69results about How to "Easy to derivatize" patented technology

A barrier film composition can comprise a thermoplastic web comprising a thermoplastic polymer and a dispersed cyclodextrin composition having substituents that compatibilize the cyclodextrin in the film. The thermoplastic / cyclodextrin film obtains substantial barrier properties from the interaction between the substituted cyclodextrin in the film material with a permeant. The substituents on the cyclodextrin molecule causes the cyclodextrin to be dispersible and stable in the film material resulting in an extrudable thermoplastic. Such materials can be used as a single layer film material, a multilayer film material which can be coated or uncoated and can be used in structural materials wherein the thermoplastic is of substantial thickness resulting in structural stiffness. The cooperation between the cyclodextrin and the thermoplastic polymer provides barrier properties to a web wherein a permeant can be complexed or entrapped by the cyclodextrin compound and held within the film preventing the permeant from passing through the film into the interior of a film, an enclosure or container. The permeant can comprise a variety of well known materials such as moisture, aliphatic or aromatic hydrocarbons, monomer materials, off flavors, toxic compounds etc.

Polymer surfaces coated with organometallic layers, wherein the organometallic layers and polymer surfaces have functional groups that react to bond the organometallic layer to the polymer surface with organometallic functional groups remaining unreacted for the subsequent covalent attachment of organic overlayers. Coating methods and coated articles are also disclosed.

The invention provides sulfamate serving as an indoleamine-2, 3-dioxygenase inhibitor and a preparation method and application thereof. The structure of the inhibitor is shown in the general formula I, wherein definitions of X, R1, R2, R3, R4, R5 and n are shown in the description and the claim. The invention further discloses the preparation method of the inhibitor. The compound shown in the general formula I can serve as the indoleamine-2, 3-dioxygenase inhibitor and is used for preparing medicine for preventing and / or treating indoleamine-2, 3-dioxygenase mediated diseases. The general formula I is shown in the description.

The present disclosure relates to the use of a nitroaniline derivative of Formula (I) for the production of nitric oxide and for the preparation of a medicament for the treatment of a disease wherein the administration of nitric oxide is beneficial. The present disclosure furthermore relates to a method for the production of NO irradiating a nitroaniline derivative of Formula (I), a kit comprising a nitroaniline derivative of Formula (I) and a carrier and to a system comprising a source of radiations and a container associated to a nitroaniline derivative of Formula (I). In Formula (I), R and RI are each independently hydrogen or a C1-C3 alkyl group; RII is hydrogen or an alkyl group.

The invention discloses an indoleamine-2,3-dioxygenase inhibitor containing sulfoximine subjected to nitrogen alkylation and arylation and a preparation method thereof. The inhibitor disclosed by the invention has a structure shown in a general formula (I), wherein the definitions of X, R1, R2, R3, R4, R7, R8, R9, n and m are shown in a description and claims. The invention also discloses a preparation method of the inhibitor. According to the indoleamine-2,3-dioxygenase inhibitor disclosed by the invention, a compound shown in the general formula (I) can be used as the indoleamine-2,3-dioxygenase inhibitor and can be used for preparing medicines for preventing and / or treating indoleamine-2,3-dioxygenase-mediated diseases. The formula (1) is shown in the description.

The invention discloses chiral organic dye molecules having circularly polarized luminescence properties as well as a preparation method and an application of the chiral organic dye molecules. The chiral organic dye molecules have structural formulas shown in the formula I1 and the formula I2. Chiral organic dyes shown in the formula I1 and the formula I2 can be used for preparing chiral organic luminescent materials, and the organic luminescent materials have multi-color circularly polarized luminescence properties. According to the method for preparing the chiral organic dyes having the multi-color circularly polarized luminescence properties, raw materials are cheap, the synthesis method is simple, the yield of products is high, and the organic dyes have the characteristic of easiness in derivatization, are good in stability and have the bright application prospect in the field of chiral photoelectric materials.

Polymer surfaces coated with organometallic layers, wherein the organometallic layers and polymer surfaces have functional groups that react to bond the organometallic layer to the polymer surface with organometallic functional groups remaining unreacted for the subsequent covalent attachment of organic overlayers. Coating methods and coated articles are also disclosed.

