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31 results about "Nitroimidazole" patented technology

5-Nitroimidazole is an organic compound with the formula O₂NC₃H₂N₂H. The nitro group at position 5 on the imidazole ring is the most common positional isomer. The term nitroimidazole also refers to a class of antibiotics that share similar chemical structures.

Preparation method of in-situ growth ZIF-71 polypropylene composite membrane and application of in-situ growth ZIF-71 polypropylene composite membrane in non-aqueous flow battery

PendingCN122011499ARegenerative fuel cellsNitroimidazolePolypropylene composites
The invention relates to a composite membrane of a zeolite imidazate framework (ZIF-71) and a polypropylene (PP) membrane in a metal organic framework, a preparation method of the composite membrane and application of the composite membrane in a non-aqueous flow battery, belongs to the technical field of flow batteries, and provides a ZIF-71 / PP composite membrane which is prepared through different in-situ growth methods and has different surface appearances. The in-situ grown 2-nitroimidazole zinc zeolite imidazate framework layer with different morphologies can effectively prevent active substances from crossing and crossing in the non-aqueous flow battery. In addition, the excellent performance of the non-aqueous flow battery verifies that the composite diaphragm of the metal organic framework and the polypropylene can still keep the structural integrity during long-term operation in an organic medium.
Owner:NANJING TECH UNIV

A zinc-based mixed imidazole ligand metal-organic framework adsorbent for efficient separation of CF4 / N2 and its preparation method

PendingCN122302306ANitroimidazoleAdsorption separation
This invention discloses a zinc-based mixed imidazole ligand metal-organic framework (ZIF) adsorbent material for highly efficient separation of CF4 / N2 and its preparation method. By strategically controlling the ratio of benzimidazole and 2-nitroimidazole ligands, a series of ZIF materials with large specific surface areas and suitable pore structures for adsorbing and separating CF4 / N2 are prepared. The 2-nitroimidazole provides a certain polarization effect to the framework, and its own electron-withdrawing effect and relatively long Zn-N bond length (easily broken) make it suitable as a parent material for ligand exchange. The benzene ring on the benzimidazole provides more adsorption sites for the framework. The metal-organic framework adsorbent material prepared by this invention can achieve highly efficient adsorption of CF4 and selective separation of CF4 / N2, exhibiting excellent performance and significant economic and social benefits.
Owner:FUZHOU UNIV +1

Nitroimidazole group meso-substituted heptamethine cyanine dye as well as preparation method and application thereof

The invention relates to a nitroimidazole group meso-substituted heptamethine cyanine dye as well as a preparation method and application thereof. According to the dye, a nitroimidazole group is introduced into the middle position of a heptamethine cyanine parent nucleus, so that the dye has excellent absorption characteristics in a near-infrared region, the excitation wavelength is 730-780 nm, the emission wavelength is 800-860 nm, and the dye has good tissue penetrating power. The nitroimidazole group can effectively quench fluorescence in an excited state through a light-induced electron transfer effect, energy is promoted to be released in a non-radiative transition mode, the photothermal conversion efficiency is remarkably improved, and meanwhile high light stability and low fluorescence quantum yield are kept. The dye can be further prepared into a nano preparation and shows excellent biocompatibility and tumor targeting ability. The compound has wide application prospects in the fields of non-diagnostic or therapeutic protein labeling, bioimaging, photothermal therapy and the like, is especially suitable for preparing efficient photosensitive reagent drugs for tumor photothermal therapy, and provides a new strategy for design of near-infrared photothermal diagnosis and treatment materials.
Owner:NINGBO INST OF DALIAN UNIV OF TECH +1

