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43 results about "Orthoester" patented technology

In organic chemistry, an orthoester is a functional group containing three alkoxy groups attached to one carbon atom, i.e. with the general formula RC(OR′)₃. Orthoesters may be considered as products of exhaustive alkylation of unstable orthocarboxylic acids and it is from these that the name 'ortho ester' is derived. An example is ethyl orthoacetate, CH₃C(OCH₂CH₃)₃, more correctly known as 1,1,1-triethoxyethane. Orthoesters are used in organic synthesis as protecting groups for esters.

Organic nano composite hydrogel as well as preparation method and application thereof

The invention discloses organic nano composite hydrogel as well as a preparation method and application of the organic nano composite hydrogel, and belongs to the technical field of biological medicine delivery. The polysaccharide-based nano prodrug in the composite hydrogel can be subjected to surface protonation under the stimulation of a tumor extracellular slightly acidic environment, so that cellular uptake is promoted, low-pH / high-concentration glutathione in tumor cells is responded, intracellular aggregation and controllable release of the nano drug are realized, the retention time of the drug in the cells is prolonged, and the bioavailability of the drug is improved. The technical effect of killing tumor cells through combined chemotherapy is achieved. According to the preparation method disclosed by the invention, the release of the polysaccharide-based nano prodrug from the hydrogel and the tissue infiltration capacity are accelerated by adopting fluorinated orthoester, the infiltration of the polysaccharide-based nano prodrug to cells is increased, and then the drug-loaded compound is encapsulated by using gellan gum, so that the slow-release effect of the polysaccharide-based nano prodrug is enhanced; therefore, the efficient enrichment of the medicine at the tumor part is realized.
Owner:ANHUI UNIV

Injectable organic composite hydrogel combined with photo-thermal chemotherapy as well as preparation method and application of injectable organic composite hydrogel

The invention belongs to the technical field of nano biological medicines, and particularly relates to injectable organic composite hydrogel combined with photo-thermal chemotherapy as well as a preparation method and application thereof. The injectable organic composite hydrogel combined with photo-thermal chemotherapy is composed of an orthoester compound and a water-phase hydrogel, the orthoester compound is emulsified and then uniformly dispersed in the hydrogel, and the hydrogel is formed by crosslinking carboxymethyl chitosan and glutaraldehyde. In the injectable organic composite hydrogel combined with photo-thermal chemotherapy provided by the invention, firstly, oily orthoester is utilized to dissolve a cis-platinum prodrug and indocyanine green to obtain an orthoester compound, then the orthoester compound is uniformly emulsified and loaded in the hydrogel, dynamic imine bonds of the hydrogel respond to tumor slightly acidic environment breakage, and then the dynamic imine bonds of the hydrogel are separated from the dynamic imine bonds of the hydrogel, so that the injectable organic composite hydrogel combined with photo-thermal chemotherapy can be used for preparing the injectable organic composite hydrogel combined with photo-thermal chemotherapy. The orthoester compound successfully escapes, along with degradation of the oily orthoester, the cis-platinum prodrug and the indocyanine green are self-assembled through hydrogen bonds to form nanoparticles, the enrichment and retention capacities of the two drugs at the tumor site are enhanced, and the overall curative effect is improved.
Owner:ANHUI UNIV

UV-cured epoxy resin material for 3D printing and preparation method thereof

The invention particularly relates to a UV-cured epoxy resin material for 3D printing and a preparation method of the UV-cured epoxy resin material. The epoxy resin material is prepared from the following raw materials in parts by weight: 60 to 65 parts of epoxy acrylate resin, 30 to 35 parts of epoxy resin, 2 to 5 parts of ANFs / graphene / MoS2 composite lubricant, 4 to 6 parts of flexibilizer, 3 to 5 parts of repairing agent, 3 to 5 parts of spiro orthoester, 1 to 3 parts of initiator, 0.6 to 1.5 parts of tetrahydrofuran acrylate and 0.1 to 1 part of rheology modifier. The UV-cured epoxy resin material for 3D printing obtained by the scheme has good toughness, impact resistance and wear resistance, and has good self-recovery capability and high long-term reliability under a heating condition for conditions such as slight scratches and cracks in 3D printing application.
Owner:SHENZHEN FRD SCI & TECH

