68 results about "Demethylation" patented technology

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.

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.

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

The invention belongs to the technical field of fluorescent probes, and particularly relates to a single-molecule fluorescent probe based on a phenothiazine structure as well as a preparation method and application of the single-molecule fluorescent probe. The preparation method comprises the following steps: firstly introducing an alkyl chain to a nitrogen atom of a raw material to obtain the phenothiazine structure-based single-molecule fluorescent probe, then carrying out regioselective formylation on the raw material to obtain the phenothiazine structure-based single-molecule fluorescent probe, then treating the raw material by adopting aluminum trichloride to realize O-demethylation, and finally carrying out intramolecular cyclization reaction on the raw material and 1H-benzimidazole-2-acetonitrile to obtain the phenothiazine structure-based single-molecule fluorescent probe. The single-molecule fluorescent probe based on the phenothiazine structure prepared by the invention is compatible with orthogonal chemical reaction activity and maintains controllable electron transfer, so that different chemical events are converted into specific optical signals, and selective and mechanism specific fluorescent response to phosgene, copper ions and hypochlorite is realized.

This invention discloses a method for preparing raloxifene EP impurity B, comprising the following steps: dissolving 6-methoxy-2-(4-methoxyphenyl)benzothiophene (Ⅰ) as a raw material in solvent one, adding NIS, and then adding a free radical initiator to react and obtain intermediate III; dissolving 4-[2-(1-pyrrolidinyl)ethoxy]benzoate salt (II) in solvent two, adding solvent two or not, and then adding a chlorinating agent to react and generate intermediate IV; dissolving intermediate III in solvent three, adding a Lewis acid, and then adding intermediate IV, and performing a Friedel-Crafts acylation reaction to generate intermediate V; dissolving intermediate V in solvent four, adding a demethylating agent, and generating bisphenol hydroxyl intermediate VI under demethylation conditions; dissolving intermediate VI in solvent five, adding a reducing agent, and generating intermediate VII through a reduction reaction; dissolving intermediate VII in formic acid, stirring, evaporating, and finally lyophilizing to generate the formate target product VIII.

The invention relates to the technical field of anti-aging drugs, in particular to application of a small molecule compound in preparation of anti-aging drugs. The small molecule compound competitively blocks the interaction between the KDM6A and a vacuolar ATP enzyme V0 structural domain subunit ATP6V0C through a specific small molecule binding pocket of targeted histone demethylase KDM6A, and further inhibits the demethylation activity of the KDM6A on 36th lysine of the ATP6V0C. The small molecule compound can effectively down-regulate the activity of senescence-related beta-galactosidase, improve cell cycle arrest and reverse nerve cell senescence phenotypes induced by environmental pollutant GenX, and is especially suitable for resisting nerve cell premature senescence caused by perfluorinated and polyfluoroalkyl compounds such as GenX. According to the technical scheme, the technical problem that drugs which are definite in component, clear in action mechanism, stable in curative effect and capable of pointedly relieving senescence are lacked in the prior art can be solved, and ideal application and popularization prospects are achieved.

The current invention concerns a synergistically effective fungicide composition comprising as component (A) a fungicidally active amount of choline phosphonate and as component (B) at least one additional fungicide selected from the group comprising quinone fungicides, succinate dehydrogenase inhibitors, benzamide fungicides, sulphur fungicides, carboxylic acid amide fungicides, demethylation inhibitor fungicides, phenylamide fungicides, copper fungicides, piperidinyl thiazole isoxazoline fungicides and sugar alcohols, wherein a weight ratio of components (A) and (B) is in a range from 1:1000 to 1000:1.The invention further concerns a kit a use of a fungicide composition according to the invention in an amount effective for controlling one or more types of fungal infections by applying the fungicide composition to the fungal infections.

The application discloses a high-temperature-resistant metalized capacitor film and a preparation method thereof, and belongs to the technical field of thin film or thick film capacitors. The application provides a novel method for preparing a metalized capacitor film, which comprises the following steps: taking 4-vinylbenzocyclobutene as raw material, and combining the raw material with hydrogen bromide after an addition reaction to obtain a substitution product; combining 2-methoxy-4-vinylphenol with the substitution product after demethylation to obtain a polymerization monomer containing a double bond and a cycloalkane structure; polymerizing the polymerization monomer with decafluorobiphenyl and 4-allylphenol to obtain a base film; and plating a metal layer on the base film to obtain the high-temperature-resistant metalized capacitor film. The application has good thermal stability, and solves the technical problem that a thermoplastic base film is deformed or decomposed at high temperature, and is difficult to meet the use requirement.

