187 results about "Demethylation" patented technology

The invention discloses a method for regulating and controlling the aging process of plant leaves. According to the method, the aging process of the plant leaves is regulated and controlled by regulating and controlling expression of RNA m6A demethylation gene ALKBH10B. Experimental results show that the overexpression RNA m6A demethylation gene ALKBH10B can effectively inhibit the aging of plant leaves; by inhibiting the expression of the RNA m6A demethylation gene ALKBH10B, the aging of plant leaves can be effectively inhibited. The method can break through the limitation of a traditional chemical regulation and control means, and the purposes of improving the crop yield and quality, enhancing the commodity value of ornamental plants and the like are achieved; and the gene involved in the method is highly conservative in different plants, and has strong applicability and great application potential.

The invention belongs to the field of biosensing detection, and particularly relates to an ATP (adenosine triphosphate) nucleic acid aptamer based on m6A epigenetic base modification and application of the ATP nucleic acid aptamer. The invention provides a nucleic acid aptamer and a nucleic acid aptamer sensor. On the basis of recognition and binding specificity of a nucleic acid aptamer probe to a target, a single-point methylation closed switch type functional probe is constructed, and living cell and living body imaging detection of endogenous demethylase is realized. Taking ATP and an aptamer thereof as an example, m6A methylation modifies key sites of the aptamer so as to influence the binding stability between the aptamer and a ligand, after endogenous FTO demethylation, the aptamer recovers active sites, can be rapidly bound with ATP and is driven to allosteric to release fluorescence, and in-situ instant detection of FTO is realized.

The invention discloses a demethylase ODM gene for synthesizing benzylisoquinoline alkaloids and application thereof, the demethylase ODM gene is an ODM1 gene or an ODM2 gene, the nucleotide sequence of the CDS region of the ODM1 gene is shown as SEQ ID NO: 1, and the nucleotide sequence of the CDS region of the ODM2 gene is shown as SEQ ID NO: 2. Aiming at the current situation that the research basis of a key gene for synthesizing corydalmine in rhizoma corydalis is weak, the ODM1 gene for catalyzing tetrahydropalmatine demethylation to specifically generate corydalmine and tetrahydrojatrorrhizine and the ODM2 gene for specifically generating tetrahydrojatrorrhizine are cloned from rhizoma corydalis for the first time. An important theoretical basis is provided for producing the corydalmine by utilizing a synthetic biological method in the future, and the corydalmine mutant has a wide application prospect and a great economic value.

The invention discloses a preparation method of an itramod intermediate, and relates to the technical field of preparation of compounds. The synthesis method of the etramod intermediate comprises the following steps: providing a compound A, replacing hydrogen in an N-H group on the compound A with a compound B, then carrying out a substitution reaction with a compound C containing a halogen substituent group to generate a compound D, and carrying out hydrolysis, decarboxylation, demethylation and esterification reaction on the compound D to obtain the etramod intermediate. The preparation method of the itramod intermediate provided by the invention is high in yield, and the obtained itramod intermediate is high in purity, low in cost and easy to popularize and use.

The invention provides a preparation method of 6-benzofuran phenol, which comprises the following steps: step S1, 6-hydroxy-2H-benzofuran-3-ketone and a methylation reagent are subjected to a reaction to generate 6-hydroxymethyl-2H-benzofuran-3-ketone, and the methylation reagent is one or more of dimethyl sulfate, methyl iodide, dimethyl carbonate and the like; step S2, enabling the 6-hydroxymethyl-2H-benzofuran-3-ketone to react with a reducing agent, so as to generate 6-hydroxymethyl-2H-benzofuran-3-alcohol; s3, the 6-hydroxymethyl-2H-benzofuran-3-alcohol is subjected to a demethylation reaction and an elimination reaction, and the 6-benzofuran phenol is generated. According to the preparation method of the 6-benzofuran phenol, the phenolic hydroxyl group is protected by methyl, demethylation and alcohol elimination are completed by a one-pot method, and an intermediate product has few impurities and is simple to purify.