Organic composite hydrogel as well as preparation method and application thereof

The invention relates to the technical field of preparation of biological materials and pharmaceutical preparations, in particular to organic composite hydrogel as well as a preparation method and application thereof. The specific preparation method comprises the following steps: dissolving a targeted drug in orthoester to obtain a targeted drug-orthoester solution; the preparation method comprises the following steps: mixing an oxidized dextran solution, a targeted drug-orthoester solution and a carboxymethyl chitosan solution, carrying out vortex treatment, and standing to prepare the organic composite hydrogel. The solubility of the targeted drug in the hydrogel is improved by utilizing orthoester, the orthoester can carry the targeted drug to efficiently escape from the hydrogel, and the targeted drug can be self-assembled to form nanoparticles along with degradation of the orthoester in the escape process, so that the retention capacity of the targeted drug at a tumor site is enhanced, and the targeting drug can be used for treating tumor tumors. The drug enrichment capacity is improved, meanwhile, the toxic and side effects of the whole body are reduced, and the problems that nano-drugs are poor in solubility, still prone to being removed after intravenous administration and poor in enrichment effect at tumor sites are solved.
Owner:ANHUI UNIV

PH response hydrogel microneedle and preparation method thereof

The invention discloses a pH response hydrogel microneedle, which comprises a microneedle substrate, microneedle tips are arranged on the microneedle substrate, the height of the microneedle tips is 100-1600 microns, the diameter of the tip ends of the microneedle tips is 5-15 microns, and the density of the microneedle tips is 200-1000 pieces per square centimeter. The preparation method comprises the following steps: preparing a hyaluronic acid solution for the microneedle substrate, preparing a methacrylated chondroitin sulfate solution for the microneedle tip, preparing methacrylated orthoester, preparing orthoester, preparing a non-steroidal anti-inflammatory drug solution, preparing a microneedle tip solution, preparing the microneedle and demolding the microneedle to prepare the complete soluble microneedle patch. The invention has the advantages of high drug efficiency, high efficiency in dissolving fat / water drugs, and long-acting slow release.
Owner:NINGBO ZHENGLI PHARM PACKING CO LTD

Preparation method and application of modified PVC adsorbent for gold extraction of carbonaceous gold ore

The invention provides a preparation method and application of a modified PVC adsorbent for gold extraction of carbonaceous gold ore, and belongs to the technical field of organic polymer materials and resource utilization. Based on construction of a hydroxylation-xanthate esterification reaction and bifunctional adsorption sites, a series of chemical modification paths of acetate nucleophilic substitution-hydrolysis-carbon disulfide alkali treatment are established, and xanthate functional groups with high reaction activity are accurately constructed on an inert PVC framework. Sulfur atoms in xanthate groups of the modified PVC are excellent electron donors and can generate strong chemical adsorption with metal impurities or polar sites on the surface of carbon, meanwhile, Van der Waals interaction between a main chain of the modified PVC and the carbon is reserved, and unmodified PVC or single hydroxylated PVC does not have the synergism of chemical adsorption and physical adsorption, so that the modified PVC can be used for preparing the carbon-modified PVC composite material, and the carbon-modified PVC composite material can be used for preparing the carbon-modified PVC composite material. And leap-type improvement of the adsorption capacity and selectivity of organic carbonaceous in minerals is realized.
Owner:CHANGCHUN GOLD RES INST

Slow reaction recyclable epoxy resin system and process for recycling composite materials

