多取代环丙烷化合物的合成研究

具有环丙烷结构的化合物是一种重要的生物代谢中间体,广泛存在于许多植物霉菌和细菌等微生物体内。三元环是一种具有很好生物活性的结构单元。三元环的反应活性不仅因为它具有类似于链状双键的化学性质,同时还具有易重排的特点,例如,由三元碳环到四元碳环、五元碳环和七元碳环的扩环反应及四元碳环到三元碳环的环收缩反应,据文献报道,给体－受体同碳取代的三元环和多取代的三元环也是一种重要的合成单元。     

5-(2’-羧乙基)-6-烷基-3,4-二氢吡喃酮的合成

吡喃酮是许多天然产物的结构单元,我们曾由4-异丁酰基庚二酸在过量醋酸酐及乙酰氯存在下回流得到7-氧代-8,8-二甲基-△~9-六氢香豆素.本文由二氰乙基-β-二酮进行酮解水解反应得到4-酰基庚二酸1_(a-c)。 在过量醋酸酐、乙酰氯存在下由1_a、1_c为底物进行反应没有得到双环的香豆素衍生物.其产物和单纯以乙酐为缩合剂时的产物2_a、2_c相同,产率分别为68％、63％。2_c可在硫酸铁催化     

二种氧氮杂环戊二烯类化合物的合成及其光性能研究

本文合成了对-(2-苯基-1,3,4,-噁二唑基-5)-(5’-苯基噁唑基-2’)苯和对-(2-苯基-1,3,4-噁二唑基-5)-(2’-苯基q罨唑基-5’)苯二类共12种化合物,测试了它们的紫外、荧光、红外光谱和激光转换效率.     

异核苷低聚核苷酸的合成及其酶促稳定性

用磷酸三酯法在溶液中合成了两个带有３′－（Ｓ）－胸腺嘧啶基－４′－（Ｒ）－羟基－５′－（Ｓ）－羟甲基四氢呋喃的三脱氧核苷酸３和４。与三脱氧核苷酸（２）相比，化合物３和４对核酸酶Ｓ１具有更大的稳定性。     

3,4,5-三甲氧基苯甲酰腙类化合物的合成与表征

以没食子酸为原料。经烷基化、肼解得3,4,5-三甲氧基苯甲酰肼(2),2与芳香醛进行缩合反应合成了9个新的酰腙化合物。其结构经元素分析。IR,1H NMR和MS表征。     

Synthesis of some heteroaryl pyrazole derivatives and their biological activities

In order to search for novel fungicides with high activity, a series of heteroaryl pyrazoles were synthesized from 5-pyra-zole formhydrazide. The structures of all new compounds were confirmed by spectroscopic methods and microanalyses. Preliminary bioassays indicated that some compounds showed fungicidal activity against Puccinia tritinia and PGR activity as well.     

Pig Liver Esterase-catalyzed Hydrolysis of Three Diesters of meso-Bicyclic Dicarboxylic Acid and Three Tetraesters of Tetrahydrofuran-2, 3,4,5-tetracarboxylic Acid

IntroductionPig liver esterase(PLE) is one of the most useful enzymes for the enantioselective hydrolysis of ester groups, which has been demonstrated by numerous examples. The enantioselectivity of PLE towards the hydrolysis of one of the diesters with prochiral centers or meso-diesters has been the subject of extensive investigations['--']. The hydrolysis of the dimethyl esters of some symmetrical dicarboxylic acids in the presence of PLE gave encouraging results[5-7].In order to prepare…     

2-(3’,5’-二硝基苯)-4-硝基-1,2,3-三唑-1-氧化物的合成与量子化学研究

以乙二醛、苯肼和盐酸羟胺为起始原料,经缩合和肟化反应制得肟基苯腙(1)。在硫酸铜-吡啶-水体系中,1经缩合环化得2-苯基-1,2,3-三唑-1-氧化物(2);2被混酸硝化合成了新化合物2-(3’,5’-二硝基苯)-4-硝基-1,2,3-三唑-1-氧化物(3),纯度99%,总收率45%,其结构经1H NMR,IR,MS和元素分析表征。在B3LYP/aug-cc-pVDZ基组水平上对3的结构进行了优化,获得稳定的几何构型。     

