2－硫代磷酸酯基－3，4－二氢呋喃并喹啉化合物的合成和抑菌活性

６－取代基－２－氧－３，４－二氢呋喃并喹啉类化合物用氢化钠还原所生成的醇钠与硫代磷酰氯缩合制备３，４－二氢呋喃并喹啉化合物，通过￣１ＨＮＭＲ，ＭＳ和元素分析鉴定了它们的结构，并初步测试了它们的抑菌活性．     

6,7—取代—1H—苯并（de）异喹啉—1,3（2H）二酮的合成

从二氢苊出发合成了６－溴－７－氨基２－（２′，４′－二甲基）苯基－１Ｈ－苯并（ｄｅ）异喹啉－１，３（２Ｈ）－二酮，６－甲氧基－７－氨基－２－（２′，４′－二甲基）苯基－１Ｈ－苯并（ｄｅ）异喹啉－１，３（２Ｈ）－二酮和６，７－二氨基－２－（２′，４′－二甲基）苯基－１Ｈ－苯并（ｄｅ）异喹啉－１，３（２Ｈ）－二酮，测定了它们的荧光量子产率，讨论了分子内重原子溴和给电子基对化合物荧光性质的影响。     

2,4—二羟基—3—芳氨基甲基苯乙酮和8—乙酰基—3—芳基—3,4—二…

研究了在氯化氢－乙醇溶液或乙醇溶液中，２，４－二羟基苯乙酮与甲醛和芳胺的Ｍａｎｎｉｃｈ反应，分别得到了５个２，４－二羟基－３－芳氨基甲基苯乙酮和５个８－乙酰基－３－芳基－３，４－二氧－５－羟基－２Ｈ－１，３－苯并恶嗪新化合物，用元素分析，ＩＲ，ＨＮＭＲ，ＭＳ，ＵＶ确定了它们的结构，并成功地实现了２，４－二羟基－３－芳氨基甲基苯乙酮和８－乙酰基－３－芳基－３，４－二氢－５羟基－２Ｈ，１，３－苯并恶嗪     

5,6—二取代—3,4—二氢—2—吡啶酮的N—烷基化反应

由四个５，６－二取代－３，４－二氢－２－吡啶酮经烷基化反应合成了九个未见文献报道的Ｎ－取代５，６－二取代－３，４－二氢－２－吡啶酮，并确定了它们的结构。     

2—氯／2—甲磺酰基—5—（2—苯基—4—喹啉基）—1,3,4—恶二唑…

借处理２－羟基－５－（２－苯基－４－喹啉基）－１，３，４－恶二唑同ＰＣｌ５／ＰＯＣｌ３之间的反应合成了２－氯－５－（２－苯基－４－喹啉基）－１，３，４－恶二唑（３）和通过２－Ｙｕ基－５－（２－苯基－４－喹啉基）－１，３，４－恶二唑的甲基化，然后氧化制得２－甲磺酰基－５－（２－苯基－４－喹啉基）－１，３，４－恶二唑（６）。并分别研究了３和６同胺、叠氮及肼的反应，得到２，５－二取代的恶二唑新衍生物。初     

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。     

2，4－二羟基－3－芳氨基甲基苯乙酮和8－乙酰基－3－芳基－3，4－二氢－5－羟基－2H－1，3－苯并■嗪的合成及其相互转化

研究了在氯化氢－乙醇溶液或乙醇溶液中，２，４－二羟基苯乙酮与甲醛和芳胺的Ｍａｎｎｉｃｈ反应，分别得到了５个２，４－二羟基－３－芳氨基甲基苯乙酮和５个８－乙酰基－３－芳基－３，４－二氢－５－羟基－２Ｈ－１，３－苯并嗪新化合物。用元素分析、ＩＲ、１ＨＮＭＲ、ＭＳ、ＵＶ确定了它们的结构，并成功地实现了２，４－二羟基－３－芳氨基甲基苯乙酮和８－乙酰基－３－芳基－３，４．二氢－５－羟基－２Ｈ－１，３－苯并嗪二类化合物的转化。     

3—芳基—5—巯基—1,2,4—均三唑的双—Mannich反应研究

研究了在氯化氢－乙醇溶液中，３－芳基－５－巯基－１，２，４－均三唑与甲醛和伯胺（芳胺或脂肪胺）的双Ｍａｎｎｉｃｈ反应，合成了１３的的稠杂环化合物３，５－二取代０四氢均三唑并「３，４－ｂ」「１，３，５」噻二嗪，经元素分析、Ｉ手ＭＳ确定了结构，初步测定了该类化合物的生物活性。     