PendingCN122037139ACyclopentenePolymer science
A slow-reaction recyclable epoxy resin system for structural composites and a process of recycling the composites made therefrom are disclosed. The system includes an epoxy resin component including: a high purity epoxy resin selected from a high purity bisphenol A epoxy resin, a high purity bisphenol F epoxy resin, and combinations thereof, where the high purity epoxy resin is in a range of from 20 wt% to 95 wt% of the total weight of the cyclopentene resin component; a standard epoxy resin selected from a standard bisphenol A epoxy resin, a standard bisphenol F epoxy resin, and combinations thereof, where the standard epoxy resin is in the range of from 1 wt% to 50 wt% of the total weight of the epoxy resin component; and a curing agent component including a curing agent having at least one cleavage bond selected from a group including an acetal bond, a ketal bond, a formal bond, an orthoester bond, or a siloxy bond. The pot life of the slow-reaction recyclable epoxy resin system is greater than 540 minutes at 25 DEG C.
Owner:ADITYA BIRLA CHEM (THAILAND) LTD

Treatment composition containing esteramine or its salt

PendingJP2026521999AOrthoesterBiology
A treatment composition comprising at least one fragrance raw material and an esteramine or a salt thereof, which may be obtained by a process using a catalytic amount of at least one orthoester, and a method for treating an article or surface, optionally comprising treating the article or surface with such treatment composition in the presence of water.
Owner:PROCTER & GAMBLE CO

Injection chemical composition, and a solidified body and soil stabilization method using the same.

To provide an injection chemical composition that can achieve both curability in water and foaming and curability in non-water environments, even after being exposed to high temperature and high humidity environments. [Solution] An injection solution composition comprising a first agent (A) and a second agent (B), wherein the first agent (A) comprises an aqueous solution of sodium silicate (A-1), an organic polyol (A-2), and a tertiary amine catalyst (A-3), and the second agent (B) comprises an organic polyisocyanate containing a mixture of diphenylmethane diisocyanate and polymethylene polyphenyl polyisocyanate having 3 or more isocyanate functional groups (B-1), or a reaction product (B-1') of an active hydrogen group-containing compound and a mixture (B-1), at least one acid component (B-2) selected from the group consisting of phosphate monoesters and phosphate diesters, and at least one hydrolyzable component (B-3) selected from the group consisting of orthoester compounds and acetal compounds.
Owner:TOSOH CORP

A method for preparing dihydropyridine drug intermediate M2

The present application provides a method for preparing a high-purity key intermediate M2 of dicardipine drugs, belonging to the technical field of drug intermediate preparation. A dehydrating agent is added during the preparation of the intermediate M2, and the dehydrating agent is an orthoester dehydrating agent. Using the method provided in the present application, the yield of the intermediate M2 is 84.3%, the HPLC purity is 99.63%, M2Z3: 0.17%; M2Z4: 0.15%; other impurities <0.10%, and the content of impurities P0Z4 (i.e., M2Z3) and P0Z5 in the further prepared nicardipine is determined to be: P0Z5 <0.02%, P0Z4 <0.02%.
Owner:成都硕德药业有限公司

Alkali-developable photocurable thermosetting resin composition

[Question] To provide an alkali-developable curable resin composition that suppresses performance degradation even under relatively harsh storage conditions. [Solution] An alkali-developable curable resin composition characterized by comprising at least (A) an alkali-soluble resin, (B) a photopolymerization initiator having an oxime bond, (C) a reactive diluent, and (D) a thermosetting resin, wherein the composition is at least a two-component system in which the (B) photopolymerization initiator having an oxime bond and the (A) alkali-soluble resin are blended into separate compositions, and at least one (E) orthoester compound is blended with the (B) photopolymerization initiator having an oxime bond.
Owner:TAIYO HOLDINGS CO LTD

Radiation-sensitive composition, hardened film and method for producing the same, semiconductor element, display element

