N—亚水杨基氨基酸3d金属配合物的合成,表征和抑菌活性

合成了丙氨酸、亮氨酸水杨醛席夫碱及其与Ｍｎ（Ⅱ）、ＣＯ（Ⅱ）、Ｎｉ（Ⅱ）、Ｚｎ（Ⅱ）、Ｃｕ（Ⅱ）的配合物，通过元素分析、摩尔电导、磁化率、红餐光谱和电子光谱等进行了睛征，用ＰＨ法测定了配合物稳定常数，实验发现，配合物抑菌活性优于配体抑菌活性。     

联苯乙酮缩氨基硫脲合铜（Ⅱ）配合物的合成和生物活性

合成了联苯乙酮缩氨基硫脲及其与Ｃｕ（Ⅱ）的配合物，通过元素分析、摩尔电导、红外光谱和电子光谱等进行表征，证明配合物为四配位的平面正方形结构．用ｐＨ法测定了配体的质子化常数和配合物的稳定常数．抗菌活性实验表明，配体具有良好的抑菌活性，与Ｃｕ（Ⅱ）形成配合物后抑菌活性大大增强．     

对溴苯乙酮缩氨基硫脲配合物的合成表征与抑菌活性

合成了对溴苯乙酮缩氨基硫脲（ＨＬ）与Ｎｉ（Ⅱ）、Ｚｎ（Ⅱ）、Ｃｏ（Ⅲ）的配合物，通过元素分析、红外光谱、磁矩、摩尔电导等表征了配合物．测试了配合物、配体及盐的抑菌活性．     

新型过渡金属配合物合成,磁性和生物活性

报道９种新的过渡金属［Ｃｒ（Ⅲ）、Ｍｎ（Ⅱ）、Ｆｅ（Ⅲ）、Ｃｏ（Ⅱ）、Ｎｉ（Ⅱ）、Ｃｕ（Ⅱ）、Ｚｎ（Ⅱ）］五苯并咪唑甲基二乙三胺双核配合物的研究。变温磁化率分析结果表明，双核离子间存在反铁磁相互作用。对于二价过渡金属离子，磁交换作用大小为．对配合物进行了体外抗癌活性和农药活性测定，发现部分配合物具有生物活性。     

Cu（Ⅱ）与L－氨基酸和5＇－嘌呤核苷酸配合物的SOD活性

Ｃｕ（Ⅱ）与Ｌ－氨基酸和５＇－嘌呤核苷酸配合物的ＳＯＤ活性邵昌平，赵丽华，刘宇新，郭和夫（中国科学院大连化学物理研究所，大连１１６０２３）关键词Ｃｕ（Ⅱ）－氨基酸配合物，Ｃｕ（Ⅱ）－氨基酸－核苷酸配合物，ＳＯＤ活性．１．前言在已发现的三种超氧化物歧化...     

Co（Ⅱ）和Co（Ⅲ）配合物与C—C的反应性研究

从二炔丙基胺（１）出发,用二氯化钴和三苯膦经二（三苯膦）氯合然合成了戊二烯Ⅱ）配合物（８）;用改进方法,八羰基二钴经多核然配合物１０合成了双钴（Ⅱ）配合物１１．分别考察了这两种不同价态的钴环配合物对富马酸二乙酯的反应活性,配合物８与活性烯烃２反应产生新的稳定的配合物９,配合物１１则生成有机化合物３,根据配合物８的Ｘ射线晶体结构解释了Ｃｏ（Ⅲ）对活性烯烃的反应活性。     

牛磺酸缩PMBP席夫碱及其金属配合物的合成、表征和抑菌活性

目的合成新型牛磺酸Schiff碱及其金属配合物,研究其抑菌活性。方法将配体溶于无水甲醇中,分别加入Zn(Ⅱ),Co(Ⅱ),Ni(Ⅱ),Cu(Ⅱ)金属醋酸盐,加热回流,过滤干燥得目标化合物;运用元素分析、红外光谱和摩尔电导率等表征其结构组成;采用打孔法对其进行抑菌活性研究。结果四种配合物组成为M(L)(H2O)2～3,属于1∶1型的非电解质。抑菌活性试验结果表明,Schiff碱及金属配合物对大肠杆菌、肺炎链球菌有中到高的抑菌活性,其中铜(Ⅱ)和钴(Ⅱ)配合物抑菌活性最强,抗菌活性且强于Schiff碱配体。结论牛磺酸缩PMBP席夫碱金属配合物的制备为配住化学增添新的内容,良好的抑菌活性为其在医药上的应用提供了依据。     