3,4,5-三苄氧基苯甲酰腙类化合物的合成及生物活性研究

以没食子酸为起始原料,设计合成了10个新的3,4,5-三苄氧基苯甲酰腙类化合物4a~4j,其结构经元素分析、1HNMR和MS表征。初步的生物活性测试结果表明,所合成的化合物均表现出不同程度的抑菌活性,其中,4f的活性最好,在50 mg.L-1浓度下对水稻纹枯病菌和小麦赤霉病菌的抑制率达90%以上。     

Synthesis, Crystal Structure and Property of a Series of Supramolecular Polymers Based on Novel 3,5-Dimethyl- 2,6-bis（3-（pyrid-2-yl）-1,2,4-triazolyl）pyridine Ligand

Solvothermal reactions of 3,5-dimethyl-2,6-bis(3-(pyrid-2-yl)-1,2,4-triazolyl) pyridine (L), 1,4-benzendicarboxylic acid (H2bdc), and transitional metal cations of MII (M = Mn, Co, Cd) in the presence of oxalic acid (H2ox) afford three novel supramolecular polymers (CPs), namely, {[M2(ox)(L)2][bdc][M2(Hox)2(OH)2(H2O)4].3H2O}n (M=Mn for 1, Co for 2, Cd for 3). Single-crystal X-ray diffraction analysis reveals that complexes 1-3 are isostructural and the 3D supramolecular structure was connected through non-covalent interactions. With the help of H2ox, the L ligands cheated with center atoms forming a butterfly [M2(ox)(L)2]2+ building block. The bdc2- ligand linked with the unprecedented [M2(Hox)2(OH)2(H2O)4] units through strong O-H…O hydrogen bonds forming a zigzag chain, which are further connected through π…π interactions between L and bdc2- ligands to form a 3D supramolecular structure. Moreover, elemental analyses, IR, thermogravimetric, PXRD and luminescence have been investigated.     

X-ray Structure of 1- (3' -Phenyl-4' -morpholinyl-2' 5' - dithiole-1' - ylidene)-3, 4-biscarboethoxy-2-thionaphthalene

1INTR0DUCTIONa-Thiocarbonylthioformamideshavebeensynthesizedsince1980[l-23,however,thereisn0reP0rtofthesecomP0undsrelatedtheirpropertiesandreactivities(3).Ac-cordingtothepublishedpapers('-",adithioketone,adithioesterandadithioth-ioesteraresnitablefort4 2JcycloadditionwithalkenicandacetylenicdienophileS.Wewanttoknowwhethera-thiocarbonylthioformamideshavethesamecharacters,thereforethereactionofathiobenzoylthioformmorpholine(1)withdiethylacetylenedicarboxylate(2)wasexplored.Theredultsshowth…     

Synthesis of affinity column of phosphatidylinositol-3,4-diphosphate

Phosphatidylinositol polyphosphates (PIPx) are related with tyrosine kinase activation, cell proliferation and carcinogenesis. In order to investigate the action mechanism of PIPx, it is desirable to synthesize affinity column of PI-3,4-P2, which is expected to be able to isolate the binding proteins of PI-3,4-P2. Thyramine reacted with CH-Sepharose 4B giving column 13. The p-amino group of 3'-(1',2'-distearoyl-glyceryl)-1-(2-p-aminobenzyl)-3,4-di-O-phosphoryl-myo-inosityl phosphate (12) was diazotized, then diazo-coupled with column 13 to give PI-3,4-P2 affinity column 14. This PI-3,4-P2 affinity column is an effective tool to pick up binding proteins of PI-3,4-P2.     

Synthesis and Crystal Structure of One Mixed- ligand Coordination Polymer Based on the Novel Terphenyl-2,5,2',5'-tetracarboxylic Acid Ligand