A copper-nitroimidazole complex, its preparation method and application

The application provides a copper-nitroimidazole complex which is self-assembled by coordination of copper ions and 2-nitroimidazole. The complex only contains copper ions and 2-nitroimidazole, and the simple two-component combination can realize the chemical kinetics treatment of GSH metabolism enhancement and induce iron death. The copper-nitroimidazole complex has GSH response and hypoxia responsiveness as a nanodrug, and can selectively act in tumor cells. The nanodrug releases copper ions and 2-nitroimidazole in tumor cells, 2-nitroimidazole consumes NADPH under hypoxic conditions to hinder the synthesis of GSH, and copper ions also consume GSH. The consumption of GSH enhances the Cu 2+ / Cu + mediated Fenton reaction to produce active oxygen. 2-nitroimidazole and copper ions self-assemble to form a nanodrug, which greatly improves the loading capacity of 2-nitroimidazole.
Owner:CHANGCHUN INSTITUTE OF APPLIED CHEMISTRY CHINESE ACADEMY OF SCIENCES

Use of compound in preparation of drug for treatment or prevention of mycobacterium tuberculosis infection

PendingUS20260191965A1NitroimidazoleMetabolite
The present invention provides use of a rifamycin-nitroimidazole conjugate molecule, or deuterated derivatives thereof, metabolites thereof, pharmaceutically acceptable salts thereof, or prodrugs thereof in the preparation of a drug for the treatment or prevention of a disease caused by Mycobacterium tuberculosis infection. The rifamycin-nitroimidazole conjugate molecule has a structure represented by formula I.The rifamycin-nitroimidazole conjugate molecule or the deuterated derivatives thereof, the metabolites thereof, the pharmaceutically acceptable salts thereof, or the prodrugs thereof in the present invention inhibit Mycobacterium tuberculosis comprising multi-drug-resistant (MDR) and extensive drug-resistant Mycobacterium tuberculosis (XDR-TB), and then are used for treating or preventing infections and a disease caused by Mycobacterium tuberculosis.
Owner:TENNOR THERAPEUTICS (ZHONGSHAN) LIMITED

A method for preparing a nitroimidazole phosphate compound

The application aims to provide a preparation method of high-purity phosphonic acid levonikosazol ester disodium hydrate, which has the advantages of controllable reaction condition, stable quality, high yield and suitability for industrial production, etc.
Owner:JIANGSU ZHONGWEIKANG PHARM RES & DEV CO LTD

Hypoxia targeting hyaluronic acid nano delivery system as well as construction method and application thereof

The invention relates to a hypoxia targeting hyaluronic acid nano delivery system and a construction method and application thereof, the construction method comprises the following preparation method: S1, dissolving 2-nitroimidazole and K2CO3 in dimethylformamide, carrying out high temperature alkali treatment, adding N-Boc-bromoethylamine, and carrying out high temperature reaction to obtain Boc-NIH; s2, dissolving the Boc-2-NIH in dichloromethane, adding trifluoroacetic acid for deprotection, and adjusting the pH value to be neutral, so as to obtain 2-NIH; s3, dissolving HA in deionized water, sequentially adding EDC and NHS to activate carboxyl, then adding 2-NIH, reacting at room temperature, and dialyzing to obtain a hypoxic targeting hyaluronic acid nano delivery carrier HA-NIH; s4, HA-NIH loads a drug, and the hypoxia targeted hyaluronic acid nano delivery system is formed. According to the invention, a bifunctional nano system with CD44 active targeting and hypoxia response release is successfully constructed, a dynamic regulation and control mechanism of HA molecular weight on a targeting-permeation-retention effect is provided, and a synergistic effect of tumor stem cell microenvironment specific response and drug space-time release is realized.
Owner:SHANGHAI UNIV OF MEDICINE & HEALTH SCI

Method for inhibiting clostridioides difficile spore germination

Oxadiazole antibiotics that exhibit bactericidal activity against C. difficile vegetative cells. We screened a library of 75 oxadiazoles against C. difficile ATCC 43255. The findings from this collection served as the basis for the syntheses of an additional 58 analogs, which were tested against the same strain. We discovered a potent (MIC50=0.5 μg / mL, MIC90=1 μg / mL for 101 C. difficile strains) and narrow-spectrum oxadiazole (3-(4-(cyclopentyloxy)phenyl)-5-(4-nitro-1H-imidazol-2-yl)-1,2,4-oxadiazole; compound 57) that is not active against common gut bacteria or other tested organisms, but is selectively bactericidal against C. difficile and targets cell-wall synthesis. Other similarly effective oxadiazole antibiotics of formula I and II are described herein, several of which inhibit or prevent C. difficile spore germination.
Owner:UNIV OF NOTRE DAME DU LAC