The invention discloses a mogrol derivative monomer as well as a preparation method and application thereof, and belongs to the technical field of structural modification of plant active ingredients. The mogrol derivative monomer is a compound shown as a formula 2, and the invention also discloses a preparation method and application of the mogrol derivative monomer. According to the mogrol derivative monomer disclosed by the invention, the C-24 site of mogrol is selectively derived into a single carboxyl group on the premise of keeping chirality of each site on a tetracyclic parent nucleus of mogrol and not changing a functional group, and the high reaction activity of the carboxyl group is convenient for further derivatization.

Novel pyridinones and their derivatives which are effective in treating or preventing Gram-negative bacterial infections are provided. The pyridinones are stable and easily derivatized; the methods by which these derivatizations occur is described. Two regioselective and functional group tolerant methods for the synthesis of the novel pyridinones are also provided. One such synthetic method involves reacting an imine and a Meldrum's acid derivative in solution. The other synthetic method is a solid phase synthesis of the pyridinones in which an imine is prepared bound to a solid support and a Meldrum's acid derivative is reacted with the imine. Novel imine intermediates useful in the solid phase and solution methods of synthesizing the pyridionones are also described.

The invention relates to a vanadium coordination compound using aminotriacetic acid derivative as a ligand, and a preparation method and application thereof. The preparation method comprises the following steps: 1. reacting aminotriacetic acid in anhydrous pyridine to obtain a compound 1; 2. reacting the compound 1 with aminophenol or hydroxyaniline to obtain a compound A; 3. dissolving vanadyl sulfate in water, and regulating the pH value with NaOH to obtain a compound 2; and 4. dissolving the compound A in water, and reacting with the compound 2 to obtain a compound B. The compound is used in preparing antidiabetic drugs. The animal experiment proves that compared with the vanadyl compound using kojic acid as the ligand, the vanadyl coordination compound using aminotriacetic acid as the ligand has the advantages of lower molecular weight, higher water solubility, higher bioavailability and simpler preparation method.

Provided is an organosilane compound expressed by the following general formula (1):where: Ar represents a divalent aromatic organic group, such as a phenylene group; R1 represents a hydrogen atom or the like; R2 to R6, which may be the same or different from each other, each represent a hydrogen atom or the like; and X represents a reactive substituent, such as a halogen atom.

The invention discloses difluoroethyl-containing nitrosamine compounds and a preparation method thereof. A series of difluoroethyl-containing nitrosamine derivatives are obtained by taking carboxylicacid as a catalyst and carrying out an aza-Michael addition / nitrosation tandem reaction on three components, i.e., difluoroethylamine, tert-butyl nitrite and 1-aryl 2-nitroethylene at room temperaturein absence of other organic solvents. Molecular skeletons of the compounds contain potentially bioactive difluoroethyl and nitrosamine groups, thus establishing a material basis for drug discovery and druggability evaluation, and having an important application value. The preparation method provided by the invention adopts the easy-to-obtain raw materials, does not need an additional organic solvent, and has the advantages of mild reaction conditions, simple operation, high yield and good substrate universality.

The present invention relates to a polymerization-curable composition for the preparation of biodegradable, biocompatible, cross-linked polymers on the basis of polyvinyl alcohol comprising: 5 to 100% by weight of (a) vinyl ester monomer(s) of one of the general formulas (I) to (III):wherein X is oxygen, sulfur, nitrogen, or phosphorus; n is 1 to 1000, at least 20% of the n being ≧2; the R1 are selected from hydrogen; straight, branched or cyclic, saturated or unsaturated, n-valent hydrocarbon groups having 1 to 30 carbon atoms, which optionally have heteroatoms and are optionally substituted with one or more substituents selected from —OH, —COON, —CN, —CHO, and ═O, and n-valent radicals of biodegradable, biocompatible oligomers and polymers; m is an integer from 1 to 5; the R2 are selected from hydrogen, —OH, ═O, and the options listed for R1; and the R3 are selected from hydrogen, —OH, and the options listed for R1; 0 to 50% by weight of ethylenically unsaturated co-monomers; 0 to 10% by weight of (a) polymerization initiator(s); and 0 to 95% by weight of solvent(s).

The invention discloses a terphenyl macrocyclic compound based on biphenyl aromatic hydrocarbon and a preparation method of the terphenyl macrocyclic compound. The preparation method comprises the steps: firstly, preparing 2,2', 4,4',6,6'-hexamethoxy terphenyl or 2,2',3,3'-tetramethoxy terphenyl as a monomer through suzuki coupling reaction, then adding paraformaldehyde and 1,2-dichloroethane into the monomer, and under the catalysis of lewis acid boron trifluoride diethyl etherate, obtaining 2,2',4,4',6,6'-hexamethoxy terphenyl arene macrocycles and 2,2',3,3'-tetramethoxy terphenyl arene macrocycles with high yield by a one-pot method. The raw materials are easy to obtain, the reaction is efficient, the one-pot synthesis is simple and convenient, the yield is high, and more methoxy side chains are provided for further modification. The similar macrocycles show great scientific research value in the field of adsorption separation materials, so that there are reasons to believe that the method has a wide application prospect in the fields of materials, environment, biology and the like.

