1-脱氢松香酰基-3-取代硫脲以及5-(脱羧脱氢松香-4-基)-3-芳氨基- 1H-1,2,4-三唑化合物的合成与生物活性

以广西的优势资源松香为原料, 脱氢松香酸与亚硫酰氯、硫氰化钾分别在回流条件下反应6 h和1.5 h, 得到脱氢松香酰异硫氰酸酯, 产率52%; 然后与胺在加热回流条件下反应1.5 h, 得到11种1-脱氢松香酰基-3-取代硫脲4, 产率63%～94%; 4a～4f 分别与水合肼在搅拌下回流反应3～6 h, 得到6种5-(脱羧脱氢松香-4-基)-3-芳氨基-1H-1,2,4-三唑化合物5, 产率70%～94%; 所有化合物的结构均经IR, 1H NMR, 13C NMR和元素分析确认. 初步生物活性测试表明, 4e, 4f, 4j, 5b对枯草杆菌抑菌率较高, 特别是4j在浓度为50 mg/L时就达到较好效果; 4b, 4h, 4i, 5e在100 mg/L时对大肠杆菌的抑菌效果较好.     

两类脱氢松香胺Schiff碱类衍生物的合成及其离子识别性能

以脱氢松香胺和降解脱氢松香胺为起始反应物,通过与一系列醛缩合,得到两个系列的脱氢松香胺Schiff碱类衍生物2a～2f和4a～4e.其结构用1H NMR,3C NMR,MS,IR和元素分析等分析手段进行了确证.随后对所合成的脱氢松香胺Schiff碱类衍生物进行了阴、阳离子的识别能力研究,并对其结构与离子识别能力的关系进行了探讨.     

二氯化-N,N-′-二(3-脱氢松香酰氧-2-羟丙基)四甲基乙二胺的合成与性能

研究了Gemini表面活性剂中疏水"尾巴"结构对性质的影响,以脱氢松香酸和环氧氯丙烷为原料合成了中间体3-脱氢松香酰氧-2-羟丙基氯,再与四甲基乙二胺反应,得到1种以脱氢松香酰基为疏水链"尾巴"的对称Gemini型双季铵盐阳离子表面活性剂:二氯化-N,N′-二(3-脱氢松香酰氧-2-羟丙基)四甲基乙二胺。在合成工艺条件的基础上,采用IR光谱、MS谱和元素分析测试技术对产物进行了结构确认。结果表明,该产物可降低水的表面张力达34.9 mN/m,临界胶束浓度为1.0×10-4mol/L。表明具有良好疏水性能的2个大"尾巴"使合成的Gemini表面活性剂更易形成胶束,大大提高了表面活性。     

二氯化-N,N-'-二(3-脱氢松香酰氧-2-羟丙基)四甲基乙二胺的合成与性能

研究了Gemini表面活性剂中疏水"尾巴"结构对性质的影响,以脱氢松香酸和环氧氯丙烷为原料合成了中间体3-脱氢松香酰氧-2-羟丙基氯,再与四甲基乙二胺反应,得到1种以脱氢松香酰基为疏水链"尾巴"的对称Gemini型双季铵盐阳离子表面活性剂二氯化-N,N'-二(3-脱氢松香酰氧-2-羟丙基)四甲基乙二胺.在合成工艺条件的基础上,采用IR光谱、MS谱和元素分析测试技术对产物进行了结构确认.结果表明,该产物可降低水的表面张力达34.9 mN/m,临界胶束浓度为1.0×10-4 mol/L.表明具有良好疏水性能的2个大"尾巴"使合成的Gemini表面活性剂更易形成胶束,大大提高了表面活性.     

几种含有酰胺基团超滤膜吸水情况的FTIR,TGA和DSC研究

对几种超滤膜的TGA、DSC及FTIR研究表明,室温下含酰胺基的干燥膜体仍以氢键的形式结合一定数量的单分子水,同时也含有微量的二聚水和多聚水。当温度上升到40℃左右,水与膜体形成的氢键几乎完全断裂。每个酰胺基吸附水量的顺序为:聚砜酰胺>聚苯并咪唑酮>芳香聚酰胺;每种膜吸附水的绝对量顺序为芳香聚酰胺>聚砜酰胺>聚苯并咪唑酮。     