Semi-solid electrolyte and preparation method and application thereof

The invention relates to a semi-solid electrolyte and a preparation method and application thereof, and belongs to the technical field of lithium ion secondary batteries. The semi-solid electrolyte provided by the invention is prepared from a polymerizable monomer, a lithium salt, an initiator and a deep eutectic solution according to a specific proportion. The deep eutectic solution is composed of a hydrogen bond acceptor and a hydrogen bond donor containing nitryl. Wherein the hydrogen bond acceptor is a lithium salt, and the hydrogen bond donor is one or more of a nitrourea-containing material, a nitrosulfonyl-containing material and a nitroimidazole-containing material. By introducing the deep eutectic solution into the semi-solid electrolyte, the movement capability of a polymer chain segment can be improved, so that the ionic conductivity of the semi-solid electrolyte at room temperature is improved. In addition, a nitro-containing hydrogen bond donor in the deep eutectic solution is beneficial for forming a stable solid electrolyte interface film on the interface of the negative electrode and the positive electrode. When the electrolyte is applied to the lithium ion battery, the electrolyte shows good stability with a positive electrode and a negative electrode, and the cycling stability of the battery can be improved.
Owner:SUN YAT SEN UNIV

Fully continuous flow preparation method and system of nitroimidazole antibacterial drug

The invention belongs to the technical field of pharmaceutical chemicals, and particularly relates to a fully continuous flow preparation method and system of nitroimidazole antibacterial drugs. According to the method, glyoxal is taken as a starting raw material, a full-continuous device system consisting of a plurality of micro-mixers, micro-reactors, gas-liquid separators and on-line solvent switching and low-boiling-point reagent feeding equipment which are communicated in sequence is used, and the high-purity nitroimidazole antibacterial drugs are obtained through multi-step chemical reaction and continuous post-treatment processes. The sulfuric acid and formic acid are recycled and reused, the use amount of the sulfuric acid can be reduced by more than 60%, the generation of waste acid and waste salt is effectively reduced, the production efficiency and the process control accuracy are greatly improved, the stable product quality is ensured, and the production cost is reduced.
Owner:JIANGXI NORMAL UNIV

A compound ophthalmic in situ gel composition for treating ocular Demodex mite infection, its preparation method and application.

PendingCN122123969ASenses disorderAntibacterial agentsNitroimidazolePyrrolidinones
This invention belongs to the field of pharmaceutical formulations and relates to a compound ophthalmic in-situ gel composition for treating ocular Demodex mite infection, its preparation method, and its application. By weight percentage, the compound ophthalmic in-situ gel composition for treating ocular Demodex mite infection comprises 0.1-2.0% of a nitroimidazole compound, 0.05-3.0% of an isoxazoline compound, 0.1-1.5% of a gelling polymer, 1.0-8.0% of a complex solubilizing system, 0.1-3.0% of pharmaceutically acceptable excipients, and the balance being water. The complex solubilizing system includes polyvinylpyrrolidone and cyclodextrin derivatives. This invention effectively solves the problem of poor solubility of isoxazoline drugs through a complex solubilizing system, and the combination of the two drugs has a significant synergistic acaricidal effect. Combined with a gelling polymer, it can achieve in-situ gelation on the ocular surface, prolong retention, and sustained drug release, with low ocular irritation, providing a highly effective, long-lasting, and safe new local treatment option for Demodex mite-related eye diseases.
Owner:XINJIYUAN (BEIJING) PHARM TECH CO LTD

