1-苯氧基乙酰基-4-(邻硝基苯甲酰基)氨基硫脲及其相关杂环化合物的合成研究

芳氧基乙酸及其衍生物对植物有很强的生理活性,广泛用作除莠剂和植物生长调节剂［１,２］．１,４－二酰基取代的氨基硫脲及其杂环衍生物亦有多种生物活性［３］．若将上述两类具有生物活性的基团聚集于同一分子中,实现其活性叠加,同时改变取代基,有望获得具有更高生物活性的物质．基于此,我们在以前工作［４］的基础上,以ＰＥＧ－４００为催化剂,在固－液相转移条件下,用邻硝基苯甲酰氯与硫氰酸铵反应,首先制得邻硝基苯甲酰基异硫氰酸酯（Ⅰ）,不经分离,Ⅰ直接与芳氧基乙酰肼加成得到了１－芳氧基乙酰基－４－（邻硝基苯甲酰基…     

N-(3-苯基2 ,3,4-三唑甲酰氨基)-N''''-芳酰基硫脲及其环化产物的合成

以PEG 4 0 0为相转移催化剂 ,通过 2 苯基 1,2 ,3 三唑 4 甲酰基肼与芳酰基异硫氰酸酯的加成反应 ,合成了系列新的酰胺基硫脲衍生物 (3 ) ,3分别在酸性和碱性条件下环化制得相应的 1,3 ,4 噻二唑衍生物和 1,2 ,4 三唑啉 5 硫酮衍生物 ,并经元素分析、IR ,1HNMR和MS确证结构。     

Microwave mediated synthesis of non-carboxylic analogues of ibuprofen with improved pharmacological activity

A series of 1,2,4-triazolo[3,4-b]-thiadiazoles were synthesized following microwave irradiation method and also by conventional method.Newly synthesized compounds were evaluated for their anti-inflammatory and analgesic activities.     

Synthesis,Crystal Structure and Bioactivities of <Emphasis Type="Italic">N</Emphasis>-(2,6-Difluorobenzoyl)-<Emphasis Type="Italic">N</Emphasis>′-[5-(Pyrid-4-yl)-1,3,4-Thiadiazol-2-yl]Urea

Abstract N-(2,6-difluorobenzoyl)-N′-[5-(pyrid-4-yl)-1,3,4-thiadiazol-2-yl]urea, 3, has been synthesized by reaction of 2-amino-5-(pyrid-4-yl)-1,3,4-thiadiazole with 2,6-difluorobenzoyl isocyanate, and its structure was characterized with X-ray crystallographic, NMR, MS and IR techniques. It crystallizes in the triclinic space group P − 1, with a = 7.0821(9) ?, b = 9.4896(13) ?, c = 11.6594(15) ?, α = 82.311(2)°, β = 82.328(2)°, and γ = 87.641(2)°. In the title compound, the urea scaffold in each molecule is essentially planar due to the presence of intramolecular N–H···O hydrogen bond. The molecules are linked by intermolecular complementary N–H···O hydrogen bonds into centrosymmetric R ₂²(8) dimers. Intermolecular π–π stacking interactions are also present. The preliminary bioassay shows that the title compound exhibits excellent fungicidal activities against Rhizoctonia solani, Botrytis cinerea and Dothiorella gregaria. Index Abstract N-(2,6-difluorobenzoyl)-N′-[5-(pyrid-4-yl)-1,3,4-thiadiazol-2-yl]urea has been synthesized and characterized with X-ray crystallographic, NMR, MS and IR techniques. The preliminary bioassay shows that the title compound exhibits excellent fungicidal activities.      

噻二唑型缓蚀剂对银片的缓蚀性能

采用增重法和金相显微技术,研究了不同浓度的沉降硫-石油醚溶液对银片的腐蚀作用,以及噻二唑型缓蚀剂TSJ-T6在不同浓度、不同温度下的缓蚀效率。 研究表明,TSJ-T6缓蚀剂对银片具有很好的缓蚀性能,且随着缓蚀剂浓度的增加,缓蚀效率也随之提高,当缓蚀剂浓度达到10.0 μg/g时,缓蚀效率达到94.37%。 经过吸附等温线拟合,得到缓蚀剂TSJ-T6在银片表面的缓蚀符合Langmuir吸附等温式,吸附过程为放热反应过程。     

3-萘基-5-萘偶氮基-[1,3,4]-噻二唑-2-硫酮的合成及谱学研究

3-萘基-5-萘偶氮基-[1,3,4]-噻二唑-2-硫酮由二-α-萘基硫代卡巴腙与二硫化碳在碱性条件下发生加成闭环反应生成.文章研究了该反应的历程,提出该反应的机理是亲核加成,并通过IR谱、UV谱和NMR谱对标题化合物的结构进行了表征.     