1-(5-苄基四唑-2-乙酰基)-4-芳酰胺基硫脲及其环化产物的合成

本文合成了一系列新的1-(5-苄基四唑-2-乙酰基)-4-芳酰胺基硫脲(2)。2在8%NaOH溶液作用下, 环化为3-(5-苄基四唑-2-亚甲基)-4-芳酰基-1,2,4-三唑啉-5-硫酮(3)。     

1-芳酰基-4-(5-芳基-2-呋喃甲酰基)氨基硫脲衍生物的合成及其生物活性

酰胺基硫脲;芳基酰肼;1-芳酰基-4-(5-芳基-2-呋喃甲酰基)氨基硫脲衍生物的合成及其生物活性     

脱氢枞酸及其衍生物生物活性的研究进展

脱氢枞酸是一种从松香中分离出来的具有三环二萜结构的树脂酸,具有广泛的生物活性,在医药、工业、农业等领域具有重要的用途。本文综述了脱氢枞酸衍生物在抑菌、抗病毒、K离子通道开启、抗肿瘤等生物活性方面的研究进展,展望了脱氢枞酸衍生物的研究和应用前景。     

脱氢松香酸β-萘酚酯的合成

松香是自然界极其丰富的一种天然树脂,利用松香等可再生天然资源代替石油发展精细化工已成为日益重要的研究课题[1]。但原料松香存在性能差,使用率低等缺点,因此对松香进行改性,使松香的化学利用由直接利用松香的初级产品向深度利用松香衍生物的方向发展已经成为松香利用的趋势[2]。脱氢松香酸(也叫去氢枞酸、去氢松香酸)主要由松香通过催化歧化后得到,具有芳香型三环二萜结构。它具有性质稳定,抗氧化能力强,比旋光度较大等一些其它的松香衍生物所不具备的独特的理化性质。因此脱氢松香酸具有极大的开发价值。本文以脱氢松香酸和β-萘酚为原…     

1-(5-苄基四唑-2-乙酰基)-4-芳酰胺基硫脲及其环化产物的合成

据报道,酰胺基硫脲及其相应环化产物具有广泛的生理活性。如可消炎止痛,镇静,降血压,抗细菌和调节植物生长等。我们曾经通过α-苯基氰乙酰肼与芳酰基异硫氰酸酯缩合制备出一些新的酰胺基硫脲和相应的杂环衍生物,观察到它们在很低浓度下具有调节小麦芽鞘生长的活性。以前的一些研究结果得知,许多5-芳基四唑-2-烷基酸和它们的酰     

Furyl- and thienyl-silatranes and germatranes

We review our research on the synthesis and study of the physical and biological properties of furyl- and thienylgermatranes and -silatranes.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 6, pp. 725–732, June, 1992.     

Review and patents and literature

The use of the insect cell/baculovirus expression system for producing recombinant proteins of bacterial, plant, insect, and mammalian origin has become widespread. The popularity of this eukaryotic expression system is due to many factors, including (1) potentially high protein expression levels, (2) ease and speed of genetic engineering, (3) ability to accommodate large DNA inserts, (4) protein processing similar to higher eukaryotic cells (e.g., mammalian cells), and (5) ease of insect cell growth (e.g., suspension growth). The following review of the literature discusses two engineering aspects of recombinant protein synthesis by insect cell cultures: bioreactor scale-up and insect cell line selection. Following this review patent abstracts and additional literature pertaining to expression of recombinant proteins in insect cell culture are listed.     

Ground- and excited-state aromaticity and antiaromaticity in benzene and cyclobutadiene

The aromaticity and antiaromaticity of the ground state (S 0), lowest triplet state (T 1), and first singlet excited state (S 1) of benzene, and the ground states (S 0), lowest triplet states (T 1), and the first and second singlet excited states (S 1 and S 2) of square and rectangular cyclobutadiene are assessed using various magnetic criteria including nucleus-independent chemical shifts (NICS), proton shieldings, and magnetic susceptibilities calculated using complete-active-space self-consistent field (CASSCF) wave functions constructed from gauge-including atomic orbitals (GIAOs). These magnetic criteria strongly suggest that, in contrast to the well-known aromaticity of the S 0 state of benzene, the T 1 and S 1 states of this molecule are antiaromatic. In square cyclobutadiene, which is shown to be considerably more antiaromatic than rectangular cyclobutadiene, the magnetic properties of the T 1 and S 1 states allow these to be classified as aromatic. According to the computed magnetic criteria, the T 1 state of rectangular cyclobutadiene is still aromatic, but the S 1 state is antiaromatic, just as the S 2 state of square cyclobutadiene; the S 2 state of rectangular cyclobutadiene is nonaromatic. The results demonstrate that the well-known "triplet aromaticity" of cyclic conjugated hydrocarbons represents a particular case of a broader concept of excited-state aromaticity and antiaromaticity. It is shown that while electronic excitation may lead to increased nuclear shieldings in certain low-lying electronic states, in general its main effect can be expected to be nuclear deshielding, which can be substantial for heavier nuclei.     

