水杨醛缩2-氨基-4-苯基噻唑及其配合物的合成与仿酶催化活性研究

The new containing Surfur Schiff base Salicylaldelye-2-amino-4-Phenylthiazole(SAPTZ) and its Cu(Ⅱ)、Zn(Ⅱ)、Ni(Ⅱ) and Co(Ⅱ) compelexes were synthesized. The structures of the complexes were characterized by elemental analysis, IR and UV-vis. The peroxidase-like activity of the complexes for the oxidation of Vc with H₂O₂ was determined.     

DIASTEREOSELECTIVE SYNTHESIS AND STEREOCHEMISTRY OF (Z)-1-[3-ARYL-2-(PHENYLSULFANYL)-2-OXIRANYL]-1-ETHANONES

Diastereoselective synthesis of a series of (Z)-1-[3-aryl-2-(phenylsulfanyl)-2-oxiranyl]-1-ethanones was effected from the reaction of (Z)-4-aryl-3-(phenylsulfanyl)-3-buten-2-ones with alkaline hydrogen peroxide in tetrahydrofuran. The stereochemistry of the oxiranes has been deduced from two-dimensional NOESY spectrum.     

2,5-取代-1,3,4-噁二唑化合物库的固相合成

本文使用组合化学方法以聚苯乙烯亚磺酸钠树脂（1）为载体合成了2，5-取代-1，3，4-二唑化合物库。树脂1首先与溴代乙酸乙酯反应生成聚合物支载的乙酸酯（2）。肼解后所得的肼树脂进一步与取代的苄氯反应得双欧讲树脂（4）。树脂4与三氯氧磷回流得聚合物支载的2，5-取代-1，3，4-二唑（5）。用W-溴代乙酰苯酮烷基化后聚合物支载的产物用三乙胺解脱得2-芳基-5-芳甲酰亚乙烯基-1，3，4-二唑化合物库，产率15％-36％。     

SYNTHESIS OF 2-THIOXOPYRIDO[2,3-d]PY RIMIDINE-4- ONES AND 1,4-BRIDGED BIS-2-THIOXO-1,2,3,4-TETRAHYDRO-5-PYRIMIDINE CARBOXYLIC ACID ETHYL ESTER DERIVATIVES

Abstract

The synthesis and structural characterization of 2-thioxopyrido[2,3-d]pynmidinethiones 5,9,12 and 4,4′-(1,4-phenylene)-di-(2-thioxo-1,2,3,4-tetrahydropyrimidines) 16-22 are described.     

A novel three-component reaction of 1, 1-dicyano-2-(trifluoromethyl)ethylenes,primary arylamines,and ketones

1, 1-Dicyano-2, 2-bis(trifluoromethyl)ethylene and 3, 3-dicyano-2-(trifluoromethyl)acrylates react with primary arylamines in the presence of ketones to form 1, 1-aryl-1, 4-dihydropyridme derivatives under mild conditions. The mechanism of this three-component reaction includes the formation of Schiffs bases as intermediates. 1, 4-Dihydropyridine derivatives, which are the products of three-component heterocyclization, were also obtained by reaction the corresponding Schiffs bases with 1, 1-dicyano-2-(trifluoromethyl)ethylenes.Translated fromIzvestiya Akademii Nauk. Seriya Khimicheskaya, No. 3, pp. 552–559, March, 1993.For preliminary communication see Ref. 1.     

SYNTHESIS AND FUNGICIDAL ACTIVITIES OF DERIVATIVES OF 2-ALKYLTHIO-3-AMINO-4H-IMIDAZOL-4-ONE

2-Alkylthio-3-phenylamino-5-arylmethylene-4H-imidazol-4-ones 5 were synthesized by S-alkylation of 3-phenylamino-2-thioxo-4-imidazolidinones 4, which were obtained via cyclization of isothiocyanates 2 with phenylhydrazine in presence of solid potassium carbonate. Compound 5 exhibited fungicidal activity.     

Condensation products of 1-aryl-4-hydrazinocarbonyl-2-pyrrolidinones with diketones

The reactions of 1-aryl-4-hydrazinocarbonyl-2-pyrrolidinones with 2,4-pentanedione and 2,5-hexanedione have been studied. It was found that heating the hydrazinocarbonyl compounds with 2,4-pentanedione gave 3,5-dimethylpyrazole compounds and with 2,5-hexanedione gave 1-substituted 2,5-dimethylpyrroles. __________ Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 2, pp. 229–232, February, 2008.     

New Method of Synthesis of 2-Amino-4(5H)-oxothiophenes

A new method is proposed for the synthesis of 2-amino-4(5H)-oxothiophenes with aryl and hetaryl substituents in position 3 of the molecule by the acylation of aryl- and 2-azahetarylacetonitriles with mercaptoacetic acid ethyl ester.__________Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 2, pp. 202–205, February, 2005.     

4-hydroxy-2-quinolones. 43. Thermolysis of ethyl esters of 1-R-2-oxo-4-hydroxy-quinoline-3-carboxylic acids

Ethyl esters of 1-R-2-oxo-4-hydroxyquinoline-3-carboxylic acids under thermolysis conditions are converted to 5,9-di-R-6,7,8-trioxodiquinolino[3,4-b;3,4-e]-4H-pyrans. One of the synthesized compounds was studied by X-ray diffraction.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 4, pp. 516–522, April, 2000.     