The invention discloses a method for demethylating C9 < + > aromatic hydrocarbon. The method comprises the following step: in the presence of hydrogen, carrying out contact reaction on a C9 < + > aromatic hydrocarbon raw material and an aromatic hydrocarbon dealkylation catalyst to obtain an aromatic hydrocarbon dealkylation material flow. According to the method, the dealkylation reaction can be fully utilized to realize demethylation of the C2 + side chain of the C9 + aromatic hydrocarbon, so that the number of methyl groups in the aromatic hydrocarbon material flow is increased, and the methyl / benzene ring ratio of a transalkylation unit is increased.

The invention provides a preparation method of a nitrosamine impurity, and belongs to the technical field of heterocyclic compounds. The clarithromycin related nitrosamine impurity is 3 '-N-demethyl-3'-N-nitroso-6-O-methyl erythromycin, and is prepared by carrying out demethylation and nitrosation on clarithromycin. The clarithromycin intermediate erythromycin oxime related nitrosamine impurity is 3 '-N-demethyl-3'-N-nitroso erythromycin A (E)-9-oxime, and the clarithromycin intermediate erythromycin oxime related nitrosamine impurity is prepared from erythromycin A (E)-9-oxime through demethylation, etherification, nitrosation and hydrolysis.

The invention belongs to the technical field of drug synthesis, and relates to a dotenorad synthesis method, which comprises: weighing 100 g of a compound 1 as a raw material, and carrying out a substitution reaction with dimethyl sulfate to obtain a compound 2; taking the compound 2 as a raw material, and carrying out esterification reaction with methanol under an acidic condition; taking the compound 3 as a raw material, and obtaining a compound 4 after chlorination; hydrolyzing the compound 4 serving as a raw material to obtain a compound A; reacting the compound 5 serving as a raw material with a formaldehyde aqueous solution to obtain a compound 6; taking the compound 6 as a raw material, and performing thioether oxidation to obtain a compound B; taking a compound A as a raw material, and carrying out amide condensation reaction with a compound B to obtain a compound C; and 6, demethylating the compound C serving as a raw material under the action of lithium chloride to obtain a compound D, namely the final product dotenorad. According to the synthesis method of dotenorad, oxidation after condensation is not needed, generation of by-products is avoided, raw materials are low in cost and easy to obtain, and the synthesis method is suitable for industrial production.

The invention discloses a high-barrier polypropylene material, a preparation method thereof and application of the high-barrier polypropylene material in an organic silica gel sealing packaging material, and relates to the technical field of high polymer materials. When the high-barrier polypropylene material is prepared, firstly, polypropylene is grafted with dichloro (vinyl) phosphine and vinylmethylsilane and then reacts with 1-ethylene-1H-pyrrole to obtain modified polypropylene, secondly, pretreated montmorillonite is subjected to demethylation through aluminum chloride and then reacts with 2-chloro-5-(1H-pyrrole-1-yl) pyridine to obtain the high-barrier polypropylene material. Then carrying out a reaction with N-triethyl-(4-vinylbenzyl) ammonium to obtain modified montmorillonite; and finally, mixing the modified polypropylene and the modified montmorillonite to obtain the high-barrier polypropylene material. The high-barrier polypropylene material prepared by the invention has high barrier rate, flame retardant property and ultraviolet aging resistance.

The invention provides a preparation method of dotenorad. The preparation method comprises the following steps: (1) carrying out cyclization reaction on SM1 and paraformaldehyde under the action of an activating agent and a solubilizer to obtain Int1; (2) carrying out substitution reaction on the Int1 and SM2 to obtain Int2; (3) carrying out oxidation reaction on the Int2 and an oxidizing agent in the presence of a catalyst to obtain Int3; and 4, carrying out a demethylation reaction on the Int3 and lithium chloride to obtain dotenorad. The purity and the yield of the dotenorad prepared by the method are greatly improved, the cost is reduced, and the method is suitable for industrial mass production.