Synthesis method of tetra-substituted (4-nitroimidazole) borane compound

The invention discloses a synthesis method of a tetra-substituted (4-nitroimidazole) borane compound, which comprises the following steps: adding anhydrous CH2Cl2 into a single-mouth flask at-20 DEG C, mixing 4-nitroimidazole with the anhydrous CH2Cl2, quickly injecting BCl3, and stirring; the subsequent reaction is detected through 11B NMR to ensure that BCl3 is completely converted; after filtering, washing by using a mixed solution of ethanol and acetonitrile, and filtering and drying to obtain white powder, namely a target compound with a structural formula as shown in the specification. The tetra-substituted (4-nitroimidazole) borane compound disclosed by the invention is relatively good in density sensitivity, relatively simple in synthesis method and relatively mild in reaction condition.
Owner:XIAN MODERN CHEM RES INST

Preparation method and application of nitro-functionalized ZIF-25-mnImx material

The invention discloses a preparation method of a nitro-functionalized ZIF-25-mnImx material and application of the nitro-functionalized ZIF-25-mnImx material in separation of acetoin and 2, 3-butanediol, and belongs to the field of inorganic functional materials. The preparation method comprises the following steps: mixing and dissolving 4, 5-dimethylimidazole (dmeIm), 4-methyl-5-nitroimidazole (mnIm) and Zn (OAc) 2.2 H2O in methanol, and reacting at 120 DEG C for 24 hours; and after the reaction is finished, washing an obtained yellowish-brown sample with methanol for multiple times, and filtering and drying at room temperature to obtain the ZIF-25-mnImx material. The nitro-functionalized ZIF-25-mnImx provided by the invention has relatively high adsorption capacity on acetoin in a biological fermentation liquid, so that the separation cost of the biological fermentation liquid is reduced; due to the existence of a competitive mechanism, acetoin is preferentially adsorbed in a mixed solution, so that the method is suitable for separating acetoin and 2, 3-butanediol from a low-concentration aqueous solution, and has a wide application prospect.
Owner:TAIYUAN UNIVERSITY OF TECHNOLOGY

Novel Phenyl Derivatives

PendingJP2026086513AOrganic active ingredientsOrganic chemistryNitroimidazoleDisease
We provide safe mitochondrial uncoupling agents. [Solution] The present invention provides 5-[(2,4-dinitrophenoxy)methyl]-1-methyl-2-nitro-1H-imidazole, a novel phenyl derivative, or a pharmaceutically acceptable salt thereof. This compound is useful for regulating mitochondrial activity, reducing obesity, and treating diseases including diabetes and diabetic complications.
Owner:RIVUS PHARMACEUTICALS INC

Method for continuously synthesizing 2-methyl-5-nitroimidazole based on microchannel reactor

PendingCN121471146AOrganic chemistryNitroimidazoleAcetic acid
The invention relates to the field of fine chemical engineering, and discloses a method for continuously synthesizing 2-methyl-5-nitroimidazole based on a microchannel reactor, which comprises the following steps: 1) mixing 2-methylimidazole with concentrated sulfuric acid to obtain a mixture A; 2) mixing fuming nitric acid with glacial acetic acid to obtain a mixture C; 3) taking acetic anhydride as a material B, simultaneously, respectively and continuously conveying the mixture A, the material B and the mixture C into a microchannel reactor for nitration reaction, and controlling the temperature to be 10-30 DEG C; 4, quenching reaction is conducted after the reaction, solids are neutralized and separated out, and filtering, washing and drying are conducted to obtain the 2-methyl-5-nitroimidazole. According to the method, a low-temperature nitration system (10-30 DEG C) is adopted, yellow smoke can be prevented from being generated, the oxidation reaction can still be effectively inhibited under the condition that ammonium sulfate is not added, and therefore the purity and yield of the product can be effectively improved.
Owner:ZHEJIANG WEILONG TECHNOLOGY CO LTD

A potential genotoxic impurity in a morpholine nitazoxanide raw material and formulations thereof, and methods of making and using the same

