Preparation of Amide-Containing Insecticidal Derivatives from the Renewable Natural Productβ-Pinene

The preparation of bioactive derivatives from the renewable natural product pinene is a hot research topic in the deep processing and utilization of pinene.In this study,β-pinene was used to develop novel molecules as a promising new precursor of insecticide.A series of amide-containing derivatives ofβ-pinene were synthesized and characterized.The insecticidal activities of these derivatives against Mythimna separate and Semiaphis heraclei were tested.The structure characterization results showed that the characterization data of amide-containing derivatives were in full agreement with their proposed structures.The insecticidal activities evaluation results indicated that amide-containing derivatives exhibited weak insecticidal activity against Mythimna separate,but exhibited moderate to good insecticidal activity against Semiaphis heraclei.After testing for 72 h,the corrected mortality against Semiaphis heraclei of compounds 5c,5e,5f,5 h,5j,and 5 m was 100%at 1000 mg/L.The structure-activity relationship analysis results showed that the introduction of an amide group into the structure of derivatives improved their insecticidal activity against Semiaphis heraclei.Meanwhile,the amide-containing derivatives containing the F and NO_(2) substituted benzene ring might improve their insecticidal activity against Semiaphis heraclei.This study will be helpful for the high value-added utilization of the natural renewable resourceβ-pinene and the development of novel insecticides.

Methanolysis of amides under high-temperature and high-pressure conditions with a continuous tubular reactor

The methanolysis of amides,which is widely employed in the synthetic organic chemistry,hardly occurs under mild conditions.To safely and controllably intensify the methanolysis reaction with hightemperature and high-pressure environment,a continuous tubular reaction technology is developed,whose space-time yield is over twice of that of the conventional batch reaction.The methanolysis of acetanilide is selected as the representative reaction,and the influences of temperature,pressure,reactant and catalyst concentration,and residence time on the reaction performances are systematically investigated.Taking the advantages of precise temperature and reaction time control by the tubular reactor,the kinetics of acetanilide methanolysis are determined and compared to the kinetics of acetanilide hydrolysis reaction.The tubular reaction method is also employed to test a variety of other amides to show the effects of substituents,steric hindrance,and alkalinity on the reaction rate of methanolysis.

Three new amide derivatives from the fungus Alternaria brassicicola

Three new amide derivatives(alteralkaloids A-C,1-3)and three known alkaloids(4-6)were afforded after phytochemical investigation of fungus Alternaria brassicicola.The structures of these compounds were confirmed by NMR spectroscopic and HRESIMS data.Furthermore,the absolute configuration of 1 was determined using the single-crystal X-ray diffraction analysis.Compounds 1-3 belong to a class of amide derivatives that have not been found in nature before,sharing the same characteristic signals of the butyl moiety and amide group.These isolated compounds mentioned above were tested for the cytotoxic activity.

Amide proton transfer imaging of Alzheimer's disease and Parkinson's disease

Amide proton transfer (APT) magnetic resonance imaging (MRI) is an important molecularimaging technique at the protein level in tissue. Neurodegenerative diseases have a highlikelihood of causing abnormal protein accumulation in the brain, which can be detectedby APT MRI. This article briefly introduces the principles and image processing technologyof APT MRI, and reviews the current state of research on Alzheimer's disease and Parkinson's disease using this technique. Early applications of this approach in these twoneurodegenerative diseases are encouraging, which also suggests continued technicaldevelopment and larger clinical trials to gauge the value of this technique.

New amide alkaloids from Piper longum fruits

Three new amide alkaloids piperlongumamides A-C(1-3),together with 12 known ones(4-15),were isolated from the fruits of Piper longum.The structures of the new isolates were determined using spectroscopic data analyses.Cytotoxic activity of these amides against HL-60(human leukemia),A-549(human lung cancer),MCF-7(human breast cancer),SMMC-7721(human liver cancer)and SW480(human rectal cancer)cell lines were evaluated.Piperchabamide B(11)exhibited weak inhibitory activity against HL-60(IC_(50)=21.32μM),A-549(IC_(50)=23.82μM)and MCF-7(IC_(50)=16.58μM)cell lines.