The invention discloses a preparation process of high-purity dotenorad, and belongs to the technical field of organic synthesis route design and raw material medicine and intermediate preparation. Benzothiazole is used as a starting material, reduction, acylation, amide condensation, oxidation, demethylation and other reactions are sequentially carried out, a dotenorad crude product is synthesized, and the required crystal form is obtained through recrystallization. The raw materials of the preparation method are cheap, easy to obtain and high in stability, the defect that the raw materials of other preparation processes are poor in stability is overcome, and the preparation method is convenient to operate and suitable for industrial production; the total yield of the prepared dotenorad in each step is 66.80%, and the purity of the dotenorad can reach 99.99%.

The invention relates to sgRNAs for demethylation editing of an fgf2 gene of oryzias melastigma, an editing system and application, and belongs to the technical field of gene editing, and the sgRNAs are sgRNA1 + sgRNA2 + sgRNA3 or sgRNA2 + sgRNA3 + sgRNA4 + sgRNA5; the system comprises a Fuw-UbC-dCas9-tet1 plasmid and a pGL3-U6-sgRNAs plasmid, and the sequence of a conserved structural domain of a tet1 gene is as shown in SEQ ID NO. 1 (sequence identifier number 1). Through co-transfection of Mix1 or Mix2, the DNA methylation level of the fgf2 gene promoter can be effectively reduced by about 20.41% at most, the off-target efficiency is extremely low, the cell growth speed is remarkably increased, and stable inheritance is achieved.

The present application relates to the technical field of pharmaceutical chemistry, and particularly relates to a preparation method of fenofibrate and impurities thereof. The present application carries out Friedel-Crafts acylation reaction on 4-chlorobenzoyl chloride, anisole, Lewis acid and benzene solvent, then carries out demethylation reaction, and then separates and purifies to obtain compound II, impurity compound IV and impurity compound V; the compound II (or impurity compound IV), 2-bromoisobutyric acid isopropyl ester, an alkaline reagent and an alcohol solvent are mixed to carry out etherification reaction, and then separated and purified to obtain fenofibrate (or impurity compound VI). The preparation method provided by the present application has high yield and high purity of fenofibrate, can realize identification of impurities in the preparation process of fenofibrate, and provides a convenient condition for quality control of bulk drug. Moreover, the raw materials and solvents used are widely sourced, low in cost and small in danger, the preparation method is high in safety factor, simple in operation, and suitable for large-scale industrial production.

The invention relates to the technical field of chemical synthesis, and discloses a preparation method and control of an abelsiril impurity A, namely 6-(4-chloro-5-fluoropyrimidine-2-yl)-4-fluoro-1-isopropyl-2-methyl-1H-benzimidazole. The preparation method comprises the following steps: S1, carrying out aromatic nucleus nucleophilic substitution reaction on a compound I and a nucleophilic reagent in an organic reagent, washing an organic phase, drying, filtering, and drying to obtain a compound II; concentrating under reduced pressure to obtain a compound II; s2, mixing the compound II, the compound III, a palladium catalyst, alkali and an organic solvent, performing heating reflux under the protection of nitrogen, performing Suzuki coupling reaction, performing vacuum concentration, and washing a filter cake with tetrahydrofuran to obtain a compound IV; s3, carrying out demethylation reaction on the compound IV to obtain a compound V; s4, the compound V reacts with a chlorination reagent, reduced pressure distillation is conducted, separation and purification are conducted, and the abelsilib impurity A is obtained. The design route provided by the invention is reasonable, the reaction site selectivity is good, and the impurity A with relatively high purity can be obtained.

