99results about "Aminosugars" patented technology

The invention relates to polystyrene cation exchange resin as well as a preparation method and application thereof. The preparation method comprises the following steps: dissolving a dispersing agent in a solvent to obtain a dispersed phase for suspension polymerization reaction, uniformly mixing a reaction monomer, a cross-linking agent, a pore-foaming agent and an initiator, and carrying out suspension polymerization reaction under segmented stirring and segmented temperature change to prepare copolymer microspheres; and putting the dried microspheres into a reaction kettle, swelling, carrying out sulfonation reaction through a variable temperature program on the basis to obtain sulfonated microspheres, and carrying out alkali exchange reaction on the sulfonated microspheres to obtain the final product cation exchange resin. Compared with the prior art, the cation exchange resin preparation method provided by the invention has the characteristics of simple and feasible process, easiness in large-scale production, low cost, high specific surface area, high adsorption capacity and high separation efficiency, and is especially suitable for separating and purifying substances containing amino groups or aminoglycosidic bonds.

Compounds and compositions that have an asialoglycoprotein receptor (ASGPR) binding ligand bound to an extracellular protein binding ligand for the selective degradation of the target extracellular protein in vivo to treat disorders mediated by the extracellular protein are described.

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.

The invention relates to the technical field of medicinal chemistry, and provides a TLR4 agonist, application thereof and a vaccine composition. The TLR4 agonist is a compound with a structure as shown in a formula 1 or a pharmaceutically acceptable salt thereof, the compound is glucosamine aminoalkyl 4-phosphate series molecules derived from MPL-12 structure modification, and the series molecules have enhanced immunostimulatory activity and selective immune response induction capability.

The application belongs to the technical field of biological medicine, and particularly relates to a galactosamine-doxetaxel conjugate as well as a preparation method and application thereof. First, doxetaxel and 3,3'-diseleno-dipropionic acid are used as raw materials, and after heating reaction, 3,3'-diseleno-dipropionic acid doxetaxel is obtained. Then, the obtained 3,3'-diseleno-dipropionic acid doxetaxel and galactosamine are used as raw materials, and after heating reaction, galactosamine-3,3'-diseleno-dipropionic acid doxetaxel conjugate is obtained through column chromatography separation and purification. The obtained conjugate can be specifically recognized by endogenous lectin receptors (such as asialoglycoprotein receptor ASGPR) which are highly expressed on the surface of hepatoma cells, so as to be taken up by hepatoma cells through a receptor-mediated pathway, and has application prospect in the direction of hepatoma targeted treatment.

The invention relates to a novel chemical cross-linking agent with mass spectrum fragmentable trehalose disaccharide as a skeleton structure and a preparation method thereof. The cross-linking agent disclosed by the invention has the following characteristics: 1) trehalose disaccharide is used as a skeleton structure, so that the cross-linking agent has excellent biocompatibility; 2) the trehalose skeleton has a pair of symmetrical mass spectrum fragmentable glucosidic bonds, so that a cross-linked peptide fragment can be simplified into a conventional peptide fragment modified by a cross-linking agent fragment; 3) the enrichment of the cross-linked peptide fragment can be realized by the trehalose skeleton under the condition of not adding an enrichment handle; and 4) active groups of the cross-linking agent comprise but not limited to a plurality of reactive groups such as succinamide ester, diaziridine, phenylsulfonyl fluoride, hydrazide group, amino group, hydroxylamine group and the like, and chemical cross-linking of a plurality of amino acids except lysine is realized. The trehalose cross-linking agent disclosed by the invention is applied to the field of proteomics, and provides technical support for realizing large-scale analysis of a protein complex in a complex sample, spatial structure analysis of protein and a protein-protein interaction network.