Preparation of Hydrogel Based on Acryl Amide and Investigation of Different Factors Affecting Rate and Amount of Absorbed Water

Hydrogel is considered as an important material in our world nowadays as it is used in many important and significant applications such as in tissue engineering and agriculture. There are hundreds of types of such materials, where most of them can be easily prepared. The main objective of this work is to prepare one of the hydrogel types which could be very useful in the agriculture of deserts where plants in dry places require water in order to grow up. There are many places around the world where raining occurs only once or twice a year. There are also places where it does not rain at all. Therefore, hydrogels are required in order to absorb water in large quantities either during raining or irrigation instead of escaping to underground and then eject them to the roots of plants over time as the plants require watering. In this research a hydrogel based on acryl amide, Poly 2-Acrylamide-2-Methyl-1-Propane Sulphonic Acid, (PAMPS) was prepared by using different percentages of a suitable cross-linking agent, Methylene-bis-Acrylamide. The cross-linker content is very important factor affects the rate and amount of absorbed water. The highest amount of absorbed water at 25°C was observed by using 0.6% cross-linking agent based on monomer mass. The temperature of absorbed water and its pH value are also essential factors that affect the rate and the amount of absorbed water and were investigated in this work. The highest amount of absorbed water was recorded at pH = 12 and at 60°C. The amount and the rate of water absorbed by Sodium Polyacrylate Hydrogel were also investigated at 25°C. The agriculture applications of hydrogel based on Sodium Polyacrylate were examined using Fenugreek seeds implanting.

Synthesis and Properties of Thermoplastic Polyisocyanurates:Polyisocyanuratoamide,Polyisocyanurato(Ester-Amide)and Polyisocyanurato(Urea-Ester)

It has been proved that introducing isocyanurate into polymer chains could improve the flame retardancy of polymers.We describe in this work the synthesis and the thermal property study of three thermoplastic polyisocyanurates,which are polyisocyanuratoamide(PICA-6),polyisocyanurato(ester amide)(PICEA-6)and polyisocyanurato(urea ester)(PICUE-6).These polymers show similar and improved thermal stability with the existence of isocyanurate rings.PICA-6 is more crystalizable than the rest two and the melting temperature is found to be around 240℃ but it still crystalizes slowly.For PICEA-6 and PICUE-6,only glass transition can be observed on the DSC traces.The glass transition temperature follows the order of PICA-6>PICEA-6>PICUE-6(101.9,77.9 and 28.7℃,respectively).

In situ Detection of Amide A Bands of Proteins in Water by Raman Ratio Spectrum

The amide A band of protein is sensitive to the hydrogen bands of amide groups of proteins. However, it is hard to distinguish the amide A band of aqueous protein in situ directly, since it overlaps with O-H stretching vibration of water. In this work, we presented a new analytical method of Raman ratio spectrum, which can extract the amide A band of proteins in water. To obtain the Raman ratio spectrum, the Raman spectrum of aqueous protein was divided by that of pure water. A mathematical simulation was employed to examine whether Raman ratio spectrum is effective. Two kinds of protein, lysozyme and （^-chymotrypsin were employed. The amide A bands of them in water were extracted from Raman ratio spectra. Additionally, the process of thermal denaturation of lysozyme was detected from Raman ratio spectrum. These results demonstrated the Raman ratio spectra could be employed to study the amide A modes of proteins in water.

Research Status of Amide Herbicides and Their Safeners

The widespread use of chemical herbicides especially amide herbicides has promoted the innovation of chemical weeding in farmland, but amide herbicides have brought invisible chemical injuries to crops in addition to weeding. Herbi-cidesafeners should be applied at the same time with herbicides to ensure herbi- cides will not injure crops while controlling weeds. The research and application of safeners is of great significance to resolving or alleviating the negative effects of herbicides on crop growth. The overview, mechanism, applied research progress and existing problems of amide herbicides and their safenars are summarized.