This invention relates to the field of medicinal chemistry, and in particular to a method for preparing gaticycline esters. The method for preparing gaticycline esters provided by this invention includes the following steps: reacting compound I, an acid-binding agent, and a solvent to obtain the gaticycline ester; the structural formula of compound I is: [structural formula missing]; the particle size of the acid-binding agent is ≤48 μm. The method for preparing gaticycline esters of this invention avoids the degradation and demethylation reaction of the generated gaticycline ester, thereby avoiding the generation of impurity compounds, and can obtain gaticycline esters with high yield and high purity.

This invention provides a method for synthesizing the anti-AIDS drug enovirine. This invention belongs to the field of pharmaceutical preparation technology. The synthesis method includes the following steps: (1) SM1 compound reacts with Grignard reagent and then reacts with SM2 compound to obtain compound III; (2) Compound III undergoes oxidation reaction to obtain compound II; (3) Compound II undergoes demethylation reaction under the action of demethylation reagent to obtain compound I; (4) Compound I undergoes ethylation reaction to obtain enovirine. The synthesis route of this invention effectively avoids the use of highly toxic cyanide reagents and expensive heavy metal catalysts. At the same time, the reaction conditions of this route are simple and mild, with high yield, and have excellent industrialization prospects.

The present application relates to the field of medicine synthesis, and discloses a preparation method and application of brominated piperonal carboxylic acid, wherein the brominated piperonal carboxylic acid compound is prepared from o-vanillin as a starting material through acetyl protection, bromination reaction, deprotection and demethylation reaction, cyclization reaction and Pinnick oxidation reaction.No longer through a brominated piperonal intermediate, and without using a live LDA reagent low-temperature lithiation reaction, the safety and stability are greatly improved.The deprotection and demethylation reaction is carried out in one pot, and the use of boron tribromide and other reagents is avoided;finally, the oxidation step from aldehyde to acid avoids using traditional silver oxide or potassium permanganate oxidation, and adopts Pinnick oxidation, which is economic, environmental protection and cost reduction, and greatly improves the yield.The whole has the advantages of easy-to-obtain raw materials, short steps, mild reaction conditions, low production cost, environmental protection, high yield and high purity, and can meet the high quality requirements of pharmaceutical products.

The present application relates to a kind of from androsta 1, 4-diene-3, 17-dione starting synthesis of estren and the method of a kind of compound thereof.Especially, the present application provides a kind of preparation method of estren shown in formula I, comprising the following steps: in inert solvent, androsta-1, 4-diene-3, 17-dione (II) with reagent R4VX carries out demethylation aromatization reaction step directly to obtain estren (I);Wherein, the definition of reaction substrate, reagent and reaction condition is as claimed in claim or specification.The method is simple in operation, and good in selectivity, and product purity is high, suitable for industrial production.

The invention provides application of GW5 gene promoter methylation based on a multi-omics gene mining technology in regulation and control of rice grain length, and relates to the technical field of biology. On the basis of a generic genome micro-core germplasm population, multi-dimensional omics data such as a genome and an epigenome are integrated, a rice epigenome map is constructed, a stable methylation polymorphism marker in the map is utilized, a rice grain width phenotype is combined to carry out multi-omics association analysis, a new epigenetic allele of the GW5 gene is successfully mined, and the GW5 gene is successfully identified. It is found that the upstream promoter region of the GW5 gene has two epigenetic states of hypermethylation and hypomethylation in different rice germplasm backgrounds, and after demethylation editing is carried out on the region, the phenotype that the grain length is remarkably increased is shown. Therefore, detection of the rice grain length character can be realized according to the promoter methylation level of the GW5 gene, and regulation and control of the rice grain length character can be realized by regulating and controlling the promoter methylation level of the GW5 gene.