Oxidizing Reactions of Azines. 7. Imination of 4-Aryl-1,2,3,6-tetrahydropyridines by Arylamines in the Presence of Potassium Permanganate. Molecular Structure of 1-Methyl-2-(4-nitrophenylimino)-4-phenyl-1,2,5,6-tetrahydropyridine

On treating 4-aryl substituted 1-methyl-1,2,3,6-tetrahydropyridines with potassium permanganate in the presence of arylamines a previously unknown intermolecular oxidative imination reaction occurs leading to the formation of 2-(arylimino)-1,2,5,6-tetrahydropyridines. The molecular structure of 1-methyl-2-(4-nitrophenylimino)-4-phenyl-1,2,5,6-tetrahydropyridine was studied by X-ray analysis and it was shown that the hydropyridine ring of the molecule has a sofa conformation and its amidine fragment is in the E-configuration.     

含1，3，4-噁二唑取代的酰基硫脲的合成及杀菌活性

大量文献报道了1，3，4-噁二唑的合成及广泛的生物活性，酰基硫脲类化合物也因其广谱的生物活性引起了人们浓厚的研究兴趣。根据活性因子叠加的原理，本文将一系列1，3，4-噁二唑引入到酰基硫脲中，从对氯苯氧乙酸出发，得到的酰基异硫氰酸酯再与一系列2-氨基-5-芳基-1，3，4-噁二唑反应，合成了10个酰基硫脲类化合物。所有化合物均经元素分析、红外光谱、核磁共振谱和质谱确认。同时对所有化合物进行了生物活性测试。合成路线如下。     

Synthesis of 1, 4-Bis[3-N-propionyl-2-aryl-1, 3, 4- oxadiazoline-5-yl]phenylenes

1, 3, 4-Oxadiazoline derivatives are found to possess significant biological activities such as antifungal1, insecticidal2, CNS depressant3-5, anticonvulsant effects and plant growth accelerator. They are highly important heterocycles, and have been used …     

Synthesis of Alkyl 5,6-Dialkyl-2-amino-3-cyanopyridine-4-carboxylates

An unusual route has been found for the hydrolysis of 3-amino-1,1-dialkoxy-6,7-dialkyl-4-aryl-3a,4,5,7a-tetrahydro-1H-pyrrolo[3,4-c]pyridine-3a,7a-dicarbonitriles in acidic medium which leads to the formation of alkyl 5,6-dialkyl-2-amino-3-cyanopyridine-4-carboxylates.     

4-Hydroxy-2-quinolones. 56. 4-(Adamant-1-yl)thiazolyl-2-amides of 1-R-4-Hydroxy-2-oxoquinoline-3-carboxylic Acids as Potential Antitubercular Agents

The synthesis, antitubercular, anti-HIV, and antitumor activity of the 4-(adamant-1-yl)thiazolyl-2-amides of 1-R-4-hydroxy-2-oxoquinoline-3-carboxylic acids have been studied. An efficient method for purifying the 4-hydroxy-2-oxoquinoline derivatives from their metal salts is proposed.     

Reaction of 1-Aryl-3-methylpyrazol-5-ones with 2-Cyanoaryldiazonium Bisulfates

2-Cyanoaryldiazonium bisulfates, obtained by the action of nitrosyl sulfuric acid on isatin 3-hydrazone and its 5-bromo and 5-nitro derivatives, couple with 1-aryl-3-methylpyrazol-5-ones and form 4-arylhydrazones of 1-aryl-3-methylpyrazole-4,5-diones. It was established on the basis of data of IR, UV, and ¹H NMR spectra and of X-ray structural analysis that the coupling products exist in the hydrazone form stabilized by an intramolecular hydrogen bond.__________Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 2, pp. 210–215, February, 2005.     

3-氨基-5-取代苯氨基-6-苯基-1,2,4-三嗪的合成

3-氨基-1,2,4-三嗪化合物具有广泛的生理活性,如:治疗支气管扩张、抑制乳酸菌和症原虫繁殖杀菌等,因此,研究这类化合物合成方法应运而生。本文以苯甲酰基硫代甲酰胺为原料,进一步合成了氨基-5-取代苯氨基-6-苯基-1,2,4-三嗪。     

Synthesis of 3,5-disubstituted 4-aminoisoxazoles by cyclization of <Emphasis Type="Italic">O</Emphasis>-(β-oxoalkyl)-substituted α-hydroxyimino nitriles

4-Amino-5-benzoyl(acetyl)isoxazole-3-carboxamides were prepared by cyclization of α-hydroxyimino nitriles O-alkylated with bromoacetophenones (bromoacetone). The purity of the target 4-aminoisoxazoles can be substantially increased by treating O-alkylated oximes with LiClO₄ before cyclization. __________ Published in Russian in Izvestiya Akademii Nauk. Seriya Khimicheskaya, No. 5, pp. 1159–1165, May, 2005.     

Synthesis and Crystal Structure of Ag2（admtrz）2（CF3CO2）2（admtrz=4—amino—3,5—dimethyl—1,2,4—triazole）

1 INTRODUCTION Transition metal complexes bridged by 1, 2, 4-triazole group can produce interesting structures and specific properties[1]. Many attempts have been made to synthesize a variety of complexes with paramagnetic centers by using such ligands, and their structures and magnetic properties have been characterized[2]. However, the polynuclear Ag(I) complexes bridged by 1, 2, 4-triazole have been poorly studied[3]. Recently, we have prepared a series of silver(I) triazole complex…