Synthesis of Novel Benzoylphenylurea Chitin Inhibitors From Chlorothalonil(Ⅱ)

IntroductionThe insecticidal activity of benzoylphenylurea( BPU ) analogues,discovered in the early1 970′s[1_ 4] ,is connected with the process ofmoult-ing and appears to affect the chitin synthesis of in-sects. The benzoylphenylurea class of insectgrowth regulators( IGRs) ,interfere with chitinsynthesis in target pests,causing death or abortivedevelopment and are considered to be the fourthgeneration of insecticides or novel materials for in-sect control.Benzoylphenylurea type insecticides…     

Synthesis of Novel Benzoylphenylurea Chitin Inhibitors from Chlorothalonil

Twenty-six novel benzoylphenylurea chitin inhibitor derivatives have been synthesized in over 30～50% yield from chlorothalonil 1 via sequential fluorine exchange, aminolysis,hydrolysis, decarboxylation and acylation reactions.     

Synthesis of Novel Benzoylphenylurea Chitin Inhibitors From Chlorothalonil （Ⅲ）

Six novel benzoylphenylurea chitin inhibitor derivatives were synthesized in the yields of 30%--50% from the readily available starting material chlorothalonil 1 via sequential fluorine exchange, aminolysis, hy-drolysis and acylation reactions.     

Synthesis and Characterization of Novel Acetohydroxyacid Synthase Inhibitors

IntroductionAcetohydroxyacid synthase(AHAS)serves as thefirst common enzyme in the pathway for the biosynthesisof the branch-chained amino acids,isoleucine,valine,and leucine[1].This pathway is found in bacteria,fun-gi,algae,and higher plants,butnotin ani…     

Synthesis of Novel Ligustrazine Derivatives as Potential Platelet Aggregation Inhibitors

Ligustrazine (lig; tetramethylpyrazine, TMP; Figure 1) is one of major efficient components from Chinese traditional medicine herb Ligusticum Chuanxiong Hort, which is currently widely used in China for the treatment of coronary atherosclerotic cardiovasc…     

Synthesis of Novel Bis(mesocyclic) polyamines

介绍了带羟基桥连双－（中环多胺）的合成。首先利用Ｎ－对甲苯磺酰基－３－羟基－１，５－二氮杂环庚烷与５种双官能基化合物在Ｎ２气氛下于无水乙腈中反应，得到５种带对甲苯磺酰基的中环多胺，然后利用ＨＢｒ／ＨＯＡｃ脱去保护基团，得到桥连双－（中环多胺）的氢溴酸盐。所有新化合物的结构均经ＩＲ、１ＨＮＭＲ、ＭＳ或元素分析证实。     

Synthesis of a Novel Series of S-Alkyl Thiobenzoate Compounds as Farnesyltransferase Inhibitors

S-akyl thiobenzoate compounds were designed as farnesyltransferase (FTase) inhibitors. An effective synthetic method was explored. The structures of the target compounds were elucidated by NMR spectral and elemental analysis.     

Synthesis and Crystal Structure of a Novel Terpyridine-based Cd(Ⅱ) Complex

A novel terpyridine-based complex CdL'S2 (L'= oxide of L; L = 10-hexyl-3-(2,6-di(pyridine-2-yl)pyridine-4-yl)-10H-phenothiazine) has been solvothermally synthesized and characterized by FT-IR spectroscopy, elemental analysis, 1 H NMR and X-ray crystallography. The sulfur of phenothiazine moiety was oxidized when the crystal is formed. The complex C36H37CdN5O2S3 crystallizes in triclinic, space group P1 with a = 9.4452(9), b = 13.0181(14), c = 14.6721(18), α = 73.872(1), β = 81.531(1), γ = 87.547(2)°, V = 1714.2(3)3 , Mr = 780.29, Dc = 1.512 g·cm-3 , μ = 0.861 mm-1 , F(000) = 800, Z = 2, the final R = 0.0456 and wR = 0.1059 for Ⅰ > 2σ(Ⅰ). The Cd(Ⅱ) is coordinated by two terminal sulfur ions and three pyridyl nitrogen atoms in a distorted trigonal bipyramidal geometry. Universal hydrogen bonds between the neighboring molecules have generated a supramolecular arrangement which contributes to the stability of the title complex. Fluorescence property and thermogravimetry of the complex have also been investigated and discussed.     

