肼类衍生物在五元唑类杂环合成中的应用进展

简要概述了肼类衍生物的结构及反应活性,总结了近十年来肼类衍生物分别在合成五元唑类杂环如吡唑、噻唑、1,3,4-噁二唑、1,3,4-噻二唑以及三唑类化合物,及其相关的稠杂环如吡唑并某环、s-三唑[3,4-b][1,3,4]-噻二唑、s-三唑[3,4-b][1,3,4]-噻二嗪,以及含有1,2,4-三唑的稠杂环化合物等合成中的应用进展.     

Functional tetrahydroquinoxalines from perfluoroaromatic precursors

A short series of bromo- and nitro-polyfluorobenzene derivatives gave the corresponding tetrahydroquinoxaline systems upon reaction with N,N′-dimethylethylene diamine. This annelation strategy gives useful quantities of functionalised tetrahydroquinoxaline systems which may be interesting scaffolds for the drug discovery arena.     

Stereoselective hetero Diels-Alder reaction of selenoaldehydes with pentavalent phosphole chalcogenides

Stereoselective hetero Diels-Alder reaction of selenoaldehydes, generated by thermal retro Diels-Alder reaction of anthracene cycloadducts, with pentavalent 3,4-dimethylphosphole chalcogenides at 110 °C in toluene to give the corresponding [4+2] cycloadducts as a single diastereoisomer in good yields, accompanied by a slight scrambling of chalcogen atoms. Higher reaction temperature led to an increase of the scrambling between chalcogen atoms.     

聚合物支持合成稠杂环化合物的研究进展

综述了近几年稠杂环化合物的固相和液相合成研究进展.     

Synthesis, crystal structures and spectroscopic characterization of two neutral heterobimetallic clusters MS4Cu4(pz)6X2 (where M = Mo (1) or W (2), X = Cl (1) or disordered Cl/Br (2), and pz = 3,5-dimethylpyrazole)

The title complexes were synthesized in acetone by the reaction of [n-Bu₄N]₂[MoS₄Cu₄Cl₄] and pz^Me2 for compound 1, and n-Bu₄NBr, [NH₄]₂[WS₄], CuCl and pz^Me2 for compound 2. X-ray diffraction studies of 1 and 2 demonstrate that four of the six edges of the tetrahedral [MS₄]²⁻ core are bridged by four copper atoms, giving a pentanuclear structure MS₄Cu₄(pz^Me2)₆X₂ (M = Mo, W) with the five metal atoms essentially coplanar. The four Cu atoms exhibit two different coordination modes. Each of one pair of mutually trans Cu atoms is coordinated by two (μ₃-S) atoms and two nitrogen atoms of pz^Me2 rings, giving a distorted tetrahedral CuS₂N₂ arrangement. The other two mutually trans Cu atoms are coordinated by two (μ₃-S) atoms, one nitrogen atom of pz^Me2 and one terminal Cl or Br ligand, giving a distorted tetrahedral CuS₂NX unit. In addition to being structurally studied by X-ray diffraction, the title compounds have been characterized by IR, UV–Vis and ¹H NMR spectroscopy. The IR results, which include low-frequency M–S_b stretching bands, are consistent with the X-ray structural analysis and confirm that the [MS₄]²⁻ cores are coordinated through all four sulfur atoms in the complexes 1 and 2.     

π-facial interactions between Cl and [S4N3]. X-ray crystal structure of [S4N3]Cl

The X-ray structure of [S₄N₃]Cl reveals three independent molecules, which all display π-facial interactions between the Cl⁻ and the pseudo-aromatic [S₄N₃]⁺ rings to produce a structure containing “inverse sandwich” systems.     

Synthesis of 4-(4-Methylsulfonylphenyl)-3-phenyl-2(3H)-thiazole Thione Derivatives as New Potential COX-2 Inhibitors

Synthesis of novel 4-（4-methylsulfonylphenyl）-3-phenyl-2（3H）-thiazole thione derivatives with functionalized diarylheterocycle pharmacophore as potential COX-2 inhibitors was described. The title compounds were synthesized by cyclocondensation of corresponding dithiocarbamate and 2-bromo-1-（4-methylsulfonylphenyl）ethanone, followed by dehydration with H2SO4. All of the target compounds were characterized by ^1H NMR, IR and mass spectral data.     

Die Reaktion des [(Me3Si)2CH]2Al?CH2?Al [CH(SiMe3)2]2 mit LiCH(PMe2)2; Bildung eines fünfgliedrigen Al2C2P-Heterozyklus

The Reaction of [(Me₃Si)₂CH]₂Al? CH₂? Al [CH(SiMe₃)₂]₂ with LiCH(PMe₂)₂; Formation of a Five-membered Al₂C₂P Heterocycle The recently synthesized methylene bridged dialuminium compound [(Me₃Si)₂CH]₂Al? CH₂? Al [CH(SiMe₃)₂]₂ 3 reacts with one equivalent of LiCH(PMe₂)₂ in the presence of TMEDA to give an adduct with one aluminium atom coordinated by the carbanionic carbon atom and the second one coordinated by one phosphorus atom. A five-membered heterocycle 5 is formed, which was characterized by a crystal structure determination showing a strongly bent ring with the phosphorus atom located above the plane of the four remaining atoms (Al₂C₂). 5 is unstable in ethereal solution decomposing under ether cleavage to the educt 3 and the diphosphinomethane derivative CH₂(PMe₂)₂.     

含芳香稠环或杂环的光致变色螺吡喃化合物的光谱性能及与DNA作用研究

研究9种带有芳香稠环或杂环基团的光致变色螺吡喃化合物的光致变色性能和荧光性质.通过紫外-可见吸收光谱和荧光光谱对该类化合物与DNA相互作用性能进行了初步探讨.     

过渡金属催化异腈参与的多组分反应研究进展

综述介绍了近5年来过渡金属催化下异腈参与的多组分反应的研究进展.