The invention discloses THK01 and derivatives thereof, a preparation method and application of THK01 and derivatives thereof in preparation of anti-inflammatory drugs, and the THK01 and derivatives thereof are prepared by performing a series of chemical reactions on o-nitrobenzaldehyde containing a specific substituent group, including Wittig reaction, Diels-Alder reaction, Cadolan reaction, Fischer indole synthesis reaction, demethylation reaction, reduction reaction, click chemical reaction and the like. The THK01 structure modified derivatives with different substituent groups are obtained. The THK01 structure modified derivative disclosed by the invention is diversified in synthetic route and high in reaction success rate; in-vitro and in-vivo experiments show that the compounds can significantly inhibit NO generation and inflammatory response at low concentration, and can effectively treat inflammatory bowel disease and acute pneumonia induced by H1N1 virus in an animal model. These findings provide valuable candidate compounds and new treatment strategies for developing novel, safe and efficient anti-inflammatory drugs.

The invention discloses a method for demethylating a lignin derivative, which comprises the following steps of: adding the lignin derivative into an acidic eutectic solvent, stirring and reacting for 0.1-72 hours at 60-200 DEG C, cooling after the reaction is finished, and extracting and separating a product by adopting an organic solvent and water. The acidic deep eutectic solvent is composed of hydrogen bond acceptor choline chloride and hydrogen bond donor p-toluenesulfonic acid, citric acid, oxalic acid dihydrate and the like, the reaction condition of the conversion process is mild, the deep eutectic solvent can be recycled, the cost is reduced, the method is environment-friendly, and the obtained demethylation product can be used as chemicals or can be further converted to prepare materials. And the method has relatively high economical efficiency and application prospect.

The invention discloses a method for separating and purifying a thiourea polymer in a demethylation compound, which comprises the following steps: mixing the thiourea polymer in a demethylation product with water, heating the obtained mixed solution to 80-90 DEG C, and keeping the temperature for 4-6 hours, so that the thiourea polymer impurity in the product is dissolved in hot water; carrying out solid-liquid separation on the obtained solid-liquid mixture to obtain a solid substance demethylated compound, wherein the demethylated substance does not contain the thiourea polymer; the water phase is cooled to the room temperature, a product is separated out, another solid phase is the thiourea polymer, and the mass percent of the thiourea polymer in the demethylation substance is smaller than 0.05%. According to the method, the demethylation compound and the impurity thiourea polymer are separated and purified by utilizing the characteristics that the solubility of the demethylation compound in water is small, and the thiourea polymer is dissolved in water. Experimental results show that the method provided by the invention can effectively improve the purity and content of demethylated substances, and is low in production cost, green and environment-friendly.

The present invention relates to a complex comprising i) a catalytically inactive site-specific nuclease linked to ii) an array of between two and ten, preferably three to seven effector domains each having a specific chromatin modifying activity, such as, for example, a specific DNA methylation activity, a histone methylation activity, a specific histone acetylation or ubiquitination activity, and / or a specific chromatin demethylation / deacetylation activity, wherein the effector domains are each separated by a linker providing sufficient distance between the domains and the nuclease in order not to substantially interfere with their specific chromatin modifying activities, and the binding of the site-specific nuclease, as well as respective methods involving the complex and use of the complex.

The invention belongs to the technical field of chemical synthesis of spices, and particularly relates to a synthetic method of vanillin and ethyl vanillin. Carrying out substitution reaction on catechol and methyl iodide to generate o-dimethoxybenzene 3; 3 and 1, 2-dichloromethyl methyl ether are subjected to formylation reaction to generate 3, 4-dimethoxybenzaldehyde 4; carrying out demethylation reaction on the 3, 4-dihydroxy benzaldehyde 5 and pyridine hydrochloride to generate 3, 4-dihydroxy benzaldehyde 5; carrying out substitution reaction on the 4-benzyloxy-3-hydroxybenzaldehyde 5 and benzyl bromide to generate 4-benzyloxy-3-hydroxybenzaldehyde 6; carrying out substitution reaction on the 4-benzyloxy-3-methoxyl / ethyoxyl benzaldehyde 6 and iodomethane / iodoethane to generate 4-benzyloxy-3-methoxyl / ethyoxyl benzaldehyde 7; 7 is reduced by hydrogen under the catalysis of palladium on carbon to generate vanillin / ethyl vanillin. Cheap catechol is adopted as a raw material, reaction conditions are mild, equipment requirements are not high, energy consumption is low, the problems that raw materials are not suitable to obtain, the price is high, separation is difficult, and three wastes are seriously generated in a traditional vanillin synthesis method are solved, and a new method is provided for synthesis of vanillin.