ActiveCN120172918BOrganic chemistryComponent separationNitroimidazoleNitroso
The present application relates to the technical field of medicine, in particular to a potential genotoxic impurity in a morpholine nitroimidazole raw material and preparation and a preparation method and application thereof.The potential genotoxic impurity is 2-methyl-5-nitro-1-nitrosoimidazole.A new structure compound 2-methyl-5-nitro-1-nitrosoimidazole of diazoles is found in the synthesis process of the morpholine nitroimidazole raw material for the first time.The compound is identified as a potential genotoxic impurity because of containing a nitrosamine warning structure.A method for analyzing the potential genotoxic impurity 2-methyl-5-nitro-1-nitrosoimidazole by using ultra-high performance liquid chromatography-mass spectrometry is established for the first time, which is of great significance to the quality control of the morpholine nitroimidazole raw material and preparation.The detection method provides a reference for the quality evaluation of other starting materials, intermediates and raw materials that can produce 2-methyl-5-nitro-1-nitrosoimidazole.
Owner:SHANDONG INST FOR FOOD & DRUG CONTROL +1

Method and system for fully continuous-flow preparation of nitroimidazole antimicrobial agent

A method for fully continuous-flow preparation of a nitroimidazole antimicrobial agent using a fully continuous-flow system is provided herein. The method adopts a raw material of a glyoxal aqueous solution, an acetaldehyde aqueous solution and an ammonium hydroxide solution followed by multi-step chemical reactions and continuous post-treatments to yield a nitroimidazole antimicrobial agent with a high purity. The fully continuous-flow system for implementing the method includes a plurality of micromixers, a plurality of microreactors, a plurality of back pressure valves, a plurality of gas-liquid separators, a first plurality of online solvent switching units and a feed unit.
Owner:FUDAN UNIVERSITY

Synthesis of a novel heterogeneous photocomposite catalyst ZnCo2O4 / g-C3N4 / Cu for the treatment of water and wastewater pollutants

UndeterminedIR114120BNitroimidazolePhotocatalytic reaction
Design and synthesis of a new heterogeneous photocomposite catalyst ZnCo2O4 / g-C3N4 / Cu for the treatment of water and wastewater pollutants. This invention is related to the field of environment and can remove some persistent and organic pollutants of water and wastewater, such as some pharmaceutical pollutants (antibiotics). Therefore, there are various methods for the destruction and removal of pollutants, and advanced oxidation processes are an effective and efficient technology for the decomposition and destruction of dangerous, non-degradable and resistant organic pollutants. The main mechanism of this method is oxidation-reduction reactions and the production of highly active species. Among advanced oxidation processes, the use of photocatalytic reactions has been considered as an environmentally friendly method. In the present work, the design and synthesis of a new heterogeneous photocomposite catalyst ZnCo2O4 / g-C3N4 / Cu in the field of water and wastewater treatment was able to remove and destroy some pollutants such as a number of antibiotics (nitroimidazole group). This method is economical, recyclable and reusable, non-toxic, high production speed and also produces safe materials at the end of the reaction.

Administration of tailored feedstock to increase antibiotic susceptibility

A method for increasing susceptibility of microorganisms to antibiotics includes providing a microorganism; administering a single type of an antibiotic including a nitroimidazole compound to the microorganism; and administering any of an uronic, aldonic, ulosonic, and aldaric feedstock to the microorganism. The feedstock is adapted to promote cell metabolism and antibiotic activation, and inhibit antibiotic inactivation pathways in the microorganism causing increased sensitivity of the microorganism to the nitroimidazole.
Owner:UNITED STATES OF AMERICA THE AS REPRESENTED BY THE SEC OF THE ARMY

Amphiphilic molecule of diselenide bond linked nitroimidazole and polyethylene glycol and application of amphiphilic molecule

The invention discloses an amphiphilic molecule with diselenide bond linked nitroimidazole and polyethylene glycol and application of the amphiphilic molecule, and belongs to the technical field of medicine. The invention provides an amphiphilic molecule MNZ-Se2-PEG linked with nitroimidazole and polyethylene glycol through a diselenide bond. The structural formula of the amphiphilic molecule MNZ-Se2-PEG is as shown in (I). The amphiphilic molecules can entrap chemotherapeutic drugs through self-assembly to form a drug delivery system. The prepared drug delivery system has the advantages of being capable of keeping the structure stable under physiological conditions, releasing drugs through radiation responsiveness, enhancing sensitivity through radiotherapy and the like, and plays a role in radiotherapy and chemotherapy synergistic treatment. And the prepared drug delivery system has good biological safety. The invention provides a reliable carrier platform for realizing synergistic interaction of chemoradiotherapy, and has excellent development potential of a chemotherapy drug delivery system.
Owner:ZHEJIANG UNIV