Solvothermal reaction of aromatic terphenyl-2,5,2',5'-tetracarboxylic acid (H 4 qptc) ligand and the transitional metal cation of Mn II in the presence of 3-(2-pyridyl)pyrazole (pp) affords one new coordination polymer, [Mn(qptc)0.5(pp)2]n·n(H2O) (1). The structure has been determined by single-crystal X-ray diffraction analyses and further characterized by elemental analyses, IR, TGA, and magnetism. The carboxyl groups of qptc 4-exhibit a μ1-η1 :η 0 coordination mode, and the qptc4- acts as a H-shaped ligand linking the Mn Ⅱ centers together to form a 2D polymeric [Mn(qptc) 0.5 ] n layer. The crystal of 1 crystallizes in orthorhombic, space group Pbca with a=9.3119(12), b=20.848(3), c=26.134(3) , V=5073.4(11) 3 , Z=8, C27H19MnN6O5 , Mr=562.42, Dc=1.473 g/cm3 , F(000)=2304 and μ(MoKα)=0.571 mm-1 . The final R=0.0468 and wR=0.1196 for 4429 observed reflections with I > 2σ(I) and R=0.0797 and wR=0.1383 for all data.     

Synthesis of Pyrazolo[3,4-b]- and Pyrido[2,3-b]-1,5-benzodiazepines

Abstract

3-Dimethylaminomethyleno-4-phenyl-1H-1,5-benzodiazepin-2-one (1) was synthesized and reacted with hydrazines, active nitriles, and amino-heterocyclic compounds to give fused heterocyclic compounds 2–14.     

CPHPUN 的合成及其在分析化学中的应用

阐述了Ｎ－１－（３－３－二羧基－４,４’－联苯撑）－（３－Ｎ－苯基三氮）,（Ｎ－１,１‘－３（３,３’－ｄｉｃａｒｂｏｘｙ１－４,４－ｄｉｐｈｅｎｙｌ）－ｈｉｓ－（３－Ｎ－ｈｙｄｒｏｘｙ－３－Ｎ－ｐｈｅｎｙｌ－ａｚｉｄｅ的合成方法。结构论证、分析性能及在光度分析中的。ＣＰＨＰＵＮ对外一有很高的显色灵敏度和很好的识别能力。在光度分析中,ε４６７．５达２．３５×１０＾６Ｌ·ｍｏｌ＾－１·ｃｍ＾－１。用     

2-Polyfluoroalkylchromones. 14. Synthesis of 4-chloro-3(5)-(2-hydroxyaryl)-5(3)-polyfluoroalkylpyrazoles

3-Chloro-2-polyfluoroalkyl- and 3-chloro-6-nitro-2-polyfluoroalkylchromones were synthesized. These compounds react with N₂H₄·2HCl on boiling in ethanol to form 4-chloro-3(5)-(2-hydroxyaryl)-5(3)-polyfluoroalkylpyrazoles.     

光学活性化合物多羟基庚酸乙酯的合成

以不对称环氧化和双羟化反应为构筑手性碳的关键步骤, 首次合成了(＋)-(2R,3S,4S,5S)-6-甲基-4,5-环氧-2,3-二羟基-庚酸乙酯(5)和(－)-(2R,3S,4R,5S)-6-甲基-2,3,4,5-四羟基-庚酸乙酯(11). 找到一条适宜于该类化合物合成的简便有效且立体选择性好的合成路线. 初步生物活性测试表明, 化合物5, 11对HL60细胞具有抑制活性.     

Synthesis of Some 2-(3-Alkyl/aryl-5-trifluoromethylpyrazol-1-yl)-4-(coumarin-3-yl)thiazoles as Novel Antibacterial Agents

Abstract

Herein, we describe a one-pot synthesis of some novel 2-(3-alkyl/aryl-5-trifluoromethylpyrazol-1-yl)-4-(coumarin-3-yl)thiazoles (6) involving the reaction of 3-alkyl/aryl-5-hydroxy-5-trifluoromethyl-4,5-dihydropyrazole-1-thiocarboxamides (3) with 3-bromoacetylcoumarins (5) in the presence of sodium carbonate in ethanol. Reaction of 3 with 5 in the absence of sodium carbonate, however, resulted in the formation of 2-(3-alkyl/aryl-5-hydroxy-5-trifluoromethyl-4,5-dihydropyrazol-1-yl)-4-(coumarin-3-yl)thiazoles, which were subsequently dehydrated to 6 by refluxing in ethanol in the presence of sodium carbonate. The structure of the synthesized compounds (6) was confirmed by infrared (IR), mass, ¹H NMR, and ¹³C NMR spectra and elemental analysis data. Newly synthesized compounds (6) showed moderate to good activity against Gram-positive bacteria.