341results about "Esterified saccharide compounds" patented technology

The present disclosure provides linker compounds of Formula (I) or (II):pharmaceutically acceptable salts thereof, and related scaffolds and conjugates. The present disclosure also relates to uses of the linker compounds, scaffolds, and conjugates, e.g., in delivering nucleic acid and / or treating or preventing diseases.

The invention belongs to the technical field of pesticides, and particularly relates to azobenzene calix [4] arene derivatives as well as a preparation method and application thereof. The invention discloses a novel azobenzene calix [4] arene derivative prepared by directional modification through an azo reduction reaction based on a calix [4] arene skeleton. The azobenzene calix [4] arene derivative has the characteristics of green environmental protection, accurate and controllable structure and efficient synthesis. After the derivative and a pesticide form a host-guest compound, the activity of the pesticide can be remarkably improved, the bioavailability of the pesticide at an action site is increased, the problem of low efficiency of the traditional pesticide is effectively solved, and the development of target drug resistance is delayed. The technology breaks through the technical bottleneck of nano-carrier environmental toxicity, provides a new thought for developing a multi-target and low-environmental-risk pesticide synergist, and has important significance for realizing pesticide decrement, synergism and resistance treatment.

To provide a compound and the use thereof for the treatment for regeneration of connective tissue following the degeneration process of articular cartilage due to osteoarthritis, in the case of humans, the degeneration process of articular cartilage caused by excessive stress, for the treatment of skin aging, and for the prevention of skin cancer.SOLUTION: For example, an amino acid derivative of glucosamine having the following structure is provided.SELECTED DRAWING: None

The invention discloses a method for synthesizing a benzodithiepinone derivative through metal-free catalysis, and belongs to the field of organic synthesis. According to the method, benzo disulfonylphenol ketone and alkyne are taken as raw materials, a dual-catalysis system composed of triethylene diamine and bis (diphenylphosphine) methane is adopted, a heating reaction is performed in a 1, 4-dioxane solvent, and the target seven-membered sulfur heterocycle (benzo [e] [1, 4] dithiepin-5-ketone compound) is obtained through separation and purification. According to the method, the problem of regioselective sulfuration of alkyne is effectively solved through a synergistic catalysis mechanism of organic amine and organic phosphine, and high-precision cyclization reaction of benzobissulfonylphenol ketone and alkyne is realized. The process is mild in reaction condition, free of inert gas protection, simple and convenient to operate and good in functional group tolerance, the atom economy can reach 100%, and an efficient and practical synthesis way is provided for construction of the benzo [e] [1, 4] dithiepin-5-ketone compound with a novel structure.

Disclosed are 1,2,4,5-tetraoxane compounds and derivatives thereof having anticancer properties. Disclosed are pharmaceutical compositions and pharmaceutical formulations in unit dosage form suitable for delivering the compounds to a subject in need thereof. In addition to the compounds, the pharmaceutical compositions or formulations can include one or more active agents, such as one or more additional anticancer agents. Also disclosed are methods of treating, mitigating, or treating or ameliorating one or more symptoms associated with cancer in a subject. The methods include (i) administering to a subject in need thereof an effective amount of a compound. The compound can be administered by oral administration, parenteral administration, inhalation, mucosal administration, or a combination thereof. The compound can selectively kill cancer cells and / or cancer stem cells, but not non-cancer cells, by inducing ferroptosis in the cancer cells and / or cancer stem cells.

The invention discloses a method for preparing fructose 1, 6-diphosphate, which comprises the following steps of: inoculating saccharomycetes into a culture medium, reacting by taking glucose as a substrate, and carrying out solid-liquid separation, clear liquid collection, ultrafiltration, permeate collection, nanofiltration, trapped fluid collection and drying on the obtained reaction liquid to obtain the fructose 1, 6-diphosphate, wherein the culture medium contains aldehyde compounds. When the method is used for producing the FDP, the single-batch catalytic yield is increased from 60g / L to 85g / L.

The present invention provides a retinoic acid derivative that has high stability and water solubility. The present invention relates to a carboxylic acid ester compound of trehalose or a derivative thereof and retinoic acid.

The invention relates to the technical field of medical adsorbents for blood perfusion, and discloses an application of a trans-cyclooctene group adsorbent based on a biological orthogonal reaction in preparation of a circulating tumor cell clearing preparation. The adsorbent adopts sephadex microspheres as a carrier, the surface of the carrier is modified with a trans-cyclooctene (TCO) group, a tetrazine (Tz) group is taken in by CTCs through modified mannose, the Tz group is expressed on the surface of a CTCs cell membrane in the form of glycoprotein through a Roseman-Warden pathway in cells, TCO and Tz are subjected to a biological orthogonal reaction specifically, and the adsorption capacity of the adsorbent is improved. The sephadex microsphere adsorbent can effectively enrich and remove CTCs in blood of the whole body of a patient through adsorption, and compared with a conventional single-antibody or multi-antibody capture technology, the sephadex microsphere adsorbent does not depend on antibody-antigen binding, and the capture efficiency of the CTCs can be remarkably improved through a biological orthogonal reaction.