The invention discloses a method for synthesizing amino-modified NIT nitroxide free radicals. The method comprises the following steps: by taking N-(2-glyoxyl) phthalimide and N,N'-dyhydroxyl-2,3-dimethyl-2,3-butanediamine as raw materials, performing three steps such as condensation, hydrazinolysis and oxidization to obtain the amino-modified NIT nitroxide free radicals. The amino-modified NIT nitroxide free radicals have wide reaction and application values, and the yield is 60 percent or higher.

The invention belongs to the field of pharmaceutical chemistry and relates to a novel phosphoinositide 3-kinase inhibitor, a preparation method and an application thereof. Specifically, the present invention provides a compound having the structure of formula I, which can be used as an efficient PI3K inhibitor and has various pharmacological activities such as tumor resistance, resistance to neurodegenerative diseases (such as Alzheimer's disease), inflammatory resistance, etc.

The invention belongs to the field of chromatographic analysis, and particularly relates to a calixarene derivative stationary phase, a capillary gas chromatography column, and a preparation and application of the calixarene derivative stationary phase. According to the calixarene derivative stationary phase, the capillary gas chromatography column, and the preparation and application of the calixarene derivative stationary phase, p-tert-butylphenol is taken as a raw material, an intermediate I is firstly formed through cyclization reaction, an intermediate II is then obtained through reactionof the intermediate I, and the intermediate II is finally nitrated to prepare calixarene derivatives (C4A-NO2), the prepared C4A-NO2 as the stationary phase of the capillary gas chromatography columncan enable the particle size distribution to be uniform, special large holes and rich functional groups are achieved, polar nitro functional groups are arranged at the upper edge of an aromatic ringof the prepared C4A-NO2, and non-polar long alkoxy functional groups are arranged at the lower edge of the aromatic ring of the prepared C4A-NO2. The problems of poor solubility of an existing calixarene derivative and low column efficiency of the prepared chromatographic column are solved, the solubility and film forming property of the calixarene derivative are improved, the chromatographic selectivity of the calixarene derivative is enriched, and the preparation method has the advantages of simplicity, easy availability, low cost and good separation effect.

The present invention discloses an efficient IDO / TDO double inhibitor containing a nitrogen heterocyclic helix structure, and in particular, relates to a compound of formula (I) or pharmaceutically acceptable salt, stereoisomers, or tautomers, or prodrugs thereof. The compound of the formula (I) can be used as an indoleamine-2,3-dioxygenase inhibitor and tryptophan-2,3-dioxygenase for preparationof drugs for prevention and / or treatment of indoleamine-2,3-dioxygenase and tryptophan-2,3-dioxygenase-mediated diseases.

The preparation method comprises the following steps: adding one of trifluoroacetic anhydride, difluoroacetic anhydride and oxalyl chloride monoester and dimethylaminopyridine into a solvent, or jointly adding one of trifluoroacetic anhydride, difluoroacetic anhydride and oxalyl chloride monoester, dimethylaminopyridine and sodium hydrocarbon acid into the solvent, and stirring the solution to obtain the polysubstituted isothiazole derivative; then performing stirring reaction with a compound 1 at 0 DEG C for 10-20 minutes, heating the mixture to 25-50 DEG C, and performing stirring reaction to generate a compound 2. The method provided by the invention has the advantages of short steps, mild conditions, low cost and wide universality, does not need to use high-toxicity reagents and rare and noble metal reagents, and is suitable for industrial production.

The invention discloses a method for synthesizing (3,5-bistrifluoromethylpyrazolyl)pyridine derivatives with potential bioactivity. The method comprises the following step: under heating conditions, carrying out substitution / cyclization / dehydration reaction on the raw material 2-bromopyridine derivatives with hydrazine hydrate and hexafluoroacetylacetone to synthesize the (3,5-bistrifluoromethylpyrazolyl)pyridine. Compared with the reported synthesis methods, the method disclosed by the invention has the advantages of accessible raw material, high synthesis efficiency, easy derivation of the product and the like.

