： 2和4-（2-羟乙氧基）苯甲醛磷酸二甲酯甲氧基胺席夫碱（4d）表现出较好的抗抑郁活性,2的活性优于丙咪嗪,4d的活性与丙咪嗪接近。     

含D-氨基葡萄糖分子的酰基硫脲衍生物合成

以D-氨基葡萄糖盐酸盐为原料,经酰化保护羟基后得1,3,4,6-四-O-乙酰基-2-脱氧-β-D-氨基葡萄糖,再与芳酰基异硫氰酸酯反应,合成了12种新型的糖基酰基硫脲衍生物。实验表明,优化反应条件为芳酰异硫氰酸酯∶上述氨基葡萄糖=1∶1.2(摩尔比),在二氯甲烷溶液中加热至40℃,反应6 h。产物结构经IR、~1H NMR、~(13)C NMR分析确证。     

新型三氮唑席夫碱吡唑衍生物的合成

以乙醇为溶剂,乙酸为催化剂,1-苯基-3-甲基-5-氯-4-吡唑甲醛与4-氨基-5-取代苯基-1,2,4-三唑-3-硫酮于65℃反应4 h合成了7个新型的三氮唑席夫碱吡唑衍生物,收率74%~87%,其结构经1H NMR,IR和元素分析表征。     

两种新型双咔唑基席夫碱衍生物的合成及其光学性质

以N-乙基-3-甲酰基咔唑为原料,合成了两种新型的双咔唑基席夫碱衍生物——N1,N2-双(9-乙基咔唑-3-亚甲基)-1,2-乙二胺(1)和N1,N3-双(9-乙基咔唑-3-亚甲基)-1,3-丙二胺(2),其结构经1HNMR,IR和MS表征。用UV和单光子荧光光谱研究了1和2的线性光学性质。结果表明:1和2有望成为具有应用价值的发光材料。     

1,2,4-三唑双席夫碱衍生物的合成及表征

氨基均三唑硫醇1a～1b与1,2-二溴乙烷缩合制得双氨基三唑硫醚2a～2b, 2a～2b与芳香醛经缩合得相应的席夫碱3a₁～3a₅与3b₁～3b₇, 收率65%～80%. 所得席夫碱类新化合物的结构均经IR, ¹H NMR, MS和元素分析确证.     

席夫碱及其金属配合物的合成及生物活性研究进展

席夫碱及其金属配合物具有独特的抗菌、抗肿瘤和抗氧化等生物活性.为筛选高效低毒的药物,人们合成了大量不同类型的席夫碱及其金属配合物并对其生物活性进行了研究.本文综述了近年来席夫碱及其金属配合物的合成,以及在抗菌、抗氧化、抗肿瘤等方面生物活性的研究进展,并为进一步研究其在医药领域的应用提供了信息支持.     

硫脲化合物的合成及其生物活性

硫脲化合物的合成及其生物活性董燕红，司宗兴（北京农业大学应用化学系北京１０００９４）关键词噻二陛－甲酰基，硫脲，胺类，合成，生物活性酰基硫脲在抗真菌、抗结核、抗病毒、除草以及调节植物生长方面具有广泛应用［１，２］。１，２，３－噻二唑杂环作为有效前体正...     

苯磺酰硫脲衍生物的无溶剂合成

等物质的量的苯磺酰胺钠盐与异硫氰酸酯在封管中、无溶剂和130℃条件下反应,得到一系列苯磺酰硫脲衍生物,产率高到中等.产物结构通过IR,1H NMR,13CNMR,ESI-MS和元素分析的表征.     

Synthesis and physico-analytical studies of some novel ferrocenyl Schiff base derivatives

A series of ferrocenyl Schiff base derivatives was synthesized by condensation reactions of 1,1′-ferrocenedicarboxaldehyde and aromatic amines containing long chain alkyl groups as free ends which were characterized by their physical properties, elemental, FTIR, ¹H NMR, ¹³C NMR spectral and thermal analysis. The thermal behaviour of the synthesized compounds was studied by differential scanning calorimetry (DSC) which revealed that these compounds may exhibit mesomorphic properties. The DSC results of aromatic amines and ferrocenyl Schiff bases were compared to study the effects of structure, i.e. rigid core and terminal chain length, on the phase transition behaviour.     