The present invention aims to provide a radiosensitive linear composition, a hardened film, a method for manufacturing the same, a semiconductor element, a display element, and a polymer that can produce a film with excellent adhesion. A radiosensitive linear composition comprises: a polymer containing a structural unit (I) having a base represented by formula (1), a photoacid generator, and an orthoester compound. In formula (1), R... 1 It can be a hydrogen atom, a halogen atom, a hydroxyl group, or an alkoxy group having 1 to 6 carbon atoms. R 2 and R 3 Each of the following can be independently a hydrogen atom, a halogen atom, a hydroxyl group, an alkoxy group with 1 to 6 carbon atoms, an alkyl group with 1 to 10 carbon atoms, or a phenyl group. "*" indicates a bond.
Owner:JICC 02 LTD

Diimine ligands, methods of making and using the same

The present application relates to the technical field of nickel-based catalyst, and discloses a diimine ligand, a preparation method and application thereof, wherein the raw materials for preparing the diimine ligand contain acenaphthenequinone, a protective agent, substituted aniline and a catalyst, the protective agent is selected from one or more than two of ortho ester, amine, hydrazine and substituted hydrazine; and the molar ratio of the acenaphthenequinone, the protective agent, the substituted aniline and the catalyst is 1:(0.5-3):(1.6-2.4):(0.1-10). In the present application, a certain amount of protective agent is added to the reaction system, the acenaphthenequinone is reacted with the ortho ester or low-molecular-weight amine to generate ketal or imine, the ketal or imine is separated or not separated, and then reacted with the substituted aniline to generate the target product diimine ligand, no water is generated in the synthesis reaction of the diimine ligand, the balance can be effectively promoted to the forward reaction, and the reaction yield is improved.
Owner:JUHUA GROUP TECH CENT

A cross-linked nanoprodrug, a nano-self-assembled hydrogel precursor sheet prepared therefrom, and its applications.

This invention discloses a cross-linked nanoprodrug, a nano-self-assembled hydrogel precursor tablet prepared therefrom, and its applications. The nano-self-assembled hydrogel precursor tablet of this invention is prepared by direct compression of the cross-linked nanoprodrug or by compression of a cross-linked nanoprodrug mixed with a drug-loaded orthoester compound. It exhibits high nanodrug content, enhanced nanoparticle release, and high storage and transport stability, as well as good patient compliance. This nano-self-assembled hydrogel precursor tablet responds to the pH gradient environment of the gastrointestinal tract. In acidic gastric juice, through protonation of functional groups, it forms a three-dimensional network structure of nano-self-assembled hydrogel mediated by hydrogen bonds. Subsequently, it stably passes through the small intestine into the colon. In the alkaline colonic environment, its functional groups deprotonate, hydrogen bonds break, and the drug is efficiently released under the electrostatic repulsion between nanoparticles and the synergistic repulsion of the orthoester compound. While preferentially adhering to colonic lesions through electrostatic interactions, it significantly improves the targeted and synergistic therapeutic effect on CRC.
Owner:ANHUI UNIV

A process for the preparation of methyl 3,4-dihydroxy-5-methoxybenzoate

The present application relates to a kind of preparation methods of 3,4-dihydroxy-5-methoxybenzoic acid methyl ester, with gallic acid as raw material, it is reacted with trimethyl orthoformate or trimethyl orthoacetate, trimethyl orthoformate or trimethyl orthoacetate can realize the protection of adjacent diphenol hydroxyl on one hand, on the other hand, carboxyl esterification and 5-hydroxyl are methylated, form the methyl ester of 5-phenolic hydroxyl methylation and 3,4-orthoester protection benzoic acid shown in formula 1a or formula 1b, further by acidic solution treatment, deprotection is carried out, and the target product 3,4-dihydroxy-5-methoxybenzoic acid methyl ester is prepared.The preparation method is mild in reaction condition, process is simple, easy to operate, product yield and purity are high, solve the wastewater problem in borax protection method, and avoid using toxic dimethyl sulfate for methylation, process condition is simple, easy to operate, convenient for industrialization, with very high application value.
Owner:TIANJIN JIURUISHENG TECHNOLOGY CO LTD +1