Hard and soft acids and bases: structure and process

Under investigation is the structure and process that gives rise to hard-soft behavior in simple anionic atomic bases. That for simple atomic bases the chemical hardness is expected to be the only extrinsic component of acid-base strength, has been substantiated in the current study. A thermochemically based operational scale of chemical hardness was used to identify the structure within anionic atomic bases that is responsible for chemical hardness. The base's responding electrons have been identified as the structure, and the relaxation that occurs during charge transfer has been identified as the process giving rise to hard-soft behavior. This is in contrast the commonly accepted explanations that attribute hard-soft behavior to varying degrees of electrostatic and covalent contributions to the acid-base interaction. The ability of the atomic ion's responding electrons to cause hard-soft behavior has been assessed by examining the correlation of the estimated relaxation energies of the responding electrons with the operational chemical hardness. It has been demonstrated that the responding electrons are able to give rise to hard-soft behavior in simple anionic bases.     

Determination and study on residue and dissipation of benazolin-ethyl and quizalofop-p-ethyl in rape and soil

A QuEChERS (quick, easy, cheap, effective, rugged, and safe) method for the determination of benazolin-ethyl and quizalofop-p-ethyl in rape and soil by high-performance liquid chromatography-tandem mass spectrometry has been developed in this study. The residue and dissipation of benazolin-ethyl and quizalofop-p-ethyl in rape and soil were determined with the developed method. The half-lives of benazolin-ethyl in rape straw and soil were 3.7–5.1 days and 14.3–26.3 days, respectively. The half-lives of quizalofop-p-ethyl in rape straw and soil were 5.0-6.1 days and 0.3–9.7 days, respectively. The residue of benazolin-ethyl and quizalofop-p-ethyl in rapeseed and soil were below the detection limit (i.e., 0.5?mg?kg^?1, the maximum residue level of European Union for quizalofop-p-ethyl).     

Syntheses and structures of P-anilino-P-chalcogeno- and P-anilino-P-iminodiazasilaphosphetidines and their group 12 and 13 metal compounds

The P-anilino-P-chalcogeno(imino)diazasilaphosphetidines [Me(2)Si(mu-N(t)Bu)(2)P=E(NHPh)] (E = O (3), S (4), Se (5), N-p-tolyl (6)) were synthesized by oxidizing the P-anilinodiazasilaphosphetidine [Me(2)Si(N(t)Bu)(2)P(NHPh)] (2) with cumene hydroperoxide, sulfur, selenium, and p-tolyl azide, respectively. The lithium salt of 4 reacted with thallium monochloride to produce ([Me(2)Si(mu-N(t)Bu)(2)P=S(NPh)-kappaN-kappaS]Tl)(7), which features a two-coordinate thallium atom. Treatment of 4-6 with AlMe(3) gave the monoligand dimethylaluminum complexes ([Me(2)Si(mu-N(t)Bu)(2)P=E(NPh)-kappaN-kappaE]AlMe(2)) (E = S (8), Se (9), N-p-tolyl (10)), respectively. In these complexes the aluminum atom is tetrahedrally coordinated by one chelating ligand and two methyl groups, as a single-crystal X-ray analysis of 8 showed. A 2 equiv amount of 4-6 reacted with diethylzinc to produce the homoleptic diligand complexes ([Me(2)Si(mu-N(t)Bu)(2)P=E(NPh)-kappaN-kappaE](2)Zn)(E = S (11), Se (12), N-p-tolyl (13)). A crystal-structure analysis of 11 revealed a linear tetraspirocycle with a tetrahedrally coordinated, central zinc atom.