3—吡唑基—6—取代均三唑并[3,4—6]—1,3,4—噻二唑的合成及生物活性

以１－甲基－３－乙基（４－氯）－５－哟唑甲作原料，经两步得到４－氨基－３－（１－甲基－３－乙基（４－氯）－５－吡唑基）－１，２，４－三唑－５－硫酮（３），３再与取代酸反应，得到一系列３（１－甲基－３－，乙基（－４－氯）－５－吡唑基）－６－取代均三并「３，４－ｂ」－１，３，４－噻二唑（４，５，６），元素分析、ＨＮＭＲ、ＩＲ和ＭＳ确定了它们的结构，初步生侧结果表明，３具有植物生长调节活性，４ｂ、４ｄ、     

Synthesis of 3,6-Disubstituted 5,6-Dihydro-s-triazolo [3,4-b]-1,3,4-thiadiazolidines through the Intramolecular Mannich Reaction

３－取代基－４－氨基－５－巯基－１，２，４－三唑在微量酸催化下与取代芳香醛经分子内Ｍａｎｎｉｃｈ反应合成了２９个新的３，６－二取代－５，６－二氢－ｓ－三唑并［３，４－ｂ］－１，３，４－噻二唑啉类化合物，其结构经元素分析、ＩＲ和１ＨＮＭＲ进行确证，并讨论了反应的立体选择性。     

稠杂环化合物的研究（XV）──6－取代－3－（1H－苯并三唑－1－亚甲基）－1，2，4－三唑并［3，4－b］－1，3，4－噻二唑的合成

研究了３－（１Ｈ－苯并三唑－１－亚甲基）－４－氨基－５－巯基－１，２，４－三唑与取代苯甲酸在三氯氧磷催化下的反应，制得１０种新的３－（１Ｈ－苯并三唑－１－亚甲基）－１，２，４．三唑并［３，４－ｂ］－１，３，４－噻二唑，通过元素分析、ＩＲ、￣１ＮＭＲ和ＭＳ确证了它们的结构并讨论了其波谱性质。     

2－氯／2－甲磺酰基－5－（2－苯基－4－喹啉基）－1，3，4－噁二唑化合物的合成及其亲核取代的研究

借处理２－羟基－５－（２－苯基－４－喹啉基）－１，３，二唑同ＰＣｌ＿５／ＰＯＣｌ＿３之间的反应合成了２－氯－５－（２－苯基－４－喹啉基）－１，３，４－二唑（３）和通过２－基－５－（２－苯基－４－喹啉基）－１，３，４－二唑的甲基化，然后氧化制得２－甲磺酰基－５－（２－苯基－４－喹啉基）－１，３，４－二唑（６）．并分别研究了３和６同胺、叠氮及肼的反应，得到２，５－二取代的二唑新衍生物．初步观察了部分化合物的抗菌活性．     

取代邻羟基二苯甲酮的合成1,3,5-三甲氧基苯与对位取代苯甲酰氯的Friedel-Crafts反应

控制反应物摩尔比、反应温度和反应时间，１，３，５－三甲氧基苯与对位取代苯甲酰氯发生Ｆｒｉｅｄｅｌ－Ｃｒａｆｔｓ反应，选择性地合成了２－羟基－４，６－二甲氧基－４－Ｒ－二苯甲酮和３－（４″－Ｒ－苯甲酰基）－２－羟基－４，６－二甲氧基－４－Ｒ－二苯甲酮。反应条件温和，产率较高。化合物的结构都经元素分析、１ＨＮＭＲ和ＩＲ确定。     

稠杂环化合物的研究（Ⅸ）──3－芳基－6－（2，4－二氯苯氧乙酰胺基）均三唑并［3，4－b］－1，3，4－噻二唑的合成

３－芳基－４－氨基－１，２，４－均三唑－５－硫酮和２．４－二氯苯氧乙酰异硫氰酸酯在丙酮中于６０℃回流，制得１０个新的均三唑并［３，４－ｂ］－１，３，４－噻二唑（３ａ－ｊ）化合物，用元素分析、ＩＲ、１ＨＮＭＲ和ＭＳ确证了结构，并讨论了反应机制。     