The application discloses an intelligent response type nutrient polymerization slow-release fertilizer and a preparation method thereof, and belongs to the technical field of slow-release fertilizers. The intelligent response type nutrient polymerization slow-release fertilizer of the application solves the problem that the molecular chain length of the nutrient polymerization slow-release fertilizer cannot be controlled by adopting a brominated acetylated substance modified methylene urea technology, and solves the problem that the fertilizer and crop interaction ability is poor by connecting an acid-sensitive substance to a methylene urea fragment with a determined nutrient release period. Organic acid secreted by roots can respond to the nutrient polymerization slow-release fertilizer, so as to promote the release of nutrients, and the nutrient release rate and release amount are positively correlated with the amount of the organic acid secreted by the roots, and the fitting degree with the crop fertilizer requirement law is also higher. Therefore, the nutrient polymerization slow-release fertilizer which can respond to the root nutrient demand signal secretion will be more widely applied to different crops such as wheat, corn, peanut, vegetable and fruit trees, and the application area will be more extensive.

The invention belongs to the technical field of biology, and particularly relates to acetylated raffinose and application thereof. According to the invention, acetylation modification is carried out on raffinose by using an acetylation reagent to obtain acetylated raffinose, the acetylated raffinose can significantly improve the scavenging ability and total antioxidant ability of raffinose on DPPH free radicals, and the scavenging ability on hydroxyl free radicals and the reduction ability on iron ions are also improved to a certain extent. The acetylated raffinose provided by the invention has potential application value in development of functional foods and antioxidants.

The present application relates to a kind of efficient active separation and purification method and purposes of elaeagnus conferta polyphenol, comprising: elaeagnus conferta powder is extracted with ethanol solution, after ultrasonic extraction, centrifugal supernatant is obtained, repeat multiple times after being combined, concentrated by rotary evaporation, and obtain elaeagnus conferta polyphenol concentrated extract;Elaeagnus conferta polyphenol concentrated extract is centrifuged, and the supernatant is used as chromatography sample liquid;Chromatography sample liquid is added to Flash liquid chromatography by liquid sample loading mode, is separated by gradient elution mode to chromatographic column, and each elution component is collected in turn, and concentrated respectively;The concentrated solution of each elution component is added to chromatographic column again to carry out second gradient elution separation, and chromatographic column separation elution is repeated three times, and three kinds of purified elaeagnus conferta polyphenol components are obtained after freeze drying.The present application realizes the high-resolution fractionation elution of polyphenol monomer with high structural similarity by the synergistic regulation of mobile phase polarity gradient and elaeagnus conferta polyphenol molecular hydrophobic interaction.

The application discloses a glucuronolactone and a preparation method thereof, and belongs to the technical field of fine chemical product preparation. The method takes potassium phytate extracted from corn soaking liquid or rice bran acid soaking liquid as raw material, obtains inositol and potassium dihydrogen phosphate after hydrolysis, separates the hydrolysis liquid through chromatography, obtains potassium dihydrogen phosphate by concentrating and crystallizing the salt phase, and the material phase is inositol solution. Enzymatic conversion reaction is carried out by using fermentation to obtain enzyme liquid, glucuronic acid liquid is obtained, glucuronolactone is obtained by concentrating and esterifying, and then the glucuronolactone is obtained by concentrating, refining and crystallizing. In the method, the yield of potassium phytate to inositol is greater than 95%, the molar conversion rate of inositol enzymatic conversion to glucuronic acid is greater than 95%, and the total yield is greater than 89%, which is much higher than the traditional yield, and the content of the obtained glucuronolactone is greater than 99.2%. The glucuronolactone is prepared by enzymatic conversion of the intermediate inositol, the by-product is high-value potassium dihydrogen phosphate, the whole has good economic benefits, and industrial production can be realized.

The current invention concerns methods for the synthesis of 6-azido-6-deoxy-2-N-acetyl-monosaccharide-nucleoside diphosphate, in particular 6-azido-6-deoxy-2-N-acetyl-D-galactosamine-nucleoside diphosphate or 6-azido-6-deoxy-2-N-acetyl-D-glucosamine-nucleoside diphosphate. The synthesis method according to the invention is characterized by being highly efficient and high yielding. Also part of the present invention are key intermediates of this process.