Disclosed in the present invention are an indoleamine-2,3-dioxygenase inhibitor and a preparation method therefor. The structure of the inhibitor of the present invention is shown in general formula (I), wherein the definitions of X, R1, R2, R3, R4, R7, R8, R9, n and m are as shown in the description and the claims. Also disclosed in the present invention is a preparation method for the inhibitor. The compound in general formula (I) of the present invention can be used as an indoleamine-2,3-dioxygenase inhibitor for the preparation of a drug for preventing and / or treating diseases mediated by indoleamine-2,3-dioxygenase.

The invention discloses a blue fluorescence chiral organic dye molecule as well as a preparation method and the application of the blue fluorescence chiral organic dye molecule. The chiral organic dye molecule comprises a left-handed (M) screw type optical activity enantiomer and a right-handed (P) screw type optical activity enantiomer, the structural formulas of the left-handed (M) screw type optical activity enantiomer and the right-handed (P) screw type optical activity enantiomer are shown in the formulas (M)-1 and (P)-1, Ar in the formula (M)-1 or (P)-1 is chosen from a phenyl group or a replaced phenyl group, and the replaced phenyl group is chosen from at least one of 4-methylphenyl, 4-methoxy phenyl, 4-fluoro-phenyl, and 4-cyano-phenyl. The chiral organic dye molecule forms a twisting structure in a way that an aromatic diester attracting an electron and a dinaphthalene derivative are connected by a 6-membered ring through methylene, moreover, the chiral organic dye molecule also has a certain spiroconjugated compound; after the extra aromatic substituent group is introduced, the fluorescence emission is promoted, the structure is more twisted, then the excitation wavelength and the emission wavelength are relatively short, taking Ar serving as the phenyl group for an example, the excitation wavelength in the tetrahydrofuran is 344 nm, the emission wavelength is 439 nm, and the Ar shows approximately pure blue color in a solution.

The invention discloses an N-methoxyl formamide-orientated method for synthesizing a ferrocene and pyridone derivative. According to the method, under the conditions that palladium acetate is taken as a catalyst, copper acetate is taken as a catalyst promoter and quaternary ammonium salt and alkali are taken as additives, an N-methoxyl ferrocene and [c] pyridine-2(1H)-ketone derivative is obtained by carrying out a cyclization reaction on N-methoxyl ferrocene formamide and alkyne. The method adopts an N-methoxyl formamide-orientated carbon-hydrogen bond and nitrogen-hydrogen bond double-activation reaction to synthesize the N-methoxyl ferrocene and [c] pyridine-2(1H)-ketone derivative in one step. The organometallic condensed heterocyclic compounds are unique in structure, thus being hard to prepare by a conventional method; the method provided by the invention has the characteristics of being easy in obtaining of raw materials and mild in reaction conditions, not needing the protection of inert gas, being high in synthetic yield, and the like; therefore, a new way is provided for the synthesis of novel ferrocene and heterocyclic compounds, and the method has an important significance for expanding the application of the compounds in the fields such as medicinal chemistry, material chemistry, catalysts and the like.

The invention belongs to the technical field of medical biomaterials and discloses an antibacterial polypyrrole / sulfosalicylic acid nanorod and a preparation method and application thereof. The methodcomprises that through a three-electrode system with a metal material as a working electrode, a mixed solution of a pyrrole monomer and sulfosalicylic acid as an electrolyte solution undergo a polymerization reaction on the surface of the working electrode through an electrochemical constant current method to produce a polypyrrole / sulfosalicylic acid nanorod, wherein the mixed solution of a pyrrole monomer and sulfosalicylic acid is obtained by dissolving a pyrrole monomer and sulfosalicylic acid in a phosphate buffer solution. The polypyrrole / sulfosalicylic acid nanorod is produced on the surface of the working electrode so that surface biological activity and antibacterial performances are improved. The preparation method has simple processes and a stable structure and has a potential application value in the field of the biological material.

Disclosed in the present invention are an indoleamine-2,3-dioxygenase inhibitor and a preparation method therefor. The inhibitor of the present invention has a structure as represented by general formula (I), wherein the definitions of Ar, E, Y, X, V, D, W, B, ring A and ring B are as shown in the description and claims. Also disclosed in the present invention is a preparation method for the inhibitor. The compound of general formula (I) of the present invention can be used as an indoleamine-2,3-dioxygenase inhibitor for preparing a medicament for preventing and / or treating indoleamine-2,3-dioxygenase-mediated diseases.