Research on synthesis and conductivity of ferrocenyl Schiff base and its salt

Ferrocenyl Schiff base was synthesized through the condensation of ferrocenecarboxaldehyde and p‐phenylenediamine under neutral conditions, and then a new interesting category of organometallic charge transfer complex was obtained by the doping of ferrocenyl Schiff base with Fe³⁺, Al³⁺ and Ti³⁺ salts. The effects of the dosage of doping agent and doping temperature on the room‐temperature electric conductivity of samples were discussed; in addition, the temperature dependence of the electric conductivity of samples was studied, their structures and compositions were characterized by ¹H‐NMR spectra, infrared spectra, ultraviolet spectra and an electron probe X‐ray microanalyser. The results showed that the electric conductivity of sample can increase 4–5 orders of magnitude after doping with a metallic salt, and the electric conductivity has a positive temperature coefficient effect. The electrical activation energies of the complexes in the range 0.09–1.54 eV were calculated from Arrhenius plots, indicating their favourable semiconducting behaviour. Copyright © 2006 John Wiley & Sons, Ltd.     

Biaryl-bridged Schiff base complexes of zirconium alkyls: synthesis structure and stability

Three substituted salicylaldimine derivatives H₂L^1-3 of 2,2′-diamino-6,6′-dimethylbiphenyl give, under appropriate conditions, isolable alkyls of zirconium [ZrL^1-3R₂] (R=CH₂Ph, CH₂Bu^t). Two molecular structures confirm their cis-α geometry (C₂-symmetric with cis alkyl ligands). They decompose via 1,2-migratory insertion of an alkyl group to imine, followed in some instances by a second similar reaction. The dimeric molecular structure of one such doubly-inserted product is presented. The kinetics of decomposition by this process are studied briefly, and it is noted that the rate increases with increased steric demand of the salicylaldimine unit.     

双水杨醛缩环己二胺类西佛碱及其配合物的合成、性质研究

合成了两种双水杨醛缩环已二胺类西佛碱N，N’-(二羟苯次甲基)环已二胺(1)和N，N’-二(3，5-二叔丁基-2-羟苯次甲基)环已二胺(2)，以及它们的金属锌配合物(3)和(4)，通过核磁共振、元素分析和红外光谱确定了四种物质的结构，研究了它们的紫外吸收光谱、荧光光谱，测定了(3)和(4)的荧光量子效率．(4)中四个叔丁基的存在使其荧光量子效率提高．此类双西佛碱金属配合物可以应用于有机电致发光材料中．     

三氯化镓席夫碱配合物的合成与晶体结构

在无水无氧条件下,利用三氯化镓与水杨醛缩间氯苯胺反应合成了一种新的席夫碱配合物C13H10ClNO·GaCl3。利用元素分析、核磁共振、红外光谱和X射线衍射单晶结构分析对其进行了表征。单晶结构表明标题配合物晶体属于正交晶系,Pnma空间群,晶胞参数:a=17.873(3),b=7.0853(13),c=12.677(2),α=90,β=90,γ=90,V=1605.4(5)3,Z=4,F(000)=808,R1=0.0283,wR2=0.0649。该配合物中镓以四配位形式存在,形成畸变的四面体结构,配合物依靠分子间的氢键作用进一步联结成二维网状结构。     

A simple and clean procedure for the synthesis of polyhydroacridine and quinoline derivatives: reaction of Schiff base with 1,3-dicarbonyl compounds in aqueous medium

A clean and simple synthesis of benzo[c]acridine, benzo[a]acridine, pyrido[2,3-c]acridine and benzo[f]quinoline derivatives was accomplished in good to excellent yields via the reaction of Schiff base with 1,3-dicarbonyl compounds in aqueous medium catalyzed by TEBA. The structures were characterized by ¹H NMR, IR and elemental analysis, and confirmed by X-ray diffraction study.     

The use of hydrogenated Schiff base ligands in the synthesis of multi-metallic compounds II

Tris(2-hydroxybenzylaminoethyl)amine (H₃L) complexes of nickel, copper and zinc are investigated as potential metallo-ligands ([(H_xL)M]; x = 0, 1: M = Ni, Cu, Zn). The homometallic complexes formed are dimetallic ([{(HL)Ni}Ni(OAc)₂] and [{(L)Zn}ZnCl]), tetrametallic ([{(L)Cu}Cu]₂²⁺) and hexametallic ([{(L)Ni}Ni₂(μ-OH)₂(OEt)(OH₂)]₂). Hetero-dimetallic complexes can be formed with [(HL)Ni] and copper chloride ([{(HL)Ni}CuCl₂]) or zinc bromide ([{(HL)Ni}ZnBr₂]). The metallo-ligand acts as a chelating agent using phenolate pairs. The remaining phenolate either does not coordinate or can be used to increase the number of metals included in the scaffold from two to four or six. Not all combinations are possible and [(HL)Cu]⁺ produces a charge separated species with zinc chloride rather than a complex. An exchange reaction is observed to take place when [(HL)Zn]⁺ is treated with the halides of nickel or copper producing [(HL)M]⁺ (M = Ni, Cu, respectively).     

