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10 results about "Nitro reduction" patented technology

A method for synthesizing a tridentate linker fragment useful for improving the hydrophilicity of antibody drug conjugates

The application discloses a synthesis method of a trident connecting segment which can be used for improving hydrophilicity of an antibody drug conjugate, and relates to the field of organic synthesis. The {[5-amino-2-(3,3,4,4-tetramethyl-2-oxa-3-silapent-1-yl)phenyl]methyl}(methyl)amino)methane acid-2-methylpropan-2-yl ester can be used for connecting a hydrophobic dipeptide, a hydrophilic chain and a small molecule drug in an ADC drug, so as to prolong the action time of the ADC drug. The application takes cheap and easily obtained commercial raw material 2-bromo-5-nitrobenzaldehyde as a starting raw material, and successfully prepares the target product through seven steps of conventional transformation such as reduction amination, protection, coupling, ozonation and nitro reduction, with a total yield of about 60% and a scale of hundreds of grams. The starting raw material is cheap, the operation and treatment are simple, and the reaction condition is mild, so that the application is a brand-new process synthesis route, and has good economic benefits and market prospects.
Owner:WUHAN AOFEI TECH CO LTD

A process for the preparation of 2-acetylamino-4-[(2-hydroxyethyl)sulfonyl]benzoic acid

The application discloses a preparation method of 2-acetylamino-4-[(2-hydroxyethyl)sulfonyl]benzoic acid. The 2-acetylamino-4-[(2-hydroxyethyl)sulfonyl]benzoic acid is prepared from 4-fluoro-2-nitrobenzoic acid methyl ester as a starting material through aromatic nucleophilic substitution reaction, nitro reduction reaction, ester hydrolysis reaction, amino acylation reaction, thioether oxidation reaction and the like. The method has the advantages of mild reaction condition, high yield, low cost, easy availability of raw materials, and the like. The synthesis process meets the requirements of green chemistry, the synthesis route is innovative, the reaction post-treatment is simple, and the product is easy to purify.
Owner:ANHUI UNIV

Inhibitors of factor xa and methods of making and using the same

PendingCN122444727AAntithrombotic AgentMannich reaction
The application belongs to the technical field of medicine and chemical industry, and particularly relates to FXa inhibitors and a preparation method and application thereof. The FXa inhibitor has a structural general formula as shown in the description, wherein R1 is,,, or. The preparation method of the FXa inhibitor comprises the following steps: taking p-nitroaniline as a starting material, and sequentially performing amide condensation, substitution and cycloaddition to prepare a compound 5; taking p-methoxyaniline as a starting material, and performing diazotization, cyclization, elimination and nitro reduction to prepare a compound 10; performing reaction of the compound 10 and 2,5-dimethoxytetrahydrofuran to obtain a compound 11, performing a Mannich reaction to obtain intermediates 12a-12e, and finally performing ammonolysis to obtain compounds A01-A05. The FXa inhibitor and the preparation method thereof synthesize novel pyrazolopyridine derivatives. When the FXa inhibitor is applied to preparation of an antithrombotic drug, high-efficiency anticoagulation activity, good pharmacokinetic properties and a low risk of bleeding are obtained.
Owner:QILU SCHOOL OF MEDICINE

Polyimides containing dibenzofuran / dibenzothiophene and triphenylamine structures, and methods of making and using the same

PendingCN122444992APolymer scienceAniline
Polyimide containing dibenzofuran (thiophene) and triphenylamine structure and preparation method and application thereof, and application thereof, the present application relates to polyimide containing dibenzofuran (thiophene) and triphenylamine structure and preparation method and application thereof. In order to solve the problem of low solubility of aromatic polyimide in organic solvent, poor optical contrast, slow response time and poor capacitor performance, 2,8-dibromodibenzofuran (thiophene) is used as raw material, and 4-methoxy-4'-nitrodiphenylamine is reacted to obtain a new precursor containing dibenzofuran (thiophene) and triphenylamine structure. The nitro group is reduced to obtain a diamine monomer, which is polymerized with dianhydride to form a new high-performance polyimide. At the same time, the polymer has excellent electrochromic performance, including excellent cycle stability, fast switching time, high optical contrast and low voltage start. It also has excellent capacitor performance, including excellent specific capacity and cycle stability. The present application is expected to be applied in the field of electrochromic supercapacitor.
Owner:HEILONGJIANG UNIV

A method for synthesizing milobalin benzylsulfonic acid

ActiveCN117886708BCyclobutaneNitromethane
This invention provides a method for synthesizing milobalin benzylsulfonic acid, comprising the following steps: a chiral enone undergoes a condensation reaction with cyanoacetate in the presence of ammonium acetate to obtain an unsaturated cyano ester; next, the unsaturated cyano ester undergoes a condensation reaction with nitromethane to obtain a nitro ester; the nitro ester is then deesterified at high temperature to obtain a chiral nitro nitrile, which is then reduced to a chiral amino nitrile; subsequently, the chiral amino nitrile is hydrolyzed to obtain the free base of milobalin; finally, the free base of milobalin is salted with benzylsulfonic acid to obtain milobalin benzylsulfonic acid. This invention stereospecifically constructs a chiral cyclobutane quaternary carbon center to obtain a chiral nitro ester with a single stereoconfiguration, avoiding the chiral isomer waste generated by chiral isomer resolution, eliminating the need for chiral column separation or chiral resolution, significantly reducing production costs, and simultaneously avoiding the environmental pollution caused by residual heavy metal titanium in the product and solid waste heavy metal titanium.
Owner:ZHEJIANG TIANYU PHARMA +1