The present application relates to a disaccharide linker, a disaccharide-small molecule drug conjugate and a sugar chain fixed-point antibody-drug conjugate, a preparation method and the use thereof. The structure of the disaccharide linker is as shown in the following formula I. The present invention provides a new-type fixed- point and quantitative antibody-drug conjugate form, and the stability and cytotoxicity of the antibody-drug conjugate are improved.

The invention discloses a chondroitin sulfate oligosaccharide derivative and a preparation method and application thereof.The chondroitin sulfate oligosaccharide derivative is shown in the formula (I), the definition of substituent groups in the formula is shown in the specification, and the derivative comprises di-, tetra-and hexasaccharide derivatives of chondroitin sulfate B and T, has endogenous anticoagulation and anti-inflammatory activity, and can be used for preparing the chondroitin sulfate oligosaccharide derivative. The compound can be developed into anticoagulant and antithrombotic drugs.

[Abstract] [Problem] To provide a method for producing a dealkoxyphenylation product with high yield from a substrate, e.g., a sugar, which is bonded to an alkoxyphenyl group through an oxygen atom. [Solution] A substrate that is bonded to a phenyl group substituted by a C1 to C5 alkoxy group at a para- or ortho-position through an oxygen atom is reacted with a λ3-iodane in a fluorous alcohol and water, whereby a dealkoxyphenylation product can be obtained with high yield under mild conditions.

The invention discloses a bio-based self-photosensitive acrylate monomer, a bio-based light-cured film and a preparation method of the bio-based self-photosensitive acrylate monomer, the structural formula of the bio-based self-photosensitive acrylate monomer is shown in the specification, in the formula, X and Y independently represent residues of a multifunctional acrylate monomer after an acryloyloxy group is removed, and in the formula, X and Y represent residues of the multifunctional acrylate monomer after an acryloyloxy group is removed. N is a positive integer between 1 and 8. A four-stage gem-carbon structure in the bio-based self-photosensitive acrylate monomer has a self-photosensitive function, the use amount of a photoinitiator can be reduced during photocuring, and an obtained photocuring film has relatively good hardness and adhesive force.

The application belongs to the technical field of organic chemical synthesis, and particularly relates to a nitrogen center chiral base derivative, a preparation method and application thereof. The preparation method of the nitrogen center chiral base derivative provided by the application can effectively synthesize a base with only a nitrogen chiral center by using a tetrahydrodibenzo-diazocine compound as a raw material and through chiral phosphoric acid catalyzed amination reaction. Moreover, the synthesis method provided by the application has the advantages of high efficiency, simple steps and strong enantioselectivity, is suitable for industrialized production of chiral bases and derivatives thereof, and provides a new approach for research and application of chiral compounds. Meanwhile, the base derivative prepared by the application is a base molecule with a nitrogen center chirality, and has wide application prospects in the fields of molecular recognition, DNA binding, supramolecular chemistry, material science, asymmetric catalysis and drug development.

Disclosed herein is a modified ribonucleotide comprising a nucleoside comprising 2′-O-acetylated ribose, and polyribonucleotides comprising the same. Also provided herein are compositions comprising a polyribonucleotide of the present disclosure and methods of making and using the same.

The invention discloses a Chinese chestnut thorn bract hydrolyzed tannin product based on a low-water-activity deep eutectic solvent and a steady-state extraction and refining method of the Chinese chestnut thorn bract hydrolyzed tannin product, and belongs to the technical field of green extraction of natural products. The method comprises the following steps: pretreating chestnut thorn bracts by adopting an antioxidant protective agent, and constructing a low water activity system by taking betaine / L-proline-urea / glycerol-beta-cyclodextrin ternary DES as an extraction solvent and optimizing the molar ratio and the water content; after ultrasonic-assisted extraction, high-purity tannin is obtained through AB-8 macroporous resin purification. According to the method, the steric hindrance of beta-cyclodextrin and a hydrogen bond network are utilized to synergistically inhibit tannin hydrolysis, and ultrasonic enhanced mass transfer is combined, so that the tannin extraction rate is increased by 115% compared with that of a traditional water extraction process, hydrolysis byproducts are reduced by 40% or above, and DES can be recycled at least five times. According to the method, resource utilization of the Chinese chestnut thorn bract waste is achieved, and a new scheme is provided for green steady-state production of the hydrolyzed tannin.