The invention discloses a partial acylated non-natural sugar for metabolic labeling and application, the partial acylated non-natural sugar is a mannose type of a pyranose structure, and 1-hydroxyl and 6-hydroxyl are protected by hydrophobic groups. According to the method, the advantages of existing non-natural sugar are taken into consideration, it is guaranteed that the non-natural sugar can be efficiently utilized by cells, S side reaction of the non-natural sugar and cysteine in protein in the metabolism process is effectively avoided, and meanwhile efficient metabolism marking is achieved. In a cell test, the use concentration of the 1, 6-diacylated non-natural sugar is one order of magnitude lower than that of the non-natural sugar without the protecting group.

The application discloses an enzyme method for synthesizing unnatural sugar and application thereof, and belongs to the technical field of organic chemical synthesis. The unnatural sugar comprises an unnatural sugar obtained by introducing an acyl group into a hydroxyl group at the 6th position of a bare sugar through an acylation reaction; and the bare sugar is obtained by performing derivatization modification on an amide site of a natural sugar. The synthesis method uses a SubC enzyme as a catalyst to realize selective acylation of the hydroxyl group at the 6th position of the bare sugar, and synthesizes the unnatural sugar with an ideal yield. The unnatural sugar can be applied to glycomics metabolic labeling and mass spectrometry analysis as a marker, has excellent biological safety, specificity and labeling efficiency, can avoid non-specific labeling, and has no obvious cytotoxicity.

The invention relates to the technical field of novel drug application of compounds, in particular to a compound Man-Tz, a biological orthogonal reaction system and application of the compound Man-Tz. The dTRIM24 is accurately released at the atherosclerotic plaque through a biological orthogonal targeting technology, and the problem of non-specific distribution caused by a traditional administration mode is effectively solved by utilizing the specific reaction of an artificial target point Man-Tz and TCO-dTRIM24-TCO. According to the technology, the TRIM24 protein of 117kDa can be specifically degraded, and macrophages are promoted to be polarized to an anti-inflammatory M2 type by inhibiting Stat6 acetylation, so that plaque formation is inhibited. Experiments prove that the system has concentration and time-dependent effects, drug exposure of non-target tissues is remarkably reduced while efficient degradation activity is maintained, and a novel targeted therapy strategy with high specificity and low toxic and side effects is provided for atherosclerosis treatment.

The present application relates to the crystal form I and crystal form II of compound N-butyryl-glucosamine and the preparation method and purposes thereof, wherein the crystal form I and crystal form II obtained by the present application have good water solubility, crystal form stability, and can be better used in pharmacy.

The activated carbon decolorizing device comprises a kettle body, a kettle cover, a driving motor, a stirring shaft and a stirring paddle, a feeding opening is formed in the kettle cover, a feeding opening cover is installed at the feeding opening, a feeding pipe is fixedly connected to the feeding opening, an end flange is arranged at the feeding pipe, the end flange is provided with a first protrusion, and the first protrusion is provided with a second protrusion. The feeding port cover is provided with a second protrusion, a limiting shaft is installed between the first protrusion and the second protrusion, and the feeding port cover is detachably and fixedly connected with the end flange. According to the decolorizing device, the feeding opening cover can be rotated in a rotating mode, and the two handles are located on the same side, so that the decolorizing device is convenient to operate by two hands, and the feeding opening cover is more convenient to open. And when the feeding port cover is opened for feeding, the inserting plate can support the feeding port cover, so that the position of the feeding port cover is stable during feeding. When the feeding opening cover is closed, the rotating block is fixed to the U-shaped fixing frame, and therefore the situation that other operations are affected due to the fact that the rotating block and the inserting plate are high when erected is avoided.

Methods for chemically modifying bioactive triterpene compounds to increase the bioavailability thereof. The resulting triterpene chemical compounds, having enhanced bioavailability, are useful in pharmaceutical compositions, alone, in combination with, or complexed with therapeutic drugs for the treatment of diseases such as cancers.