Synthesis and Crystal Structure of 3,3-Di(acetic ether)-2,4-pentanedione

合成和表征了３，３－二乙酸乙酯基－２，４－戊二酮。得出其为单斜晶系，空间群为Ｃ２／ｃ，ａ＝１４．８６４（２），ｂ＝１０．５６７４（７），ｃ＝９．５０５３（６），β＝１０１．８２５（６）°，υ＝１４６１．１３（２）３，Ｚ＝４，Ｄｘ＝１．２３８ｍｇ／ｍ３，μ＝０．０９８ｍｍ－１，ｆｉｎａｌＲ＝０．０３１４，Ｒｗ２＝０．０８９１     

1－（取代吡唑－4－基）－1，2，4－三唑的合成及生物活性研究

合成了２３个新的１－（取代吡唑－４－基）１，２，４－三唑化合物，经ＥＡ、ＩＲ、~１ＨＮＭＲ和ＭＳ确定其组成和结构，并对其进行了抑菌及生长调节活性的初步观察。     

经分子内Mannich反应合成3,6—二取代—5,6—二氢—s—三唑并（3,4—b）—1, …

３－取代基－４－氨基－５－巯基－１，２，４－三唑在微量酸催化下与取代芳香醛经分子内Ｍａｎｎｉｃｈ反应合成了２９个新的３，６－二取代－５，６－二氢－ｓ－三唑并（３，４－ｂ）－１，３，４－噻二唑啉类化合物，其结构经元素分析，ＩＲ和＾１ＨＮＭＲ进行确证，并讨论了反应的立体选择性。     

1—芳酰基—4—取代吡唑甲酰基氨基硫脲和环化产物的合成及生…

利用１－苯基－３－甲基－５－氯－４－吡唑甲酰基异硫氰酸酯（１）与芳酰肼（Ⅱ）的加成反应合成了系列新的酰胺基硫脲衍生物（Ⅱ）并将Ⅲ在酸性条件下进行环化反应得到２－取代吡唑甲酰基氨基５－芳基－１，３，４－噻二唑（Ⅳ）生物活性测定结果表明部分化合物Ⅲ和Ⅳ具有较好的除草活性。     

二氧化碳和丙烯直接合成甲基丙烯酸的NiPMo/TiO2催化剂的研究

用溶胶-凝胶法以磷钼酸(MPA)的镍盐溶液水解钛酸四丁酯制备了NiPMo/TiO2催化剂.使用ICP、 XRD、 TG-DTA、 IR、 TPD-MS和微反应技术研究了催化剂的化学组成、热稳定性、化学吸附性质和催化反应性能.杂多钼酸盐与TiO2通过O2-在TiO2表面发生了键合.在623 K下,杂多阴离子仍保持原有的Keggin结构.CO2在Lewis酸位Ni(Ⅱ)和Lewis碱位Ni-O-Mo的桥氧协同作用下生成CO2卧式吸附态Ni(Ⅱ)←O-(CO)←(O--Ni).丙烯有多种吸附态在催化剂上吸附.在563 K、 1 MPa和空速1500 h-1的反应条件下,丙烯的摩尔转化率为3.2%,产物MAA选择性为95%.     

Toward new camptothecins. Part 6: Synthesis of crucial ketones and their use in Friedländer reaction

In the context of the preparation of camptothecin and luotonin A analogs, the synthesis of some key keto-precursors and their use in Friedländer condensation are described. This paper also focuses on the stability of these keto intermediates and emphasizes the major differences between indolizinones and pyrroloquinazolinones series. Noteworthy is also the report of some original structures isolated as by-products of some experiments.     

