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综合制备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。     

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。     

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－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．     

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。     

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。     

2,4—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     

磷杂螺环化合物的合成──3，9－二氢－3，9－二硫代－2，4，8，10－四氧杂－3，9－二磷杂螺环［5，5］十一烷的合成及其与α－芳基－β－硝基烯的加成反应

本文合成了３，９－二氢－３，９－二硫代－２，４，８，１０－四氧杂－３，９－二磷杂螺环－［５，５］十一烷２，研究了２在Ｎ，Ｎ－二甲基乙酰胺介质中，在氢化钠作用下与α－芳基－β－硝基烯的加成反应，得到５个新的加成产物３_（ａ－ｅ），对２及加成物３_（ａ－ｅ）的~１ＨＮＭＲ谱进行了归属，并得到元素分析和ＩＲ的证实。     

电子受体与诺氟沙星的电荷转移反应

本文研究了电子受体对苯醌、２，３－二氰－５，６－二氯－１，４－对苯醌、四氯对苯醌和四溴对苯酯与诺氟沙星［１－乙基－６氟－１，４－二氢－１，４－二氢－４－氧人－７－（１－哌嗪基）喹啉－３－羧酸］电子给体之间的荷移反应。     

3－芳基－5，6－二氢噻唑并［2，3－C］均三唑和3－芳基－6，7－二氢均三唑并［3，4－b］［1，3］噻嗪的合成

３－芳基－５，６－二氢噻唑并［２，３－Ｃ］均三唑和３－芳基－６，７－二氢均三唑并［３，４－ｂ］［１，３］噻嗪的合成王忠义，史海健，史好新（安徽师范大学化学系，芜湖２４１０００）张自义（兰州大学化学系）三唑类化合物具有相当广泛的生物活性，如：抗菌、抗痉...     

A carbanion induced synthesis of highly congested pyrazole and imidazole containing heterocycles

An efficient approach to the synthesis of highly congested di, penta and hexacyclic pyrazoles as well as imidazole fragment containing novel heterocyclic molecule has been developed through a carbanion induced transformation of suitably functionalized 2H-pyran-2-ones, benzo[h]chromene and thiochromeno[4,3-b]pyrans. Due to the presence of fluorescence, we report their prime application metal sensor as off/on switching in ferric ions.     

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.     

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%).     

Selective synthesis of 4,5-dihydroimidazo- and imidazo[1,5-a]quinoxalines via modified Pictet–Spengler reaction

An efficient tandem approach for the selective synthesis of 4,5-dihydroimidazo[1,5-a]quinoxalines 6a–g and imidazo[1,5-a]quinoxalines 7a–h by the reaction of 2-imidazolyl anilines 4a–c with aryl aldehydes 5a–k under mild reaction conditions is described. Introduction of electron releasing alkyl groups in substrates 4a–b was found to be instrumental for the success of the reaction.     

Understanding the Diels-Alder reactivity of 1,2-azaborine analogues

The Diels-Alder reactivity of 1,2-heteroborines (H₄C₄B(H)X, X?=?NH, PH, AsH; O, S, Se) has been computationally explored by means of Density Functional Theory (DFT) calculations. The influence of the HB?=?X fragment on the reactivity of the system has been quantitatively analyzed in detail by means of the so-called Activation Strain Model (ASM) of reactivity. It is found that the interaction between these species and the dienophile is significantly stronger than that computed for their all-carbon isoelectronic counterpart, benzene. In addition, the strain energy plays a key role in the observed reactivity trends. The role of the aromaticity strength of these heteroarenes on the reactivity is also assessed.     

Synthesis of N-substituted carbazolones from α-iodo enaminones via Pd(0)-catalyzed intramolecular coupling under microwave irradiation

A variety of N-aryl and N-alkyl carbazolones were conveniently achieved in good to high yields via Pd₂(dba)₃-mediated intramolecular coupling of N-substituted α-iodo enaminones under microwave irradiation. The Pd(0)-catalyzed cyclization was found to proceed favorably with the more electron-deficient phenyl ring during the reactions involving unsymmetrical N,N-diaryl α-iodo enaminones. This unique property enables the construction of carbazolone skeleton containing nitro substituted benzenoid ring.     

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.     

Facile synthesis of bicyclic 1-arylpyrazol-5-ones

In this Letter, we described a facile method for constructing fused bicyclic 1-arylpyrazol-5-one ring system. We employed various methylene-containing carboxylic acids as the substrates and proved that the pyrazolone ring closure requires activated methylene group in intermediate II. Accordingly, a series of structurally diversified, fused bicyclic 1-arylpyrazol-5-ones was prepared in moderate to high yields using the requisite substrates.     

Synthesis of substituted 2,4,5,6-tetrahydrocyclopenta[c]pyrazoles and 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles by intramolecular nitrilimine cycloaddition

Both substituted 2,4,5,6-tetrahydrocyclopenta[c]pyrazoles and 2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazoles have been synthesized by the 3+2 intramolecular dipolar cycloaddition of nitrilimines to alkynes. This cyclization has been extended to more versatile 3-bromo derivatives by the use of alkynylbromides as dipolarophiles.