The application discloses an enzyme method for producing glucosamine salt and a purification method thereof, and belongs to the technical field of bioengineering. The application takes N-acetyl glucosamine as raw material, obtains glucosamine and acetic acid through deacetylase hydrolysis, separates the glucosamine salt through an acid solution elution cation exchange column, and recovers byproduct sodium acetate through anion exchange. The obtained glucosamine salt is concentrated, crystallized, decolorized and dried to obtain high-purity glucosamine salt crystals. The application combines the enzyme recycling process, residual substrate recycling process and acetic acid recovery process, improves the conversion rate of N-acetyl glucosamine and the total yield of the glucosamine salt product, recycles the enzyme, fully converts the residual substrate, recycles the acetic acid, and through normal-temperature operation conditions, the resin loss rate is low, the amount of hydrochloric acid waste liquid is extremely small, and the economic benefits of energy saving and consumption reduction and the environmental protection and safety effects are realized.

The application discloses a non-natural sugar and a synthesis method and application thereof. At room temperature, hydroxyl groups of an amino sugar are fully trimethylsilyl-protected, amino groups on the sugar are selectively exposed, and after coupling and conversion of the amino groups at room temperature, a non-natural sugar with orthogonal groups and full trimethylsilyl protection is obtained. The non-natural sugar with orthogonal groups and full trimethylsilyl protection is removed from trimethylsilyl protection groups, and a non-natural sugar without protection groups is obtained. The application takes into account the advantages of existing non-natural sugars, ensures that the non-natural sugars can be efficiently utilized by cells, effectively avoids S side reactions with cysteine in proteins in the metabolic process of the non-natural sugars, and simultaneously realizes efficient metabolic labeling. In a cell test, the use concentration of 1,6-bisacylated non-natural sugar is one order of magnitude lower than that of non-natural sugar without protection groups.

The application discloses a full synthesis method of fortimicin B and derivatives thereof, and specifically, the method comprises the following steps: 3-ester group-2-pyrone and N-substituted-2-oxazolone are subjected to asymmetric reverse electron demand Diels-Alder reaction to generate a bridged lactone intermediate, then a series of transformations are performed to obtain an amino cyclic polyol fragment fortimicin B derivative; amino aldehyde and halogenated amino acid ester are subjected to carbon-carbon bond generation reaction mediated by divalent chromium and monovalent cobalt to obtain an amino alcohol intermediate, and subsequent transformation is performed to obtain an amino sugar fragment 6-isomer-erythromycin amine derivative; under the action of a gold catalyst, stereoselective glycosidation reaction occurs between the amino cyclic polyol fragment fortimicin B derivative and the amino sugar fragment 6-isomer-erythromycin amine derivative, ring opening and deprotection steps are performed, and fortimicin B and derivatives thereof are obtained. The synthesis route is short, the operation is simple, raw materials and reagents are easy to obtain, the synthesis route has the advantages of modularity and divergence, and fortimicin B and derivatives thereof which are difficult to synthesize according to the prior art can be synthesized.

Disclosed is a method for preparing an N-acetyl-D-galactosamine tripolymer precursor. In the preparation of the tripolymer precursor, a compound 4 is prepared by the following steps: adding a compound 3, a 4 Å molecular sieve powder, and a reaction solvent into a reactor; inflating and changing protective gas for 3 times; stirring; firstly adding an enol, followed by slowly dropping trimethylsilyl trifluoromethanesulfonate; after a reaction, quenching the reaction with an alkali solution; and performing extraction, separating liquid, washing, drying, filtration, etc., so as to obtain the compound 4. According to the present disclosure, the problems of various production processes, more times of column chromatography for purification of products accompanied by lower yields in the prior art are solved.

The invention relates to a preparation method and application of a sialylated glycan derivative, which comprises the following steps of: uniformly mixing chemically modified sialic acid monosaccharide with a receptor substrate, cytidine triphosphate (CTP), MgCl2, a CMP-sialic acid synthetase preferable mutant and sialyltransferase, transferring a sialic acid derivative to a 3-site or 6-site hydroxyl group on non-reducing end galactose of glycan by a one-pot enzymatic method, and carrying out reaction to obtain the sialylated glycan derivative. And collecting a reaction product to obtain the sialylated glycan derivative. The method is simple and can be used for editing glycans on the surfaces of the immune cells so as to enhance the specificity and cytotoxicity of the immune cells to tumor cells.