Markers, conjugates, compositions and methods for hypoxia imaging, mapping, and therapy

Described herein are markers, conjugates, compositions and methods for hypoxia imaging, mapping, and therapy. A compound comprising bio-reductively activated (BA) arm, linker arm and a mapping click wherein BA contains one for more of substituted or unsubstituted 2 / 4 / 5-substituted nitroimidazoles, or substituted benzotriazene-1,4-dioxides, or substituted 1,2,3 / 1,2,4-triazoles, or substituted 1,4-benzoquinones, or a combination of two homo-or hetero BA moieties, wherein linker arm contains C1-16 alkane, alkene, alkyne, alicyclic or aromatic linkers with or without hetero atoms as in ethers, amine, esters, acid, amides, 5 and 6 membered sugar sings with the substitution as described above, both monosaccharides and disaccharides, wherein mapping click contains one of substituted or unsubstituted —N3-, CN, SCN, substituted alkynes for click chemistry. Said compound undergoes in situ click reaction after its distribution in cells or tissues to link to a reporting group which may be unchelated or chelated with a metal-radioactive or non-radioactive-, or a radiohalogen for PET / SPECT, or a dye for fluorescent / optical reporting group, thus accomplishing hypoxia imaging.
Owner:WWIKY BIOSCIENCES INC

Process for the synthesis of isomeric derivatives of alvocidib

ActiveCN117777196BGroup 5/15 element organic compoundsNitroimidazoleDiisopropyl azodicarboxylate
The application belongs to the field of medicine synthesis, and specifically provides a synthesis method of alovudine isomer derivative. 4-nitro-1H-imidazole is used as raw material, substitution, elimination and reduction reaction are carried out to generate (1-alkyl-4-nitro-1H-imidazol-5-yl)methanol; then 2-haloethylamine halide acid salt and phosphorus oxychloride are reacted to generate N,N'-bis(2-haloethyl) diaminophosphonic acid; finally, (1-alkyl-4-nitro-1H-imidazol-5-yl)methanol, N,N'-bis(2-haloethyl) diaminophosphonic acid, triphenylphosphine and anhydrous tetrahydrofuran are added into a reaction bottle, the system is reduced to 0 DEG C, diisopropyl azodicarboxylate (DIAD) is added dropwise, the temperature is increased to 25 DEG C, reaction is carried out for 3h, and then the crude product is obtained through concentration under reduced pressure, and alovudine isomer derivative is obtained through purification through a silica gel column.
Owner:CHANGZHOU UNIV

Crystalline forms of 5-[(2,4-dinitrophenoxy)methyl]-1-methyl-2-nitro-1h-imidazole

The present disclosure relates to polymorphic forms of 5-[(2,4-dinitrophenoxy)methyl]-1-methyl-2-nitro-1H-imidazole for treating various disorders or conditions, including mitochondria-related disorders or conditions and cardiovascular disorders or conditions.
Owner:RIVUS PHARMACEUTICALS INC

Preparation of novel ferroptosis micelle capable of consuming NADPH (Nicotinamide Adenine Dinucleotide Phosphate)