2—氨基噻唑缩水杨醛合Zn（Ⅱ）配合物的合成,表征及抑菌活性

２－氨基噻唑缩水杨醛合Ｚｎ（Ⅱ）配合物的合成、表征及抑菌活性梁芳珍郝京诚黄汝骐（山东师范大学化学系济南２５００１４）众多的Ｓｃｈｉｆ碱及其金属配合物以其良好的抑菌、抗癌和抗病毒的生物活性［１］，一直受到人们的重视。含硫Ｓｃｈｉｆ碱是其中有影响的一类，...     

2-氨基噻唑缩取代水杨醛Zn(Ⅱ)配合物的合成、表征及抑菌活性

合成了４个２－氨基噻唑缩取代水杨醛Ｚｎ（Ⅱ）的配合物,通过元素分析,ＩＲ,１ＨＮＭＲ及ＵＶ－ｖｉｓ光谱进行了结构表征。抑菌实验结果表明,配合物的活性优于配体     

间硝基苯乙酮双缩硫代对称二氨基脲Cu(Ⅰ)、Zn(Ⅱ)、Fe(Ⅱ)Sn(Ⅱ)、Pb(Ⅱ)配合物的直接电化学合成

芳香醛、酮缩氨基硫脲及其金属配合物因其具有良好的抑菌、抗癌和抗病毒的生物活性［１～３］而受到人们的重视。以往芳香醛、酮缩氨基硫脲金属配合物的合成大都是配体和相应金属的盐在乙醇溶剂中完成,用金属阳极在含配体的非水溶剂中的电化学氧化直接合成金属配合物尚未见报道,而非水溶剂电化学阳极溶出法是合成低价金属化合物的有效途径之一［４］。为此,我们合成了新希夫碱间硝基苯乙酮双缩硫代对称二氨基脲（ＨＬ）,并用金属阳极电化学氧化法合成了该配体的Ｃｕ（Ⅰ）、Ｚｎ（Ⅱ）、Ｆｅ（Ⅱ）、Ｓｎ（Ⅱ）、Ｐｂ（Ⅱ）配合物。通过…     

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%.     

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.     

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.     

A general and convenient synthesis of 4-(tosylmethyl)semicarbazones and their use in amidoalkylation of hydrogen,heteroatom, and carbon nucleophiles

A general synthesis of previously unknown semicarbazone-based α-amidoalkylating reagents, 4-(tosylmethyl)semicarbazones, has been developed. The synthesis involved three-component condensation of semicarbazones of aliphatic or aromatic aldehydes with the same or other aldehydes and p-toluenesulfinic acid. The scope and limitations of this reaction were investigated. The compounds obtained were demonstrated to be an efficient α-(4-semicarbazono)alkylating agents. They were reacted with H- (sodium borohydride), O- (sodium methylate), S- (sodium phenylthiolate), N- (pyrrolidine, sodium succinimide), P- (trialkyl phosphites), and C-nucleophiles (sodium diethyl malonate) to give the corresponding products of the tosyl group substitution, 4-substituted semicarbazones, including analogues of nitrofurazone. Among the prepared compounds tested in vitro for antibacterial and antifungal activity, three nitrofuryl-containing semicarbazones exhibited high biological activities with minimum inhibitory concentration (MIC) values of 8–32 μg/mL.     

Synthesis of novel chiral bidentate hydroxyalkyl-N-heterocyclic carbene ligands and their application in palladium-catalyzed Mizoroki–Heck couplings and asymmetric addition of diethylzinc to benzaldehyde

A small library of new chiral bidentate hydroxyalkyl-imidazolium salts 1 is conveniently synthesized on multi-gram scale from inexpensive and commercially available chiral pool amino acids. The corresponding carbenes, generated by deprotonation of imidazolium salts 1, in combination with palladium(II) chloride were tested in the Mizoroki–Heck coupling reaction. The most significant results in terms of yields and reactivities were achieved with low catalyst loading. The catalytic activities of these imidazolium salts were also investigated in the asymmetric addition of diethylzinc to benzaldehyde. The use of MgO nanoparticles as an additive in conjunction with these ligands played a crucial role in increasing the efficiency of these reactions.     

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.     

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.