L-theanine: A potential multifaceted natural bioactive amide as health supplement

Natural bioactive compounds from plants are of great importance in modern therapeutics,which are used to prepare antibiotics, growth supplements or some other therapeutics. Ltheanine is such a bioactive amide amino acid presented in different plants and fungi,especially in tea. Theanine has influential effects on lifestyle associated diseases, such as diabetes, cardiovascular disorders, hypertension, stress relief, tumor suppression,menstruation and liver injury. This amino acid can maintain normal sleep and improve memory function and nullify effect of the neurotoxins. The rate of bioavailability and its medium of ingestion in the body is one of the great concerns for its additional antioxidant properties. Pharmacokinetics of the bioactive compound and its mode of action are described herewith. The biosynthesis and industrial synthesis are also reviewed to promote accelerated production of this bioactive compound in the pharmaceutical industries.

Synthesis of 2, 6-(substituded)pyridine Derivatives Using Amide and Imine Groups

A new wo-armed?acyclic diamide Ia 2, 6-bis(1-ethanecarbozamido-2-amino)pyridine, and a new series of aromatic aldehyde schiff bases containing pyridine ring and amide bridge, IIa-f, were prepared. The compounds were characterized by elemental analysis, IR, 1HNMR and MS. The bioactivity half inhibitory concentration C1/2 is given.

Synthesis and Anti-tumor Activity of Novel Amide Derivatives of Ursolic Acid

Ursolic acid was modified at C3 and C28 position to obtain fourteen derivatives including twelve novel compounds, and their chemical structures were characterized by IR, ^1H NMR and MS. Cell growth inhibitory effects of the derivatives against Hela cell were evaluated by MTT assay. All these derivatives were found to have stronger cell growth inhibitory than their parent compound, ursolic acid. The derivatives with a substituted acetyl group at C3 hydroxyl group show better activities than those with an unsubstituted hydroxyl group.

Measurement and Correlation for Solubility of （S）-（＋）-2,2-Dimethylcyclopropane Carbox Amide in Different Solvents

（S）-（＋）-2,2-dimethylcyclopropane carbox amide is a key intermediate of Cilastatin, an inhibitor of dehydropeptidase-I. Its corresponding solid-liquid equilibrium data will provide essential support for industrial design and further theoretical studies. The solubilities of （S）-（＋）-2,2-dimethylcyclopropane carbox amide in toluene, dichloromethane, trichloromethane, ethyl acetate, ethanol and pure water at different temperature were measured using the synthetic method by a laser monitoring observation technique. The solubility data were correlated with the modified Apelblat equation.The calculated values were good in agreement with the experimental values.

Amide Ionic Liquids(AILs)/L-Proline Synergistic Catalyzed Asymmetric Mannich Reactions

Amide ionic liquids （MLs）/L-proline synergistic catalyzed Mannich reactions of isovaleraldehyde, methyl ketones, and aromatic amines were carried out in moderate to high yields （ up to 96% ） and high stereo selectivities （ 〉99% e. e. ）. The products were easily isolated by extraction; and the catalyst system was readily recycled at least thrice without significant loss of efficiency. The scope of the substrates was studied and the interpretation of the manifest improvement of the reaction rates and enantio-selectivity of the novel catalyst system was speculated.

Measurement and Correlation for Solubility of (S)-(+)-2,2-Dimethyl-cyclopropane Carbox Amide in Different Solvents

(S)-(+)-2,2-dimethylcyclopropane carbox amide is a key intermediate of Cilastatin, an inhibitor of de- hydropeptidase-I. Its corresponding solid-liquid equilibrium data will provide essential support for industrial design and further theoretical studies. The solubilities of (S)-(+)-2,2-dimethylcyclopropane carbox amide in toluene, di- chloromethane, trichloromethane, ethyl acetate, ethanol and pure water at different temperature were measured us- ing the synthetic method by a laser monitoring observation technique. The solubility data were correlated with the modified Apelblat equation. The calculated values were good in agreement with the experimental values.

