醋酸锰催化合成萘并噻唑衍生物研究型综合实验

设计了“醋酸锰（Ⅲ）催化合成2-邻氯苯甲酰氨基萘并[1，2-d]噻唑”研究型综合化学实验，以自制的醋酸锰（Ⅲ）为催化剂，催化氧化1-萘基-3-邻氯苯甲酰基硫脲合成2-邻氯苯甲酰氨基萘并[1，2-d]噻唑。通过该实验项目的教学，可使学生掌握醋酸锰（Ⅲ）、1-萘基-3-邻氯苯甲酰基硫脲和2-邻氯苯甲酰氨基萘并[1，2-d]噻唑的合成方法，掌握有机化合物结构表征的方法，可以培养学生的实践动手能力、科研创新能力以及综合运用知识的能力。该实验项目集无机合成实验、有机合成实验和仪器分析实验于一体，具有较强的可操作性和实用性，可作为基础化学研究型综合化学实验或开放性实验开设。     

Water-Mediated Synthesis of Benzazole and Thiourea Motifs by Reacting Naturally Occurring Isothiocyanate with Amines

An efficient, green, and facile method has been developed for the synthesis of benzazole and thiourea analogues from naturally occurring erucin in moderate to good yields. The reaction was carried out in water without using any metal catalyst or base. The present method tolerated the various functional groups on aromatic rings and also applicable for other isothiocyanates.     

A novel heterogeneous nanocatalyst: 2‐Methoxy‐1‐phenylethanone functionalized MCM‐41 supported Cu(II) complex for C‐S coupling of aryl halides with thiourea

An environmentally friendly copper‐based catalyst supported on 2‐Methoxy‐1‐phenylethanone functionalized MCM‐41 was prepared and characterized by FT‐IR, FE‐SEM, TEM, XRD, EDX, BET and ICP techniques. The catalyst was applied for the C?S cross‐coupling reaction of aryl halides with thiourea. Corresponding products were produced in good yields in aerobic conditions. The catalyst could be recovered and recycled for several times.     

Synthesis and Structure of N-Ethoxycarbonyl-N′-O-Methoxyphenylthiourea

N-ethoxycarbonyl-N′-o-methoxyphenylthiourea was synthesized and characterized by elemental analysis, TG-DTA analysis, IR, and ¹H NMR spectrum, and single crystal X-ray diffraction analysis. The compound crystallizes as a planar molecule in the monoclinic space group P2(1)/c, with a = 9.690(2)Å, b = 8.595(2)Å, c = 15.944(4)Å, α = 90°, β = 106.467(4)°, γ = 90°, and D_calc = 1.326 g/cm³ for Z = 4. Intramolecular H-bonds promote the stability of the title compound and change the coordination ability of the thiourea ligand. Intermolecular N─H…S H-bonds link pairs of two molecules.     

新型N-(取代芳氧乙酰胺基)-N'-(1-甲基环己基酰基)硫脲及其环合产物的合成及其杀虫活性

采用亚结构拼接法,将苯氧乙酸类结构引入酰基硫脲中,设计并合成了8个新型的硫脲类化合物——N-(取代苯氧乙酰胺基)-N'-(1-甲基环己基酰基)硫脲(5a~5h);5a~5h在酸性条件下关环形成8个新型的含1,3,4-噻二唑的酰胺类化合物——1-甲基-N-(5-取代基-1,3,4-噻二唑-2-基)环氧甲酰胺(6a~6h),其结构经1H NMR和ESI-MS表征。初步的生物活性测试结果表明,在用药量为500mg·L-1时,N-(2,4-二氯苯氧乙酰胺基)-N'-(1-甲基环己基酰基)硫脲对粘虫的抑制率为80%。     

Divalent manganese,cobalt, copper and cadmium complexes of (Z)‐N‐benzoyl‐N′‐(1H‐1,2,4‐triazol‐3‐yl)carbamimidothioic acid: Preparation,characterization, computational and biological studies

In this work, (Z)‐N‐benzoyl‐N′‐(1H‐1,2,4‐triazol‐3‐yl)carbamimidothioic acid and its Mn(II), Co(II), Cu(II) and Cd(II) complexes were introduced for the first time. This carbonyl thiourea ligand was prepared by the reaction of 1H‐1,2,4‐triazol‐3‐amine with benzoyl isothiocyanate. The structural elucidation of these compounds was performed using elemental analysis and spectral and magnetic measurements. Octahedral structures of all complexes, except Cd(II) complex with a tetrahedral geometry, were confirmed by applying DFT structural optimization. The thermal decomposition behaviour of metal complexes of carbonyl thiourea ligand is discussed. The calculation of kinetic parameters for prepared complexes (E_a, A, ΔH*, ΔS* and ΔG*) of all thermal degradation stages has been evaluated using two comparable approaches. Antimicrobial and ABTS‐antioxidant studies indicated potent activity of Cd(II) complex compared with the other investigated compounds. The cytotoxic activity of the prepared compounds was investigated in vitro. The results indicated potent activity of Mn(II) complex against both HePG2 (liver carcinoma) and MCF‐7 (breast carcinoma) cancer cells.     

Antitumor Activity of Some Novel 1,2,5-Thiadiazole Derivatives

Some novel thiourea,1,2,4-triazole, quinazoline, thieno[2,3-d]pyrimi-dine, and thiazolidine derivatives were synthesized to evaluate their antitumor activity. Compound (3f) is nearly as active as reference drug, (Doxorubicin) as positive control.     

A New Simple Voltammetric Method for Thiourea and Thiourea Dioxide Determinations

Abstract

Linear sweep voltammetry at glassy carbon or other carbon materials is shown to be a simple, highly sensitive, and relatively versatile analytical method for the determination of thiourea and thiourea dioxide. Using the first one-electron oxidation peak occurring at ～0.6V, thiourea can be determined directly in a variety of electrolytes from concentrated acids to solutions of pH ～5. The thiourea dioxide determination is based on the two-electron oxidation peak which appears in a number of electrolytes at ～1.2V.     

Facile and Rapid Synthesis of 4,5-Dihydrothiazol-2-ylamine Derivatives via Reaction Between Thiourea and Diaroylacetylenes

Heterocyclic systems 4,5-dihydrothiazol-2-ylamine derivatives are synthesized via an intramolecular thioiminoformamide annulation reaction.     

Rapid Synthesis of N-Acyl Ureas from Their Thio Analogues Using Wet Silica-Supported Permanganate Under Solvent-Free Conditions

A rapid method to N-acyl ureas from corresponding N-acyl thioureas is described. N-coumaroyl-N′-arylthioureas, which are easily prepared by the reaction of coumarin-3-carboxylic acid chloride with potassium thiocyanate and arylamines, can be expeditiously transformed into corresponding N-acyl ureas via r.t. grinding with wet silica supported potassium permanganate under solvent-free conditions in an excellent yield.