CoFe2O4自形成磁性液体场致结构化对磁化的影响

The Langevin paramagnetic theory can’t describe the relation between magnetization of ferrofluids and applied magnetic field. The structuralization of ferrofluids, which is considered the main influence factor of the magnetization, is regarded. The part of magnetization works is deposited when the structure is forming. This action influences the magnetization of ferrofluids directly or indirectly. On the base of the “compressing” model, the Langevin function that usually describes the magnetization of ferrofluid is modified, and a well-fitted curve is obtained. An equation of the relation between the equivalent volume fraction after being “compressed” and the intensity of magnetic field is discovered, which approximately describes the process of magnetization. The relation between the approximate initial susceptibility and the volume fraction can be obtained from modified formula.     

Highly regioselective Buchwald–Hartwig amination at C-2 of 2,4-dichloropyridine enabling a novel approach to 2,4-bisanilinopyridine (BAPyd) libraries

The highly regioselective Buchwald–Hartwig amination at C-2 of the cheap and readily accessible reagent, 2,4-dichloropyridine with a range of anilines and heterocyclic amines is described. This new methodology is robust and provides a facile access to 4-chloro-N-phenylpyridin-2-amines on 0.25 mol scale. These intermediates undergo a further Buchwald–Hartwig amination at higher temperature to enable rapid exploration of the chemical space at C-4 and to provide a library of 2,4-bisaminopyridines.     

KMnO4-mediated oxidative CN bond cleavage of tertiary amines: Synthesis of amides and sulfonamides

KMnO₄-mediated oxidative CN bond cleavage of tertiary amines producing secondary amine was introduced, which was trapped by electrophiles (acyl chloride and sulfonyl chloride) to form amides and sulfonamides. The reaction could take place at mild condition, tolerating a wide range of function groups and affording products in moderate to excellent yields.     

Chemistry of heterocyclic compounds at the A. E. Favorsky Irkutsk Institute of Chemistry, Siberian Branch of the Russian Academy of Sciences, over 50 years (Review)

The review contains a concise historical account and information on the most significant researches undertaken by the staff at the A. E. Favorsky Irkutsk Institute of Chemistry, Siberian Branch of the Russian Academy of Sciences on the Chemistry of Heterocyclic Compounds. Dedicated to Academician of the Russian Academy of Sciences B. A. Trofimov on his 70th jubilee. Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 10, pp. 1443–1502, October, 2008.     

Sulfur-directed metal-free and regiospecific methyl C(sp3)–H imidation of thioanisoles

Regiospecific and direct imidation of the methyl C(sp³)–H bond of thioanisoles is realized under mild and metal-free conditions with N-fluorobis(benzenesulfonyl)imide as an oxidant and nitrogen source. Proposed mechanism suggests that thionium ion intermediates and a Pummerer-type reaction are involved. The imidation has advantages such as high step-economy, excellent functionality tolerance, and regiospecificity, giving structurally diverse imidation products.     

Selective syntheses of 2H-1,3-oxazines and 1H-pyrrol-3(2H)-ones via temperature-dependent Rh(II)-carbenoid-mediated 2H-azirine-ring expansion

The Rh(II)-catalyzed reaction of 2-carbonyl-substituted 2H-azirines with ethyl 2-cyano-2-diazoacetate or 2-diazo-3,3,3-trifluoropropionate provides an easy access to 2H-1,3-oxazines and 1H-pyrrol-3(2H)-ones. These compounds can be selectively prepared from the same starting material using temperature as the only varied parameter. The 2-azabuta-1,3-diene intermediate, a common precursor for both heterocyclic products, isomerizes into 2H-1,3-oxazine under kinetic control, while 1H-pyrrol-3(2H)-one is the sole product of the reaction at elevated temperatures. According to DFT-calculations a one-atom oxazine ring contraction involving ring-opening to a 2-azabuta-1,3-diene intermediate, followed by a 1,5- and 1,2-prototropic shift leads to the consecutive formation of imidoylketene and azomethine ylide, which then further undergo cyclization to the pyrrole derivative.     

Synthesis of 1-benzyloxypyrazin-2(1H)-one derivatives

Different approaches for the synthesis of 1-benzyloxypyrazin-2(1H)-one derivatives from simple amino acids have been investigated. A library of 33 precursors for the preparation of N-hydroxy pyrazinones was obtained in moderate to good yields.