PH-responsive supramolecular salicylic acid nanogel as well as preparation method and application thereof

PendingCN121754449Asolve solubilityresolve irritating conflictsCosmetic preparationsAntibacterial agentsActive agentSalicylic acid
The invention discloses a pH-responsive supramolecular salicylic acid nanogel and a preparation method and application thereof, and the pH-responsive supramolecular salicylic acid nanogel comprises the following preparation raw materials by mass: 3-30% of salicylic acid; 0.6 to 1.5 percent of orthoester; 30 to 50% of poloxamer; 0.5 to 5.0 percent of polyhydric alcohol; 0.5-1% of a surfactant; and the balance solvent. Through supramolecular design, salicylic acid molecules and a precursor containing a pH sensitive group (orthoester) are integrally constructed into a nanogel network through non-covalent self-assembly, so that the contradiction between solubility and irritation of high-concentration salicylic acid is fundamentally solved; the prepared pH-responsive supramolecular salicylic acid nanogel can realize the synergistic effects of stable loading of high-concentration salicylic acid, targeted response release of an inflammatory site and low skin irritation, and the preparation process is simple, convenient and environment-friendly, is suitable for industrial production, and has a wide application prospect in the field of functional skin care products.
Owner:ANHUI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE

PH-responsive hydrogel microneedle as well as preparation method and application thereof

The invention discloses a pH response hydrogel microneedle as well as a preparation method and application thereof. The pH response hydrogel microneedle comprises a hydrogel microneedle main body and colchicine loaded in the hydrogel microneedle main body, the hydrogel microneedle main body is hydrogel with a three-dimensional network structure, which is formed by covalent cross-linking of methacrylated hyaluronic acid and methacrylated orthoester. The hydrogel microneedle prepared by taking the methacrylated hyaluronic acid and the methacrylated orthoester as cross-linking components not only has good mechanical property, swelling property and biocompatibility, but also can respond to the microenvironment pH of an inflammation part by virtue of the pH sensitivity of the methacrylated orthoester, so that the utilization rate of a medicine is improved, and the bioavailability of the medicine is improved. The acute gout arthritis can be quickly and efficiently treated, and the clinical application potential is huge.
Owner:ANHUI UNIV

Preparation method of cellulose-based radiation cooling material

PendingCN120988347ACelluloseSilicic acid
The invention discloses a preparation method of a cellulose-based radiation cooling material, and belongs to the technical field of cooling materials. Comprising the following steps: adding a tetraethyl orthosilicate solution into absolute ethyl alcohol, stirring, then adding deionized water, adjusting the pH value to be alkaline by using ammonia water, and continuously stirring to obtain a SiO2 spherical prepolymer; continuously adding xanthate cellulose nanofibers, stirring, and centrifuging to obtain a precipitate; finally, adding water into the precipitate to uniformly disperse the precipitate, so as to prepare a SiO2 (at) CNF mixed solution; adding tert-butyl alcohol into the SiO2 (at) CNF mixed solution, and stirring to obtain a dispersion; and pouring the dispersion into a mold, carrying out freezing treatment, and then drying to obtain the SiO2 (at) CNF hybrid aerogel. The aerogel can be applied to the field of radiation cooling.
Owner:TIANJIN POLYTECHNIC UNIV

Sustained release drug delivery systems and related methods

The present disclosure provides for methods of producing analgesia in a subject. In some cases, methods produce analgesia in a subject undergoing arthroscopic subacromial decompression surgery. The present disclosure also relates to improved sustained release drug delivery systems. In some cases, a composition comprises an active pharmaceutical agent; at least one of sucrose acetate isobutyrate and a polyorthoester; an organic solvent; and 2,6-dimethylaniline, wherein the 2,6-dimethylaniline is present at a level less than 500 ppm. In some cases, a composition comprises bupivacaine N-oxide at a level less than 1 wt %, based on weight of the composition. In some cases, a composition comprises metal present at a level less than 5 ppm. Dosage forms and methods are also provided.
Owner:MEDICIS PHARMACEUTICAL CORP

