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...     

光学活性2－氨基－6，6－二甲基庚酸的合成

光学活性２－氨基－６，６－二甲基庚酸的合成袁荣鑫，张雅文，陈克潜（徐州医学院化学教研室，２２１００２）（苏州大学化学系，２１５００６）为合成一类新型ＬＨＲＨ类似物，我们首先合成了一系列含有叔丁基结构的大量非蛋白氨基酸，其中包括２－氨基－６，６－二甲基...     

3－嘧啶胺基或三嗪胺基甲酰基－4－羟基－2H－1，2－苯并噻嗪－1，1－二氧化物的合成及活性

通过３－乙氧甲酰基－４－羟基－２－氢（甲基）－２Ｈ－１，２－苯并噻嗪－１，１－二氧化物与取代嘧啶胺或均三嗪胺的胺解反应，合成了标题化合物。生物活性测定结果表明多数化合物具有较好的除草活性，部分化合物显示好的植物生长调节活性和抗炎免疫活性。     

γ－［N_1－取代－1，4，5，6－四氢（及1，6－二氢）－6－氧－3－哒嗪酰胺基］丁酸乙酯类化合物的合成

γ－［Ｎ_１－取代－１，４，５，６－四氢（及１，６－二氢）－６－氧－３－哒嗪酰胺基］丁酸乙酯类化合物的合成许凤荣，王书玉，徐萍，黎辉，胡长风，欧阳荔（北京医科大学药学院、分析计算中心波谱室，北京，１０００８３）关键词６－氧－３－哒嗪酸，哒嗪类衍生物，...     

2－烷基环戊－2－烯酮衍生物的合成及抗炎活性研究

２－烷基环戊－２－烯酮衍生物的合成及抗炎活性研究齐传民计志忠，李玉兰，王彪（北京农业大学应用化学系，北京，１０００９４）（沈阳药科大学）关键词环戊烯酮衍生物，β－氨基甲基酮，Ｍａｎｎｉｃｈ反应，缩合反应，抗炎活性目前，许会抗炎药物是芳香酸类比合物，它...     

3－芳基－1（2H，4H）－吖啶酮衍生物的合成及其镇痛作用

３－芳基－１（２Ｈ，４Ｈ）－吖啶酮衍生物的合成及其镇痛作用韩光范，魏永慧，尹荣王进军姜贵吉（吉林医学院检验系吉林１３２００１）（吉林化工学院精细化工系吉林）（延边大学化学系延吉）关键词吖啶酮衍生物，合成，镇痛作用吖啶及吖啶酮类化合物具有抗疟、抗菌、抗...     

α，α，2，6－四氯甲苯合成反应的色－质谱联用研究

本文利用ＧＣ、ＧＣ／ＭＳ研究了通过２－氯－６－硝基甲苯（Ａ）氯化制备α，α，２，６－四氯甲苯的反应过程。发现氯化首先在α－甲基上进行，生成α，２－二氯－６－硝基甲苯（Ｂ），Ｂ经硝基取代氯化（主要途径）生成α，２，６－三氯甲苯（Ｃ），Ｃ进一步发生α－氯代生成目的产物（Ｄ）。少量Ｂ还可经进一步的α－氯化形成α，α，２－三氯－６－硝基甲苯（Ｅ），Ｅ进一步发生硝基的氯取代而形成Ｄ。     

1－（取代异噁唑基）－1，2，4．三唑和1－（取代嘧啶基）－1，2，4－三唑的合成及生物活性

合成了１５个新的１－（取代异噁唑基）－１，２，４－三唑和１－（取代嘧啶基）－１，２，４－三唑化合物，经元素分析、ＩＲ、１ＨＮＭＲ和ＭＳ证实其结构，并对其代表化合物进行了抑菌及植物生长调节活性的初步观察     

螺［异苯并呋喃－1（3H），9＇－（9H）－2＇－N，N－二苄胺基－6＇－二乙胺基占吨］－酮－3的合成及晶体结构研究

合成了螺［异苯并呋喃－１（３Ｈ），９＇－（９Ｈ）－２＇－Ｎ，Ｎ－二苄胺基－６＇－二乙胺基占吨］－酮－３，Ｃ＿（３７）Ｈ＿（３４）Ｎ＿２Ｏ＿３，单斜晶系，空间群Ｃｃ，晶体学参数为ａ＝１６．８２６（４），ｂ＝１０．６４８（４），ｃ＝１７．６１８（７），β＝９２．２５（２）°，Ｖ＝３１５４（２），Ｚ＝４，Ｍ＿ｒ＝５６６．７，Ｄ＿ｘ＝１．１９ｇ／ｃｍ３，Ｆ（０００）＝１２００。结构由直接法解出，偏离因子Ｒ＝０．０８０。分子由占吨和异苯并呋喃两部分组成Ｙ形结构，占吨部分相连的苄基的两个苯环位于占吨部分的两侧。     

一个新的Gibbs试剂：2，6－二苯基－p－苯醌－4－氯亚胺

设计并合成了２，６二苯基－ｐ－苯醌－４－氯亚胺１ｃ，作为一个新的使酚类显色的Ｇｉｂｂｓ试剂，与酚类在碱性溶液中生成兰绿色的２，６－二苯基靛酚盐２ｃ。由于苯基的引入，扩大了靛酚的共轭体系和极化效应，故２，６＝二苯基靛酚盐２ｃ的λ＿（ｍａｘ）和ε＿（ｍａｘ）都比相当的２，６－二氯靛酚盐２ａ为大。２ｃ经酸化后成为红色的游离２，６－二苯基靛酚，具有良好的化学稳定性。     

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%).     

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.     

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.     

Synthesis of pyrrolo[1,2-a]pyrazines and pyrazino[1,2-a]indoles by Curtius reaction in Morita-Baylis-Hillman derivatives

Synthesis of substituted pyrrolo[1,2-a]pyrazines and pyrazino[1,2-a]indoles from the Morita-Baylis-Hillman derivatives of acrylates via saponification followed by Curtius reaction is described.     

正丁胺对激光染料荧光谱影响的研究

用正丁胺作为碳源,采用射频辉光放电制备碳膜,选用激光染料R6G和聚乙二醇混合液作为蒸气源,采用单源热蒸发,在蒸发室与染料同时沉积得到混合膜,用拉曼光谱和红外光谱分析了碳膜的结构和键合方式,分析表明:碳膜中存在胺基团和氢原子.混合膜的荧光谱测量结果表明,认为正丁胺对染料荧光谱的影响是因为胺基和氢原子的存在.     

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.