A Novel Total Synthesis of (±)Shikonin

Shikonin 1 was a key component isolated from the traditional Chinese herbal medicine, Zicao(Lithospermum erythrorhizon Sieb.et Zucc), which possesses multiple biological activities1. There have been many synthetic routes to shikonin, however, all these ro…     

Synthesis and Bioactivity of Novel N,N'-Diacylhydrazine Derivatives Containing Furan (Ⅱ)

Diacylhydrazines have been found as molting hormone analogs since RH‐5849 was reported as the first nonsteroidal ecdysone agonist in 1988. Optimizations on diacylhydrizines with benzoheterocycle containing oxygen were widely explored in recent years. In order to find novel compounds with high bioactivity, a series of mono‐ ( I ) and di‐acylhydrazine ( II ) derivatives containing furan were designed and synthesized. Their structures were confirmed by ¹H NMR, IR, elemental analyses and single crystal X‐ray diffraction analyses ( II ₇). The bioassay results showed that some of the mono‐acylhydrazine ( I ) derivatives exhibited good larvicidal activity against Culex pipiens pallens at 10 mg/L and better than those of di‐acylhydrazines ( II ). Generally, the anti‐tumor activity of di‐acylhydrazines ( II ) was better than that of mono‐acylhydrazines ( I ).     

Synthesis and Characterization of a Novel Liquid Crystalline Chitin — Quaternary Ammonium Chitosan Salt

N-Butyl chitosan(NBCS) derivatives were prepared by introducing butyl groups into the amine groups of chitosan via Schiff base intermediates. The quaternization of NBCS was carried out by using ethyl iodide to produce water-soluble cationic polyelectrolytes. The degree of the substitution of the products was measured by means of the electron spectroscopy for a successful chemical analysis. The quaternary ammonium chitosan salt(QACS) was proved to be a novel cholesteric liquid crystalline chitin, by means of the polarized optical microscopy and the circular dichroism spectropolarimetry. The critical mass fraction of the QACS/formic acid solution forming a lyotropic liquid crystal phase was 50%, which was almost the same as that of the NBCS/formic acid solution, but much hiuher than that of the chitosan in the same solvent.     

Preparation of AChE Inhibitors From Jujubogenin

The advanced medical technology has lengthened the life expectancy of human beings.This makes some previously ignored diseases prominent, such as Alzheimer disease(AD). The low level of acetylcholine (ACh) in brain is considered to be one of mainreasons for suffering such memory loss disease. Thereby, how to elevate ACh level inbrain and enhance the cognition has become a main issue l'2. One of the approaches is toinvestigate acetylcholinesterase (AChE) inhibitors, which can prevent the hy…     

Synthesis of Novel (p‐Substituted Styryl) Spirobenzopyrans

A series of (p‐substituted styryl) spirobenzopyrans were synthesized by the Wittig reaction of Fisher's bases with 5‐(p‐substituted styryl) salicylaldehyde derivatives. The final spirobenzopyrans were characterized by the ¹H NMR, IR, UV, and GC‐MS analyses.     