Propylene carbonate-based thermal conductive fluid

PendingJP2026524803AOrthoesterPropylene carbonate
Alkene carbonate-based anhydrous cooling fluids have low toxicity and electrical conductivity, and high heat capacity. The fluids provide corrosion protection to cooling systems and remain liquid below -30°C. Furthermore, the fluids exhibit low viscosity at low temperatures. Some formulations contain dehydrating orthoesters.
Owner:CCI NORTH AMERICA CORP

Drug delivery system for increasing endosome escape

A composition comprising (a) a therapeutic agent or a pharmaceutically acceptable salt thereof; (b) a PEG (polyethylene glycol)-monoorthoester-lipid; (c) an amphiphilic lipid; (d) a cationic lipid and / or a [beta]-alanyl-prolyl-cysteine methyl ester; and optionally (e) a steroid and / or ceramide and / or DOPE. The composition is used as a medicament.
Owner:MAX PLANCK GESELLSCHAFT ZUR FOERDERUNG DER WISSENSCHAFTEN EV

Manufacture of xanthate by continuous conversion

A method for the manufacture of high purity xanthate continuously in a system of reactors in a liquid organic medium by reacting caustic and alcohol to form alcoholate in a large circulating charge of previously reacted alcoholate at an elevated temperature, preferably no more than 110° C. A portion of the alcoholate is continuously withdrawn, cooled preferably to no more than 35° C. and rapidly dispersed with carbon disulfide to form xanthate in a large circulating charge of previously reacted xanthate while maintaining precise temperature control. Average contact time with byproduct water is 10 minutes. The product is continuously withdrawn and immediately dried to obtain in excess of 95% pure product.
Owner:EDWARDS CARY RIDER

Injectable organic composite hydrogel combined with photothermal chemotherapy and its preparation method and application

The present invention belongs to the field of nano-biomedicine technology, and specifically relates to an injectable organic composite hydrogel combined with photothermal chemotherapy, a preparation method, and an application. The injectable organic composite hydrogel combined with photothermal chemotherapy of the present invention is composed of an orthoester complex and a hydrogel of an aqueous phase. The orthoester complex is uniformly dispersed in the hydrogel after emulsification, and the hydrogel is cross-linked by carboxymethyl chitosan and glutaraldehyde. In the injectable organic composite hydrogel combined with photothermal chemotherapy provided by the present invention, cisplatin prodrug and indocyanine green are first dissolved by oily orthoester to obtain an orthoester complex, and then the orthoester complex is emulsified uniformly and loaded into the hydrogel. The dynamic imine bond of the hydrogel breaks in response to the micro-acidic environment of the tumor, and the orthoester complex successfully escapes. Along with the degradation of the oily orthoester, the cisplatin prodrug and indocyanine green are self-assembled through hydrogen bonds to form nanoparticles, thereby enhancing the enrichment and retention capacity of the two drugs at the tumor site and improving the overall efficacy.
Owner:ANHUI UNIV

Efficient process for making 6-carboxy benzoxazole derivatives

The present invention is directed to an efficient process for preparing benzoxazole derivatives comprising the step of reacting a 4-Amino-3-hydroxybenzoic acid compound of Formula III with a 3,5-Dichlorophenyl ortho ester compound of Formula II to provide the compound of Formula Iwherein R1, R2a, R2b and R2c are as described herein.
Owner:PFIZER IRELAND PHARMACEUTICALS (CORPORATION)

N-substituted carbamoyl xanthate flotation collectors and methods of making and using same

