1－芳酰基－4－芳基氨基脲类化合物的合成及表征

利用N－取代三氯乙酰胺与芳基酰肼反应，合成了6个新的1－芳酰基－4－芳基 氨基脲类化合物，其结构经IR，^1H NMR和元素分析证实。初步生物活性测试表明 ，具有一定的除草活性。     

2－取代－5－氟脲嘧啶的β－D－乙酰基木糖苷的合成

以相转移催化法和Ｋｏｅｎｉｇｓ－Ｋｎｏｒｒｓ反应，使α－溴代乙酰基木糖与２－取代－５－氟脲嘧啶或其银盐作用，合成了１１个未见文献报道的糖苷类化合物。其结构经ＩＲ、１ＨＮＭＲ、ＭＳ等证实。其中有些化合物有一定的抗肿瘤活性。     

α－取代乙酰胺类化合物结构与除草活性的构效关系研究

分别研究了Ｎ，Ｎ－二取代－α－氯代乙酰胺类化合物及Ｎ，Ｎ－二取代－α－二硫代磷酰基乙酰胺类化合物结构与除草活性的定量关系。结果表明：氮原子上取代基的大小对两类化合物的除草活性具有相同的影响，只是最适宜的疏水性不同，两类化合物可能具有相同的作用机制。     

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－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．     

3，7，10－三甲基杂氮硅三环类化合物的合成及结构分析

３，７，１０－三甲基杂氮硅三环类化合物的合成及结构分析鲁开娟，王天用（中国科学院化学研究所北京１０００８０）带有Ｎ－Ｓｉ配位键的杂氮硅三环类化合物，其性质主要取决于环骨架结构和硅原子上所连接的Ｒ取代基。作者曾将杂氮硅三环化合．物的一个五之环结构扩大成...     

1聚代苯基—4—烃基氨基硫脲的合成及抗菌作用

由烃基异硫氰酸酯与取代邻肼基苯甲醚类化合物的加成反应，合成了１０种新的取代氨基硫脲类化合物，其结构经元素分析、ＩＲ、＾１ＨＮＭＲ等确证。初步生理活性实验表明，对金黄色葡萄球菌和大肠杆菌都有不同程度的杀菌和抑菌作用。     

邻位取代1，2－二苯乙烯催化不对称二羟基化反应

邻位取代１，２－二苯乙烯催化不对称二羟基化反应张生勇，孙晓莉（第四军医大学化学教研室西安７１００３２）关键词　不对称二羟基化，手性二醇近年催化的反式稀烃的不对称二羟基化反应取得明显进展［１］，但催化的邻位取代的１，２－二苯乙烯类化合物的不对称二羟基化...     

α－羰基烯酮环二硫代缩醛化学XXI：β，β－1，3－亚丙二硫基－α，β－不饱和酮与胍的缩合反应

在乙醇为溶剂，乙醇钠为碱的条件下，标题类化合物归１ａ～ｃ，３ａ，４ａ与胍缩合反应生成相应的嘧啶类化合物２ａ～ｃ，３ｂ，３ｃ，４ｂ。在以ＤＭＦ为溶剂，乙醇钠为碱的条件下，化合物与胍反应可生成２－氨基－４－二甲氨基－６－苯基嘧啶２ａ’。该缩合反应的特点为标题类化合物与肌缩合生成嘧啶类化合物的同时，将乙氧基或二甲氨基引入嘧啶环的确定位置。为新的嘧啶类化合物。     

取代甲基亚磺酰基苯并咪唑类化合物的合成

合成了一系列取代甲基硫代苯并咪唑类化合物，并在过氧乙酸的氧化下得到了 取代甲基亚磺酰基苯并咪唑类化合物，收率较好(79%～97%)，代替了用间氯过氧苯 甲酸进行氧化，反应过程稳定，降低了成本。     

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.     

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.     

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.     

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%.     

Catalyst free,visible-light promoted photoaddition reactions between C60 and N-trimethylsilylmethyl-substituted tertiary amines for synthesis of aminomethyl-1,2-dihydrofullerenes

An efficient and benign method for the preparation of aminomethyl-substituted fullerenes has been developed. The process, involving catalyst free, visible-light irradiation of 10% EtOH-toluene solutions containing fullerene C₆₀ and N-trimethylsilylmethyl-substituted amines by using a 20 W compact fluorescent lamp, leads to formation of aminomethyl-substituted fullerene adducts in a highly efficient manner. The photoaddition reaction takes place via a pathway initiated by visible light absorption by C₆₀, followed by SET from the amine to the triplet excited state of C₆₀. Ethanol-promoted desilylation of the resulting a minimum radical then generates the corresponding α-amino radical which couples with the C₆₀ radical anion to form the anion precursor of the fullerene adducts. The new approach using visible-light takes place under mild conditions and it does not require the use of photocatalysts. Thus, the method developed in this effort could broadens the range of functionalized fullerene derivatives that can be readily prepared.     

Highly efficient and stereoselective cycloaddition of nitrones to indolyl- and pyrrolylacrylates

The reactions of various nitrones with indolyl- and pyrrolylacrylates proceeds regioselectively with high diastereoselectivity in the case of aldonitrones, and represents an effective method for obtaining new indolyl- and pyrrolyl-substituted isoxazolidine carboxylates stabilized by weak (CH?O) and moderate (NH?N) strength intramolecular hydrogen bonding. The resulting cycloadducts exhibit promising in vitro anti-influenza activities.     

Transition metal-free direct amination of benzoxazoles using formamides as nitrogen sources

A transition metal-free method for the direct amination of benzoxazoles using formamides as nitrogen sources is reported, which was mediated by an inexpensive and environmentally friendly tetrabutylammonium iodide/tert-butyl hydroperoxide system and gave the 2-aminobenzoxazole derivatives with moderate to good yields.     

l-Proline-catalyzed five-component domino reaction leading to multifunctionalized 1,2,3,4-tetrahydropyridines

Multifunctionalized 1,2,3,4-tetrahydropyridines are concisely synthesized in good yields via l-proline-catalyzed or l-proline/FeCl₃-cocatalyzed one-pot multicomponent reactions (MCRs). The MCRs involve a domino hydroamination/prins reaction/Mannich-type reaction/intramolecular dehydration-cyclization process. The molecular structure of 5baa, one of multifunctionalized 1,2,3,4-tetrahydropyridines, was confirmed by single-crystal X-ray diffraction.