Synthesis, Crystal Structure and Antimicrobial Activity of a Novel Ni(Ⅱ) Complex

A new nickel(Ⅱ) complex, C34H38N8NiO4, has been prepared and charac-terized by X-ray diffraction analysis. It crystallizes in the monoclinic system, space group P21/c with a = 11.715(5), b = 12.328(5), c =11.113(5) A, β= 92.589(5)°, Z = 2, Dc = 1.411 g/cm3, μ = 0.658 mm-1, the final R = 0.0427 and wR = 0.1099 for 2229 observed reflections with Ⅰ> 2σ(Ⅰ). The complex is a centrosymmetric plane in which nickel(Ⅱ) is coordinated in a regular octahedron to the ligand phenytoin through the nitrogen atoms of ethylenediamine, imine and amine. The complex was valued for its antimicrobial activity against bacterial strands using the agar diffusion method, and found to be active against the four test bacterial organisms. Preliminary screening for antimicrobial activities showed that the title complex is quite active against standard strains of Salmonella species, Staphylococcus aureus, Bacillus pumilus and Eschierichia coli.     

Novel Synthesis of Barbiturates

Knovenagel reaction of barbituric acid with different aldehydes were used to synthesize new barbiturates. This is a novel method which can be used to synthsis various types of new generation of barbiturates which are different from the previously reported.     

Synthesis, Structure and Magnetic Properties of Novel Carboxylato-bridged Pentanuclear Copper(Ⅱ)-Lanthanoid(Ⅲ) Complexes

ＩｎｔｒｏｄｕｃｔｉｏｎＰｏｌｙｎｕｃｌｅａｒｍｉｘｅｄ－ｍｅｔａｌｃｏｍｐｌｅｘｅｓｃｏｎｔａｉｎｉｎｇｂｏｔｈｔｒａｎｓｉｔｉｏｎａｎｄｌａｎｔｈａｎｏｉｄｍｅｔａｌｉｏｎｓａｒｅｏｆｓｐｅｃｉａｌｃｕｒｅｎｔｉｎｔｅｒｅｓｔｉｎｒｅｌａｔｉｏｎ...     

Synthesis and Crystal Structure of a Novel Bis(chlorido)-bridged One-dimensional Chain-like Copper(Ⅱ) Polymer

A copper(Ⅱ) complex [LCu_2Cl_4]n was synthesized by a new bis-Schiff base ligand containing quinoline unit, 1,4-bis[2-(4-fluorophenyl)iminomethyl-8-quinolinoxy]butane(L). X-ray crystal structure shows that it is a binuclear complex, and the crystal belongs to the triclinic system, space group P1, with a = 9.387(2), b = 9.968(2), c = 10.291(2) ?, α = 87.532(3), β = 63.762(2), γ = 86.628(3)o, V = 862.1(3) ?~3, Z = 1, Dc = 1.640 Mg/m~3, F(000) = 428, R = 0.0416 and wR = 0.1141. Each Cu(Ⅱ) metal ion coordinates with a quinoline N atom, an imine N atom, an ether oxygen atom and three chlorides, forming a distorted six-coordinated octahedronal structure. Each copper(Ⅱ) complexation unit links with one of the adjacent ligand copper complexation units through the chlorido bridging groups, thus generating an infinite one-dimensional chain structure. Such 1D chains further construct a 2D network structure by π-π stacking interactions.     

Synthesis,Crystal Structure and Magnetic Property of a Novel Cu(Ⅱ)-Fluconazole-azide Complex

The title compound formulated as Cu2(C13H11N6OF2)(N3)3CH3OH was synthesized and structurally characterized by elemental analysis,IR and single-crystal X-ray diffraction.In the structure of the complex,the deprotonated fluconazole and azide anion link two copper centers to construct a binuclear SBU and the azide anion exhibits a μ1,1-coordination mode.Each triazole group of fluconazole links two SBUs and the compound exhibits a chain-like architecture with strong antiferromagnetism.     

Synthesis of Polymer-Bonded Carbonyl Ruthenium (Ⅱ) and Osmium (Ⅱ) Porphyrins

Studyonmetalloporphyrincomplexesusedasenzymemodelcatalyzingtheoxidationofalkaneandepoxidationofalkeneiscurrentlyaveryactiveresearchfieldl.ThereactivityofrutheniumporphyrincomplexeswasusedasoxidationcatalystsbecausetheirrelationstocytochromeP-450haveb...