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

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 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.

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 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 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.

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 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.