A method of photo-initiated nitro-reduction hydrogenation

The application discloses a method for photo-induced nitro reduction hydrogenation, and belongs to the field of medical compound synthesis.The method provided by the application takes iron trichloride and palladium-carbon as the catalysts of main reactions, and realizes nitro reduction into amino under the conditions of normal temperature, normal pressure and nitrogen, the reaction has high catalytic efficiency and fast reaction rate, the reaction time is only 10 minutes, the yield of the product obtained by nitro reduction is high, the experimental cost is greatly reduced, the method is suitable for the synthesis and amplification of later-stage compounds, the method has simple steps, wide substrate application range, and the effects of high efficiency, green environmental protection, safety and cost saving, and the reaction has fast reaction rate, and has excellent application prospect in industrial production.
Owner:SHANDONG FIRST MEDICAL UNIV & SHANDONG ACADEMY OF MEDICAL SCI

Photoresist for capacitive touch sensor and preparation process thereof

The invention relates to the technical field of photoresist, in particular to photoresist for a capacitive touch sensor and a preparation process of the photoresist. The invention discloses a preparation process of photoresist for a capacitive touch sensor. The preparation process comprises the following steps: preparing a modified photoreaction agent; preparing modified polyimide resin powder; preparing silicon dioxide hollow carbon spheres and nano titanium dioxide hybrid particles; and preparing the photoresist. The preparation method comprises the following steps: firstly carrying out nitration reaction on 4-tert-butylphenol, then reducing nitryl into amino to obtain amino substituted 4-tert-butylphenol, protecting the amino by di-tert-butyl dicarbonate ester, then oxidizing iodobenzene into a high-valence iodine active intermediate by taking m-chloroperoxybenzoic acid as an oxidizing agent, and reacting with Boc-amino substituted 4-tert-butylphenol to obtain the high-valence iodine-substituted 4-tert-butylphenol. And finally, carrying out a replacement reaction with silver trifluoromethanesulfonate, carrying out deprotection to obtain a modified photoreaction agent, and carrying out a condensation polymerization reaction on the modified photoreaction agent, 4, 4 '-hexafluoroisopropyl phthalic anhydride and the like to generate a polyamic acid prepolymer, so that the photoetching resolution can be greatly improved.
Owner:江苏佳合盛科技有限公司

A fluorine-containing bromoaniline compound and a preparation method thereof

This invention discloses a fluorobromoaniline compound and its preparation method, belonging to the field of organic synthesis technology. The method employs a three-step synthetic pathway starting with 2,6-difluoronitrobenzene, involving sequential ammonolysis, diazotization bromination, and nitro reduction. Utilizing the triple function of the nitro group: firstly, it acts as a strong electron-withdrawing group, guiding the ammonolysis reaction selectively at the fluorine atom at the 6-position, generating 2-fluoro-3-nitrobenzene; subsequently, the diazotization step stabilizes the diazonium salt intermediate, ensuring the specific substitution of the bromine atom at the original amino position, yielding 2-fluoro-6-bromonitrobenzene; finally, the nitro group is gently reduced to the amino group to obtain the target product. This invention eliminates the need for amino protection and deprotection steps, avoiding the use of precious metal catalysts and hazardous reagents. It possesses advantages such as high regioselectivity, high atom economy, and a simple procedure, making it suitable for continuous industrial production and providing a novel approach for the efficient preparation of pharmaceutical and material intermediates.
Owner:FUXIN JINHONGTAI CHEM

A method of synthesizing relugolix

ActiveCN117327091BOrganic chemistryNitro reductionHydrolysis
The application provides a synthesis method of relugolix, comprising the following steps: reacting compound 2 with di-tert-butyl dicarbonate to obtain compound 3; reacting compound 3 with dibromohydantoin to obtain compound 4; reacting compound 4 with dimethylamine hydrochloride to obtain compound 5; hydrolyzing compound 5 to obtain compound 6; condensing compound 6 with 6-methoxy-3-aminopyridazine to obtain compound 7; deprotecting the amino group of compound 7 to obtain compound 8; performing reductive amination on compound 8 with 2,6-difluorobenzaldehyde to obtain compound 9; performing nitro reduction on compound 9 to obtain compound 10; and reacting compound 10 in the presence of carbonyldiimidazole and methoxyamine hydrochloride to obtain relugolix. The synthesis method is more efficient than prior art, avoids potential genotoxic impurities in the prior art, has mild process conditions, high reaction yield in each step, effectively reduces industrial production cost and safety risk, and is suitable for industrial production.
Owner:ZHEJIANG TIANYU PHARMA