2,6—二甲基—3—苯基—4α—对甲苯基—7—苯甲酰基—4α,5,6,12—四氢—1H,7H—1,3

通过２－甲基－４－对甲苯基－１－苯甲酰基－２，３－二氢－１Ｈ－１，５－苯并二氮杂Ｚｈｏｕ与由不对称１－苯基－２－偶氮－１，３－丁二酮热解产生的α－羰基烯酮的「２＋４」环加成反应制备了标题化合物（Ｃ３４Ｈ３０Ｎ２Ｏ３，Ｍｒ＝５１４．６２），用Ｘ射线衍射测定了其单晶结构。     

钾通道启开剂研究（I）——反式—4—氨基—3—羟基—3,4—二氢—2,2…

通过溴醇两步环氧化法并采用三苯基膦脱氧合成了一系列新型的反式－４－氨基－３－羟基－３，４－二氢－２，２－二甲基－２－氢－１－苯并吡喃类化合物，通过ＩＲ，ＮＭＲ，ＭＳ和元素分析等手段对其结构进行了确证，研究了其中１３个化合物对ＫＣｌ刺激大鼠胸主动脉条收缩抑制作用，考察了其体外血管扩张活性，还对其中１１个化合物进行了Ｓ．Ｄ．大鼠体内降血压实验，结果表明，所测化合物对低钾刺激引起的收缩均有不同程度的抑制     

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.     

α-Amino acid derived enaminones and their application in the synthesis of N-protected methyl 5-substituted-4-hydroxypyrrole-3-carboxylates and other heterocycles

A new and simple synthesis of novel N-protected methyl 5-substituted-4-hydroxypyrrole-3-carboxylates, which exist in equilibrium with their 4-oxo tautomers, has been developed in two steps starting from N-protected α-amino acids. The key intermediates are enaminones, which can also be isolated, characterized, and used for the construction of other functionalized heterocycles, before they spontaneously decompose to pyrrole products. 4-Hydroxypyrroles are prone to partial aerial oxidation but can be efficiently alkylated or reduced to stable polysubstituted pyrrolidine derivatives.     

Specific intramolecular aromatic CH insertion of diazosulfonamides

The chemoselectivity in the intramolecular CH insertion of various diazosulfonamides has been experimentally studied. The results reveal that the aliphatic 1,4-, 1,5-, or 1,6-C(sp³)?H insertions of diazosulfonamides are not accessible, while the aromatic 1,5-C(sp²)?H insertion can be realized specifically by adjusting the diazo-adjacent group. In addition, the general chemoselectivities in the intramolecular CH insertions of diazosulfonyl compounds are summarized. Generally, diazosulfones undergo both aromatic 1,5-C(sp²)?H and aliphatic 1,5- and 1,6-C(sp³)?H insertions, while diazosulfonates undergo aliphatic 1,5- and 1,6-C(sp³)?H insertions. However, diazosulfonamides only undergo aromatic 1,5-C(sp²)?H insertion.     

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.     

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.     

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.     

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.     

N-Heterocyclic carbene-palladacyclic complexes: synthesis,characterization and their applications in the C-N coupling and α-arylation of ketones using aryl chlorides

N-Heterocyclic carbene-palladacyclic complexes 3 were successfully achieved in a one-pot procedure under mild conditions. The structure of 3a was unambiguously confirmed by X-ray single crystal diffraction and it was an active catalyst in the Buchwald-Hartwig amination and α-arylation of ketones even at very low catalyst loadings (0.01?mol%).     

Iodine-mediated oxidative Pictet-Spengler reaction using terminal alkyne as the 2-oxoaldehyde surrogate for the synthesis of 1-aroyl-β-carbolines and fused-nitrogen heterocycles

An efficient iodine-mediated oxidative Pictet-Spengler reaction in dimethyl sulphoxide (DMSO) using terminal alkynes as the 2-oxoaldehyde surrogate for the synthesis of aryl (9H-pyrido[3,4-b]indol-1-yl)methanones is described. The scope of the protocol includes the total synthesis of Fascaplysin, Eudistomins Y₁ and Y₂. The methodology is extended for preparing pyrrolo[1,2-a]-quinoxaline and indolo[1,5-a]quinoxaline derivatives. The utility of 1-aroyl-β-carbolines was demonstrated by performing palladium-catalyzed β-carboline directed ortho-C(sp2)-H functionalization of the phenyl ring with thiomethyl (SMe) group using DMSO as source and for accessing 4-aryl-canthin-6-ones.