Synthesis of Novel Poly(aryl ether amide)s Containing the Phthalazinone Moiety

Two novel heterocyclic diamine monomers: 1,2-dihydro-2-(4-aminophenyl)-4-[4-(4-aminophenoxy)phenyl] (2H)phthalazin-1-one and 1,2-dihydro-2-(4-aminophenyl)-4-[4-(4-aminophenoxy)-3,5-dimethylphenyl](2H)phthalazin-1-one were successfully synthesized from readily available heterocyclic bisphenol-like monomers in two steps in high yield. A series of novel poly(aryl ether amide)s containing the phthalazinone moiety were successfully prepared by the direct polymerization of the novel diamines and aromatic dicarboxylic acids using triphenyl phosphite and pyridine as condensing agents.

The Anticancer Activities Phenolic Amides from the Stem of Lycium barbarum

Four new phenolic amides,4-O-methylgrossamide(1),(E)-2-(4,5-dihydroxy-2-{3-[(4-hydrox-yphenethyl)amino]-3-oxopropyl}-phenyl)-3-(4-hydroxy-3-methoxyphenyl)-N-(4-hydroxyphenethyl)acryl-amide(2),(Z)-lyciumamide C(3),(Z)-thoreliamide B(4),together with thirteen known phenolic amides were identified from the stem of Lycium barbarum.The structures of the new compounds were determined by spectroscopic methods.All compounds were evaluated for their anti-cancer activities against human glioma stem cell lines.

Synthesis and Properties of Gemini Cationic Surfactants with Amide Spacers

Four gemini cationic surfactants {N,N′-di[2-(lauryldimethylamino)acetyl]polymethylenediamine dichloride, LAA-s-LAA, s=2,3,4,6} were synthesized by using four bis(α-chloroacetamide)s and N,N-dimethyllaurylamine, respectively. The molecular structures were characterized by means of IR, ~ 1H NMR, \{~ ~13 C NMR\} and MS, and the behavior of their aqueous solutions was studied. The critical micell concentrations(CMC) of LAA-s-LAA were one order of magnitude lower than that of dodecyltrimethyl ammonium chloride(DTAC). With the change of the length of spacer chain(s), their CMC values change, and CMC reaches the top value at s=4.

Synthesis of Eu(Ⅲ) and Tb(Ⅲ) Complexes with New Aryl Amide Type Tetrapodal Ligand and Their Luminescence Properties

A new aryl amide type tetrapodal ligand L (1, 1, 1, 1 tetrakis-{[(2 benzylaminoformyl) phenoxyl]methyl}methane) and its europium and terbium nitrate complexes were synthesized. The luminescence properties of these complexes were also studied.

Reinvestigation on the Reaction of Salicylic Chloride with Salicylic Amide and X-ray Crystal Structure of a New Macrocyclic Polyester

The reaction of salicylic chloride and salicylic amide at 170 ℃ gave benzoxazine and a new macrocyclic polyester 3, whose crystal structure has been determined by single-crystal X-ray diffraction analysis. Compound 3: C28H16O8, Mr = 480.41, monoclinic, space group P21/n, a = 15.353(3), b = 14.196(3), c = 21.147(4) ? b = 103.32(3), V = 4485(2) ?, Z = 8, F(000) = 1984, Dc = 1.423 g/cm3 and m = 0.106 mm-1. The final R = 0.0535 and wR = 0.1275 for 7903 observed reflections (I ≥ 2(I)). In the asymmetric unit of the compound there exist two independent molecules which are connected by weak aromatic CH…O hydrogen bonding between C(47)?H(47) and atom O(7) of the carbonyl group.