To provide a new composition for adjusting a refractive index, which can be suitably used for adjusting the refractive index of various materials, especially resin materials. The present invention also provides a refractive index-adjusting agent containing the refractive index-adjusting composition and a resin composition containing the refractive index-adjusting agent.SOLUTION: The composition for adjusting the refractive index is a composition used for adjusting the refractive index and contains a sucrose naphthoate compound. The refractive index adjusting composition of the present invention contains a trehalose naphthoate compound.SELECTED DRAWING: None

The application relates to the technical field of organic synthesis, and discloses a tyrosine compound olefination reaction method based on ligand promotion. The application successfully modifies tyrosine compounds by using compounds containing ethenyl as terminal groups by taking tyrosine as an embedded guiding group and by optimizing reaction raw materials and reaction conditions, and provides a method for C-H functionalization modification and reaction of polypeptide macromolecules. The reaction provided by the application can be carried out as long as the peptide molecule contains tyrosine, and tyrosine does not need to be used as a terminal residue of the peptide molecule, so that the olefination reaction method provided by the application has a wide application range.

The invention particularly relates to 4 '-thiosugar and a preparation method thereof. The preparation method comprises the following steps: taking D-ribose as a raw material, firstly carrying out methylation protection on C1-site hydroxyl, and then carrying out benzylation protection on other hydroxyl; the preparation method comprises the following steps: firstly, carrying out hydrolysis on a glucosidic bond at a C1 site, carrying out reduction through hydroboron to obtain open-loop ribitol (formula V), carrying out sulfonic acid esterification and bromination substitution on hydroxyl of the ribitol, forming a sulfur bridge bond by taking sodium sulfide as a nucleophilic reagent to obtain benzyl-protected thiosugar, oxidizing a thioether bond into sulfoxide, rearranging to obtain acetoxy thioether, and carrying out debenzylation reaction and hydroxybenzoylation reaction to obtain the high-purity acetoxy thioether. According to the present invention, the multi-step intermediate reaction only needs simple purification, the key intermediate can be obtained through recrystallization, the method is simple, the yield is high, the amplification production is convenient, and the obtained 4 '-thiosugar as the basic sugar can participate in the reaction with a variety of basic groups to form the sulfur-containing nucleoside so as to provide the good foundation for the subsequent drug development or activity screening.

The invention discloses a staurosporine glucoside derivative as well as a preparation method and application thereof, and belongs to the field of medicine synthesis. C3-NHCH3 of staurosporine is subjected to glycosylation modification, and the staurosporine glycoside derivative shown in the formula (I) is prepared. The glycoside derivative prepared by the invention has a better inhibition effect on human acute myeloid leukemia cells THP-1, human bladder cancer cells 5637, human colon cancer cells HCT-116, human pancreatic cancer cells PATU8988T and human liver cancer cells HuH-7, and the compound 5 also has an excellent inhibition effect on human gastric cancer cells MKN-45. A candidate compound is provided for development of drugs for bladder cancer, colon cancer, pancreatic cancer, liver cancer, stomach cancer or acute myeloid leukemia.

The present invention provides fluoroalkoxyalkylenedihydroimidazo[5,1-d]tetradinone compounds and related compounds, pharmaceutical compositions, and their use in the treatment of cancer.

The present invention provides a method of isolating arjunetin from the bark of Terminalia arjuna. The invention provides a simplified, cost-effective method and scalable method for isolation of arjunetin from the Terminalia bark. The present invention encompasses an ethanolic extract of arjunetin that comprises arjunetin with 95% purity. The ethanolic extract of arjunetin is obtained from solvent extraction without using column chromatography. Arjunetin has various therapeutic applications, anti-diabetic, anti-inflammatory, anti-cancer, and anti-viral drugs.

Compositions of de-acylated carbohydrate compounds and methods of making them are provided. The methods can be designed to produce the desired products under conditions of moderate temperature, moderate pH, and without the use of harsh solvents.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to preparation and application of beta-, gamma-or delta-aminoketone derivatives, the structure of the derivatives is shown as a general formula (I), in the formula, R1 is alkyl, aryl and the like; r2 represents an aryl group, a heteroaryl group, an alkynyl group, an alkenyl group, a cyano group or the like; r3 is hydrogen, alkyl, aryl or the like; r4 represents an aryl sulfonyl group, a heteroaryl sulfonyl group, an alkyl sulfonyl group, a sulfonate group or the like; in the structural formula, n represents the length of a carbon chain, and the value is 0-2. The derivative is novel in structure, has good antiviral activity, particularly has a good inhibition effect on H1N1 virus, and has great application potential in the aspect of antiviral effect; meanwhile, the preparation method has the advantages of few reaction steps, no need of metal catalysis, no need of complex substrate preparation, simplicity and safety in operation, mild reaction conditions, low cost, higher atom economy and high yield.