The invention discloses a series of colchicine deuterated derivatives for resisting multiple myeloma, which can effectively inhibit proliferation of multiple myeloma cells by improving the metabolic effect of colchicine in the multiple myeloma cells and overcome the defect of large toxic and side effects of metabolism of original drugs. According to the series of colchicine deuterated derivatives capable of resisting multiple myeloma, colchicine is used as a raw material, two reactions of demethylation and deuterated methyl are sequentially performed to obtain a target compound, the reaction steps are few, the reaction conditions are mild, the operability is high, and the efficiency is high.

The invention provides a bidentate cobalt complex containing an imidazo [1, 2-alpha] pyridine group as well as a preparation method and application of the bidentate cobalt complex, and belongs to the technical field of organic chemical synthesis. The structural formula of the bidentate cobalt complex is shown in the specification, and the preparation method comprises the following steps: carrying out bromination reaction and cyclization reaction on 2-methoxy-6-acetylpyridine to obtain a bidentate ligand with methoxy and imidazo [1, 2-alpha] pyridyl, and carrying out demethylation reaction on the ligand to obtain another bidentate cobalt complex with hydroxyl and imidazo [1, 2-alpha] pyridyl. The imidazo [1, 2-alpha] pyridyl-containing bidentate cobalt complexes are prepared from imidazo [1, 2-alpha] pyridyl-containing bidentate ligands, and the two ligands react with anhydrous cobalt chloride respectively to obtain various imidazo [1, 2-alpha] pyridyl-containing bidentate cobalt complexes. The electron effect of the complex is adjusted by changing substituent groups on imidazo [1, 2-a] pyridine groups, then the activity of the complex in catalytic reaction is adjusted, and the complex can be further applied to hydrosilylation reaction of styrene and has very important application prospects.

The application belongs to the technical field of medicine production, and particularly relates to a preparation method and application of five deuterium-substituted glucose. The method comprises deuterium substitution of D-methyl glucoside, and demethylation of the deuterium-substituted D-methyl glucoside to obtain a target product, namely [2,3,4,6,6'-d5]-D-glucose. The preparation method of the five deuterium-substituted glucose is simple in process route, convenient to operate, mild in experimental conditions, and the synthesized five deuterium-substituted glucose is successfully applied to the description of glycolysis metabolism in a brain glioma model, which is helpful to the clinical conversion application of metabolic imaging technology.

The invention belongs to the technical field of chemical synthesis, and particularly relates to an indazole alkaloid derivative as well as a preparation method and application thereof. Comprising the following steps: under an alkaline condition, carrying out alkylation reaction on a compound a and an alkylating agent to obtain a compound b; performing demethylation reaction on the compound b and a demethylation reagent to obtain a compound c; carrying out glycosylation reaction on the compound c and sugar bromide to obtain a compound d; in a sodium methoxide and solvent system, removing acetyl on glycosyl of the compound d to obtain the indazole alkaloid derivative. Or carrying out oxidation reaction on the compound d and methyl iodide to obtain an intermediate; and removing acetyl on glycosyl of the intermediate in a sodium methoxide and solvent system to obtain the indazole alkaloid derivative. The invention provides a preparation method of an indazole alkaloid derivative, which is green, simple, convenient and efficient.

The invention relates to methods of modifying DNA methylation by contacting a cell with a catalytically inactive site specific nuclease fused to an effector domain having methylation or demethylation activity and one or more guide sequences.

The invention discloses a method for preparing olotoxin, wherein tetramethyl olotoxin is subjected to demethylation to obtain the olotoxin.