PendingCN122644195AChalcopyriteOrthoester
The present application belongs to the technical field of mineral flotation, and particularly relates to N-substituted carbamoyl xanthate flotation collector and preparation method and application. Halogenated acyl compound is used as bridging structure, and fatty amine and xanthate are introduced into two ends thereof. Compared with the prior art, the present application has the beneficial effects that the flotation collector molecule of the present application contains two functional groups of amide group and xanthate group, and the synergistic effect of the two functional groups makes the collector molecule form stable adsorption on the surface of chalcopyrite, compared with the traditional flotation collector Z-200 or xanthate, the recovery rate of the flotation collector of the present application on chalcopyrite is better under the same low dosage condition. The flotation collector of the present application can realize efficient flotation of chalcopyrite under the natural pH condition of ore pulp; a one-pot two-step method is used, and water is used as solvent, so that the use of organic solvent is avoided; the reaction condition is mild, the operation process is less, and the product yield can be up to 94% or more, which is beneficial to industrial production.
Owner:QINGDAO UNIV OF SCI & TECH

Bionic nanoparticle suspension dosage form based on orthoester compounds and preparation method thereof

The present invention belongs to the technical field of biomedicine, and discloses a bionic nanoparticle suspension dosage form based on orthoester compounds and a preparation method thereof. The bionic nanoparticle suspension dosage form includes liquid excipients, as well as a photosensitizer and bionic nanoparticles dispersed in the liquid excipients. In the present invention, an orthoester compound represented by Formula I is used as the liquid excipient, and the bionic nanoparticles and the photosensitizer are simultaneously introduced into OE to obtain a bionic nanoparticle suspension dosage form with multiple anti-tumor mechanisms. Among them, the bionic nanoparticles are nano-drugs encapsulated by cancer cell membrane vesicles, and through the cancer cell membrane bionic technology, the homologous targeting function provided by the cancer cell membrane is utilized to significantly improve the active targeting and cellular uptake of the nano-drugs. Formula I:
Owner:ANHUI UNIV

Method for stereoselectively constructing C-alkyl glycosylation by visible light mediated EDA complex formed by glycosyl xanthate and NHC-borane

The invention discloses a method for stereoselectively constructing C-alkyl glycosylation through a visible light mediated EDA complex formed by glycosyl xanthate and NHC-borane, and belongs to the technical field of sugar chemistry, # imgabs0, compounds shown in a formula I and a formula II are dissolved in an organic solvent, and a target product shown in a formula III is obtained through a reaction under the conditions of NHC-BH3 and illumination. The glycosyl free radicals of the present application are generated by an EDA complex of metal-free / alkali-free photoactivated glycosyl xanthate and NHC-BH3. The process does not require high temperature, and the reaction is cleaner compared to conventional peroxide initiation. In view of green and mild conditions, the strategy shows a wide substrate range and functional group compatibility. Formation and possible reaction ways of the EDA compound are proved through mechanism research. The work not only opens up a new application of the glycosyl xanthate as a photocatalyst in synthetic chemistry, but also opens up a new way for general application of an EDA mediated system in photocatalysis.
Owner:JIANGXI NORMAL UNIV

A process for the preparation of a non-zanidatamab

The application discloses a preparation method of fezolinetant, and belongs to the technical field of medicinal chemistry. The cheap and easily obtained 2-halogenated-3-methyl pyrazine is used as a raw material in the route, and is sequentially reacted with hydrazine hydrate and ortho ester, and then is subjected to a hydrogenation reduction reaction to generate compound 4; the compound 4 is subjected to chiral resolution or chiral separation and condensation reaction with p-fluorobenzoyl halide to obtain intermediate compounds 5 or 5' and new intermediate compound 6. The compound 6 is reacted with a halogenating reagent to obtain compound 7; the compound 7 is subjected to Suzuki coupling reaction with compound 8 to obtain the compound fezolinetant of formula A; the route is simple in reaction, high in preparation efficiency, and the reaction yield of each step can be higher than 90%; the reaction condition is not harsh, the operation is safe, the post-treatment is simple, and the environmental pollution is small. The route is suitable for large-scale production, can obtain high-chiral products, and the chiral purity of the final product is as high as 99.5%, and has good market value and far-reaching practical significance.
Owner:SHANGHAI HAOYUAN CHEMEXPRESS CO LTD