The application discloses a kind of glucosamine hydrochloride crude product purification refining process, comprising the following steps: (1) glucosamine hydrochloride crude product is dissolved in water, then add the composite precipitant consisting of sodium chloride and sodium hydroxide, after standing, solid-liquid separation, collected separated liquid phase.(2) after the liquid phase is concentrated, add sodium percarbonate and mix evenly and stand still.After completion, pass in carbon dioxide to convert sodium hydroxide in concentrated solution into sodium carbonate, then continue to add calcium nitrate under stirring condition to make carbonate ion in system complete precipitation, i.e., the liquid to be extracted is obtained.(3) after the liquid to be extracted is cooled, add ethanol for alcohol precipitation, after completion, carry out solid-liquid separation, and the obtained solid product and separated liquid are collected respectively.The solid product is washed with ethanol and dried, and glucosamine hydrochloride finished product is obtained.The above process not only can improve the purity of glucosamine hydrochloride, but also can improve the yield of glucosamine hydrochloride in alcohol precipitation process, thereby reducing waste.

Compounds and compositions that have an asialoglycoprotein receptor (ASGPR) binding ligand bound to an extracellular protein binding ligand for the selective degradation of the target extracellular protein in vivo to treat disorders mediated by the extracellular protein are described.

The present disclosure belongs to the field for preparation of chitosan oligosaccharide, and particularly relates to a chitosan oligosaccharide sulfate and a preparation method thereof. The method is as follows: adding an equal volume of 1.0%-2.0% by mass of potassium sulfate solution into 2.0%-4.0% by mass of chitosan oligosaccharide hydrochloride solution and evenly mixing to obtain a mixed solution, allowing a molar ratio of amino to sulfate ions in the mixed solution to be 2:1, then adding absolute ethyl alcohol to obtain a chitosan oligosaccharide sulfate suspension, standing, filtering, collecting precipitates, washing, drying and smashing to finally obtain the chitosan oligosaccharide sulfate. This method cleverly utilizes a characteristic that the chitosan oligosaccharide sulfate is difficultly dissolved into 75% ethyl alcohol aqueous solution, while potassium chloride is slightly dissolved into 75% ethyl alcohol aqueous solution, the chitosan oligosaccharide sulfate is obtained using a precipitation method. Moreover, the preparation method used in the present disclosure is simple to operate, economic and environmental-friendly, does not need the use of highly corrosive sulfuric acid, and is friendly to operation staffs, environments and production equipment.

The present technology is direct to methods of producing 6,6′-diamino-6,6′-deoxy-trehalose (“DATH”) or a salt thereof. The methods include optionally protecting one or more hydroxyl groups of D-trehalose and converting the primary hydroxyl groups of D-trehalose to product DATH or a salt thereof through use of a halogen, azide, and / or protected amine to. The present technology is also direct to intermediate products of the methods.

Compounds and compositions are described that have an asialoglycoprotein receptor (ASGPR) binding ligand conjugated to an extracellular protein binding ligand that selectively degrades target extracellular proteins in vivo to treat disorders mediated by the extracellular proteins.

To provide polar units, linker intermediates, linkers, drug-linkers and conjugates thereof.SOLUTION: Provided is a Linker intermediate having the following formula (V): wavy line (AA)s-[L2] double wavy line (V) or a salt thereof, (where, AA is an amino acid unit having from 1 to 12 amino acid subunits; s is 0 or 1; L2 is a linker subunit having from 1 to 4 attachment sites for a drug unit; and each wavy line indicates an attachment site for a stretcher unit; and the double wavy line indicates an attachment site for a drug unit), at least one Polar unit being present within the amino acid unit, the linker subunit, or both, and the polar unit being selected from a sugar unit, a PEG unit, a carboxyl unit, and combinations thereof.SELECTED DRAWING: Figure 1A