Design,synthesis, and antilung adenocarcinoma activity research of novel paeonol Schiff base derivatives containing a 1,2,3-triazole moiety

A new series of paeonol Schiff base derivatives containing a 1,2,3-triazole moiety were synthesized using the copper(I) catalyzed azide-alkynecycloaddition (CuAAC) reaction and evaluated for their cytotoxicity in vitro against human cervical carcinoma HeLa cells, human lung cancer A549 cells, and human liver cancer HepG2 cells. Unfortunately, all the tested compounds showed poor activities toward the human cervical carcinoma HeLa cells and human liver cancer HepG2 cells. However, compounds (E)-2-(1-(((1-[2-fluorophenyl]-1H-1,2,3-triazol-4-yl)methyl)imino)ethyl)-5-methoxyphenol ( 4c ) and (E)-2-(1-(((1-[3- chlorophenyl]-1H-1,2,3-triazol-4-yl)methyl)imino)ethyl)-5-methoxyphenol ( 4i ) exhibited inhibitory activities toward human lung cancer A549 cells (IC₅₀ = 45.1 μM for 4c and 78.9 μM for 4i ) compared with that of paeonol, which indicated that such paeonol Schiff base derivatives containing a 1,2,3-triazole moiety could be further modified to obtain good cytotoxicity in vitro against human lung cancer A549 cells.     

Synthesis,characterization and in vitro antimicrobial activity of some novel 5-substituted Schiff and Mannich base of isatin derivatives

With the aim of developing potential antimicrobials, a series of novel Ciprofloxacin methylene isatin derivatives incorporating different aromatic aldehydes were synthesized and characterized by FTIR, ¹H NMR, Mass spectroscopy and bases of elemental analysis. In addition, the in vitro antibacterial and antifungal properties were tested against some human pathogenic microorganisms by employing the disc diffusion technique. A majority of compounds were showing activity against several of the microorganisms. The relationship between the functional group variation and the biological activity of the evaluated compounds is discussed. From comparisons of the compounds, 3c was determined to be the most active compound.     

Synthesis and characterization studies of 3-formyl chromone Schiff base complexes and their application as antitumor,antioxidant and antimicrobial

A novel Schiff base namely (E)-3-((2,6-dihydroxypyrimidin-4-ylimino)methyl)-4H-chromen-4-one and its Co (II), N (II)i, Cu (II) and Cd (II) complexes have been synthesized and proved by elemental analysis, molar conductance, thermal analysis (TGA), Inductive Coupled plasma (ICP), magnetic moment measurements, X-ray powder diffraction, IR, EI-mass,¹H NMR, ¹³C NMR,UV–Vis. and ESR spectral studies. On the basis of these data, it is evident that the Schiff base acts as bidentate via oxygen atom of carbonyl group and azomethine nitrogen atom for Co (II) complex; monobasic bidentate ligand for Ni (II), Cu (II) and Cd (II) complexes via oxygen atom of hydroxyl group and nitrogen atom of pyrimidine ring. The results showed all complexes have octahedral geometry. The average particle size of the ligand and its complexes were found to be 1.010–0.343 nm. The pharmacological action (antioxidant, antimicrobial and anticancer) of the prepared compounds is studied. The antitumor activity of the ligand and its metal complexes is evaluated against human liver carcinoma (HEPG2) cell. The data displayed the Co (II) complexes strong cytotoxicity where IC₅₀ values of Co (II) complex and 5-fluorouracil (stander drug) are 9.33 and 7.86 μg/ml respectively. The Co (II) and Cd (II) complexes have antibacterial activity more than ampicillin (stander drug). The interaction of the synthesized compounds with calf-thymus DNA (CT-DNA) has been performed via absorption spectra and viscosity technique. The DNA- binding constants have been determined.