PendingCN121550152AEnergy modified materialsPharmaceutical non-active ingredientsTirapazamineNitroimidazole
The invention discloses preparation and application of a novel ferroptosis micelle capable of consuming NADPH (Nicotinamide Adenine Dinucleotide Phosphate). The micelle is formed by self-assembly of an amphiphilic copolymer mPEG-Azo-P (Asp-NI)-Ce6, a hydrophilic segment is mPEG and is connected with a hydrophobic segment P (Asp-NI) through an azobenzene connecting bridge with hypoxia response, and the hydrophobic segment contains a nitroimidazole group with dual response to hypoxia and singlet oxygen and is bonded with a photosensitizer Ce6. The micelle can be further used for physically encapsulating a hypoxia activated prodrug terapazamine. The micelle disclosed by the invention can respond to a hypoxia condition in a tumor microenvironment to realize PEG shedding and enhance cellular uptake; meanwhile, singlet oxygen generated by photodynamic therapy is responded, so that micelle disintegration and quick release of the medicine are realized. By combining the Ce6-mediated photodynamic therapy and the PDT-activated TPZ chemotherapy, the synergistic anti-tumor effect is achieved. The invention also provides a preparation method of the micelle, which is simple and convenient to operate and good in reproducibility. The nano platform provides a new strategy for efficient co-delivery of the photosensitizer and the chemotherapeutic drug, and particularly shows a good application prospect in breast cancer treatment.
Owner:BENGBU MEDICAL COLLEGE

N-oxygenase ancestor enzyme and application thereof

PendingCN121518414ABacteriaMicroorganism based processesNitroimidazoleOxygenase
The invention discloses an N-oxygenase ancestor enzyme and application thereof, and belongs to the technical field of biological catalysis. According to the invention, seven N-oxygenase ancestors with relatively high catalytic performance are obtained through an ancestor reconstruction method; the N, N-oxygenase ancestor enzyme can catalyze 2-aminoimidazole to synthesize 2-nitroimidazole, and the yields of 2-nitroimidazole synthesized within the same time are 4.0 times, 1.4 times, 1.1 times, 1.2 times, 2.1 times, 1.3 times and 1.7 times of those of a control enzyme respectively; wherein the catalytic capacity of ASR90 is the highest and is 4.0 times that of known N-oxygenase double mutant enzyme with the highest catalytic activity; according to the method, the N-oxygenase is used as a catalyst, the in-vitro catalytic reaction is carried out for 20 minutes, and the concentration of the 2-nitroimidazole obtained by catalyzing the 2-aminoimidazole is 142.9 M. The problems that the existing N-oxygenase is insufficient and the synthesis efficiency of the 2-nitroimidazole is insufficient are solved.
Owner:DALIAN INSTITUTE OF CHEMICAL PHYSICS CHINESE ACADEMY OF SCIENCES

A continuous flow synthesis of secnidazole

ActiveCN116813554BOrganic chemistryNitroimidazoleOrganic synthesis
The application belongs to the technical field of organic synthesis, and particularly relates to a continuous flow synthesis method of secnidazole. The continuous flow synthesis method comprises the following steps: step 1, pumping a mixed solution of 2-methyl-5-nitroimidazole, formic acid and concentrated sulfuric acid with a mass fraction of 98%-100% into a continuous flow mixer 1, pumping a toluene solution of propylene oxide into the continuous flow mixer 1, mixing, and then reacting in a continuous flow reactor 1 to obtain a reaction liquid A; step 2, pumping the reaction liquid A into a continuous flow mixer 2, pumping a toluene solution of propylene oxide into the continuous flow mixer 2, pumping concentrated sulfuric acid with a mass fraction of 98%-100% into the continuous flow mixer 2, mixing, and then reacting in a continuous flow reactor 2, collecting a reaction liquid, and separating to obtain a secnidazole product. The method has the advantages of low cost, simple process, safety and green environmental protection, and has a good application prospect.
Owner:ASTATECH (CHENGDU) BIOPHARM CORP

A heteromorphic bifunctional crosslinking agent, a preparation method and application thereof

ActiveCN117658991BPeptide preparation methodsCyclic peptideNitroimidazole
The application provides a heteromorphic bifunctional crosslinking agent and preparation and application thereof. The heteromorphic bifunctional crosslinking agent provided by the application is a bifunctional crosslinking agent containing N-hydroxysuccinimide (NHS) active ester and a dinitroimidazole functional group (DNIm), and can connect together a compound containing amino and a compound containing sulfydryl. The DNIm module of the crosslinking agent provided by the application is more stable than a maleimide module. In addition, the addition product of DNIm and sulfydryl is also more stable than the addition product of maleimide and sulfydryl. In a near neutral buffer, no side reaction product of the addition of DNIm and amino is found through LC-MS analysis, that is, no addition reaction with amino occurs under the condition. The crosslinking agent provided by the application can be applied to the construction of cyclic peptides of different sizes, and the selective single modification of sulfydryl or amino of proteins, including biotinylation, PEGylation or the introduction of fluorescent substances, and the double modification of a single protein molecule, including biotinylation and PEGylation.
Owner:NANCHANG UNIV