Sulfonated salicylidene thiadiazole complexes with Co (II) and Ni (II) ions as sustainable corrosion inhibitors and catalysts for cross coupling reaction

Condensation of 2,5‐dihydrazinyl thiadiazole with 5‐sodium sulfonate salicylaldehyde afforded dibasic tetradentate pincer N,O,O,N‐salicyldiene thiadiazole ligand (H₂Sanp). The novel dipolar ligand formed para‐magnetic pincer complexes within Co (II) and Ni (II) ions (Co‐Sanp and Ni‐Sanp) under sustainable conditions. The water‐soluble ligand and its metal‐complexes were estimated by mass, IR and UV–Visible spectroscopy, EA (elemental analyses), TGA (Thermogravimetric analyses), magnetic susceptibility, and conductivity measurements. The catalytic reactivity of Co‐Sanp and Ni‐Sanp were evaluated in the Suzuki and Buchwald‐Hartwig cross coupling reaction in aqueous‐methanol binary mixtures. Both reactions of boronic acid or aryl amines with aryl halides gave high chemoselective yield of C―C or C―N product. The inhibition characteristics of H₂Sanp and its Ni‐ and Co‐complexes were performed for the C‐steel corrosion in 1.0 M HCl using electrochemical measurements and surface analysis methods. These methods indicated that the synthesized compounds have served as efficient mixed‐type corrosion inhibitors and their adsorption on the steel surface obeyed isotherm model of Langmuir. Co‐Sanp inhibitor displays the best corrosion inhibition efficiency, and the capacity is up to 97.11% at of 250 mg L^?1. Surface analysis confirms formation of protective layer on the C‐steel surface.     

3,6-二苯氧甲基-1,2,4-三唑并[3,4-b]- 1,3,4-噻二唑衍生物的合成及生物活性

以4-氨基-5-苯氧甲基-3-巯基-1,2,4-三唑与取代苯氧乙酸为原料,三氯氧磷为溶剂,回流反应, 合成了3,6-二苯氧甲基-1,2,4-三唑并[3,4-b]-1,3,4-噻二唑衍生物。通过IR、1H NMR和元素分析确定了各化合物分子结构,并对其进行了室内毒力测试,结果表明此类化合物具有较好的杀菌、抑菌活性。     

Synthetic profile of thiadiazoloquinazolines

According to the biological screening reports, a thiadiazoloquinazoline scaffold constitutes a promising source of inspiration for the synthesis of novel bioactive molecules. The current review article summarizes the most recent synthetic routes toward thiadiazoloquinazoline derivatives. According to the position of fusion between the thiadiazole and quinazoline rings, thiadiazoloquinazoline derivatives are classified into three major types, thiadiazolo[2,3-b]quinazolines, thiadiazolo[3,2-a]quinazolines and thiadiazolo[3,2-c]quinazolines.     

Electrochemical Properties of Electrode Modified with Langmuir‐Blodgett Film of p‐tert‐Butylcalix[4]arene Derivatives and Its Application in Determining of Silver

A new type of voltammetric sensor, Langmuir‐Blodgett (LB) film of 5,11,17,23‐tetra‐tert‐butyl‐25,27‐di(3‐thiadiazole‐propanoxy)‐26,28‐dihydroxycalix[4]arene modified glassy carbon electrode (LB_TZCA–GCE), was prepared. The electrochemical properties of LB_TZCA–GCE were researched in detail and its recognizing mechanism for silver ion in aqueous solution was discussed. Using this voltammetric sensor, a new stripping voltammetric method for determining of Ag⁺ was erected with good sensitivity, selectivity, reproducibility and recovery. The detection limit was 8×10^?9 M at accumulation time of 180 s. By this method, real samples (lake water, tap water and synthesis sample) were analyzed and the results obtained were well satisfactory.