The present invention relates to a process for the synthesis of at least one C-glycoside comprising the following successive steps: (A) the introduction into a first mechanochemical reactor, separately or previously mixed, of at least one sugar in the form of pyranose and / or furanose and of the D and / or L series, said sugar having at least one hydroxyl function at the obligatorily free anomeric position, of a first reagent which is a β-diketone and of a base, in order to form a first initial mixture; (B1) at least a first grinding of said first initial mixture at a temperature greater than or equal to 20°C, in said first mechanochemical reactor, for a residence time less than or equal to 6 hours, so as to form a ketone C-glycoside; (C) the recovery at the outlet of the first mechanochemical reactor of a final mixture.The present invention also relates to the use of the mechanochemical reactor for synthesizing a C-glycoside or a C-glycoside derivative comprising said at least C-glycoside. Figure for the abstract: no figure.

The invention relates to uridine diphosphate-N-difluoroacetyl galactosamine as well as a preparation method and application thereof. The chemical structure of the UDP-GalNDFA is similar to that of a natural substrate UDP-GalNAc, and the core difference is that N-acetyl at the site 2 of the UDP-GalNDFA is replaced by N-difluoroacetyl. The preparation method comprises the following steps: (1) preparing difluoroacetyl galactosamine; and (2) preparing the UDP-GalNDFA by taking the difluoroacetyl galactosamine as a substrate. As a novel artificial donor sugar, the UDP-GalNDFA has the characteristics of high activity, difficulty in hydrolysis and capability of being artificially synthesized. Compared with the existing donor sugar UDP-GalNTFA, the glucose UDP-GalNTFA has higher catalytic activity on glycosyl transferase, has stronger stability, is not easy to hydrolyze, and can be used as a donor substrate for synthesizing a chondroitin oligosaccharide skeleton, a chondroitin oligosaccharide intermediate and a chondroitin oligosaccharide derivative by a chemical enzyme method.

A method of preparing glucodiamine, comprising contacting glucose with an enzyme oxidation catalyst under conditions suitable for the formation of glucodialdose; contacting glucodialdose with a nitrogen-containing compound under conditions suitable for the formation of glucodioxime; and reducing glucodioxime under conditions suitable for the formation of glucodiamine. A method of preparing glucodiamine, comprising contacting glucodioxime with a dehydration catalyst under conditions suitable for the formation of glucodinitrile; and reducing glucodinitrile under conditions suitable for the formation of glucodiamine. A chemoenzymatic method of producing a bio-based amide platform chemical, comprising: contacting glucose with a biocatalyst under conditions suitable for the formation of glucodialdose; contacting glucodialdose with a base under conditions suitable for the formation of glucodioxime; and contacting glucodioxime with a hydrogenation catalyst in the presence of hydrogen under conditions suitable for formation of glucodiamine.

The object of the present invention is to provide novel means that can be used for solubilizing proteins with poor water solubility. Provided is a hydrophilic solubilizing group for proteins or peptides, comprising a sugar chain moiety; and a functional group moiety that is bound to the amino or carboxy group of said sugar chain, and that binds to the amino acid side chain and can be detached from said protein or amino acid side chain in the presence of an acid.

This invention discloses a comprehensive preparation process for vegetarian glucosamine hydrochloride, comprising the following steps: (1) adding hydrochloric acid to a clarified fermentation broth for hydrolysis, followed by neutralization with alkali to obtain a hydrolysate containing glucosamine hydrochloride. Ethanol is added to the hydrolysate for alcohol precipitation, followed by solid-liquid separation, and the resulting ethanol waste liquid and crude glucosamine hydrochloride are collected separately. (2) The crude glucosamine hydrochloride is reconstituted, and a decolorizing agent is added for decolorization under light. After completion, the decolorizing agent is separated, and the resulting decolorized liquid is concentrated and then ethanol is added for further alcohol precipitation, followed by solid-liquid separation, and the resulting ethanol waste liquid and vegetarian glucosamine hydrochloride product are collected separately. This process not only facilitates the recycling of ethanol waste liquid generated during alcohol precipitation but also forms a decolorizing agent that can achieve decolorization and purification of crude glucosamine, thus improving the purity of glucosamine.