A method for removing nitro compounds from water using pyrite-mediated atomic hydrogen reduction.

This invention discloses a method for removing nitro compounds from water by pyrite-mediated atomic hydrogen reduction, comprising the following steps: (1) washing and drying natural pyrite, then grinding it into a gray-black powder catalyst using a ball mill; (2) placing the catalyst in an aqueous solution of nitroimidazole or nitrobenzene at room temperature and pressure, followed by the addition of sodium borohydride, and continuously bubbling the solution with an inert gas; (3) under low catalyst dosage (0.8 g / L) and sodium borohydride dosage (<0.16 g / L), metronidazole, ornidazole with an initial concentration of 20 ppm are completely removed within 1 min, and nitrobenzene with a removal rate of 0.6 mM reaches 98.98% within 20 min, with the main reduction products being the corresponding amino compounds. This invention uses natural pyrite as a catalyst to mediate the generation of atomic hydrogen, with a simple process and safe reagents, providing a practical strategy for reducing nitro compound pollution in the aquatic environment.
Owner:SUN YAT SEN UNIV

A size-controllable zeolite imidazolate framework material and a preparation method thereof

PendingCN122302305ANitroimidazoleEthyl group
This invention discloses a size-controllable zeolite-like imidazole ester framework material and its preparation method. The preparation method includes the following steps: Step 1, dissolving an organic ligand in a solvent to obtain an organic ligand solution; Step 2, adding a metal salt to the organic ligand solution under stirring conditions, and reacting at room temperature to obtain a suspension; Step 3, sequentially centrifuging, washing, and drying the suspension to obtain the zeolite-like imidazole ester framework material. The metal salt is selected from any one or two of cobalt salts and zinc salts. The organic ligand is selected from any one or more of imidazole, 2-methylimidazole, 2-ethylimidazole, 2-nitroimidazole, imidazole-2-carboxaldehyde, and benzimidazole. This invention, without adding other raw materials or changing the reaction conditions, can successfully synthesize zeolite-like imidazole ester framework materials of different sizes simply by precisely controlling the concentration of the reaction precursor (i.e., imidazole derivative and coordinating metal ions). The control mechanism is simple and clear.
Owner:XIAN MODERN CHEM RES INST

Titanium solid catalyst, its preparation method and its application in synthesis of diphenyl carbonate

PendingCN122352363ANitroimidazoleTitanium chloride
This invention belongs to the field of catalytic materials and green organic synthesis technology, and provides a titanium solid catalyst, its preparation method, and its application in the synthesis of diphenyl carbonate. The titanium solid catalyst of this invention is a coordination compound formed by a titanium precursor and an imidazole ligand; the titanium precursor includes one or more of tetrabutyl titanate, tetraisopropyl titanate, titanium tetrachloride, tetraethyl titanate, and titanium acetate; the imidazole ligand includes one or more of imidazole, 2-methylimidazole, 2-ethylimidazole, 2-hydroxyimidazole, 2-aminoimidazole, and 2-nitroimidazole. The titanium solid catalyst of this invention is a solid powder, heterogeneous, insoluble in the reaction system, and can be filtered and recovered, completely solving the problem of the inability to separate liquid titanates. The titanium solid catalyst of this invention has resistance to hydrolysis, aggregation, and deactivation; the imidazole ring strongly coordinates to protect the Ti center, and its stability is far superior to that of titanates and traditional chelates.
Owner:LANZHOU INSTITUTE OF CHEMICAL PHYSICS CHINESE ACADEMY OF SCIENCES