The application discloses a preparation method of a catalyst for synthesizing pyridine from 3-methylpyridine and relates to the technical field of catalysts. The catalyst comprises the following steps: ZSM-5 is used as a carrier, V2O5, CoO and Ag are used as active components, molecular sieve ZSM-5, citric acid, ammonium metavanadate, cobalt nitrate, silver nitrate and deionized water are mixed, and then are filtered, dried and calcined to obtain a supported high-efficiency catalyst; the catalyst is filled in a fixed bed, 50% 3-methylpyridine is used as raw material, and a demethylation reaction is carried out under the action of high temperature, the catalyst and air to produce pyridine. The catalyst used in the application does not need to be frequently activated, the activation frequency is low, the catalyst stability is good, the catalyst is not prone to deactivation, can continue to operate stably after activation, catalyst loss is greatly reduced, 3-methylpyridine can be efficiently converted into pyridine by using the prepared catalyst, and the dilemma of waste caused by small demand for 3-methylpyridine in the market is solved.

This invention provides a ( E This invention relates to the field of pharmaceutical synthesis technology and provides a method for synthesizing 3,5-dihydroxy-4-isopropylstilbene. The method comprises three steps: starting with 3,5-dimethoxy-bromobenzene as a starting material, isopropylation is carried out under acidic conditions to obtain 3,5-dimethoxy-4-isopropylstilbene; further, a Heck reaction is performed with styrene under palladium catalysis to obtain (…). E )-3,5-dimethoxy-4-isopropylstilbene; demethylation reaction yields the ( E 3,5-Dihydroxy-4-isopropylstilbene. Compared to existing synthetic routes, the synthetic method of this invention significantly shortens the synthetic path, has higher atom utilization, higher product yield, and is environmentally friendly.

The invention discloses a flexible bamboo lignin-based polymer material as well as a preparation method and application thereof. Arginine modified polyphenol bamboo lignin and lipoic acid are used as raw materials, and the flexible bamboo lignin-based polymer material with excellent performance is prepared through lipoic acid ring opening polymerization and sulfydryl free radical-polyphenol Michael addition reaction. The preparation method specifically comprises the following steps: carrying out demethylation phenolation modification on bamboo lignin by using a one-pot method, grafting arginine, improving the reaction activity of the bamboo lignin, quantitatively introducing lipoic acid, blocking by using allylurea, and synthesizing the bamboo lignin-based polymer material containing the allylurea, wherein the polymer material contains a dynamic disulfide reversible ring-opening structure. The method breaks through the limitation that the existing lignin is low in reaction activity and lignin-based macromolecules are difficult to recycle, expands the application scene and range of the lignin, and realizes a green mode of oriented preparation, cyclic processing and efficient utilization of the lignin-based macromolecules; and a theoretical basis and guiding significance are provided for high-quality development and high-valued frontier application of the forest resource lignin.

The invention provides a method for converting 2, 6-dimethylphenol into o-methylphenol. The method comprises the following steps: mixing raw materials including 2, 6-dimethylphenol, water and hydrogen, and carrying out a continuous demethylation reaction under the action of a catalyst to obtain o-methylphenol, the catalyst comprises a molecular sieve carrier and a metal oxide loaded on the molecular sieve carrier. According to the present invention, the molecular sieve carrier in the catalyst has characteristics of suitable pore size and large specific surface area so as to easily adsorb more 2, 6-dimethylphenol and hydrogen gas, such that the reaction efficiency of the 2, 6-dimethylphenol and the hydrogen gas is improved; by adopting the method disclosed by the invention, the low-value 2, 6-dimethylphenol is converted into the o-methylphenol with wider application and higher additional value, so that the value of the byproduct 2, 6-dimethylphenol in the process of producing the o-methylphenol through phenol methylation is greatly improved, and meanwhile, the problem that the byproduct 2, 6-dimethylphenol is difficult to recover and treat is also solved.

The invention belongs to the technical field of bioactive components, and particularly relates to a screening method of a deep-eutectic solvent and application of the deep-eutectic solvent in selective demethylation of polymethoxylated flavonoids. According to the method, the five eutectic solvents are screened on the basis of physicochemical properties and thermodynamic properties, the eutectic solvent capable of being efficiently demethylated is obtained, and the requirement for obtaining hydroxylated PMFs is met; meanwhile, the concentration, the reaction temperature and the reaction time of the demethylation reagent are optimized, and the optimal reaction condition is obtained, so that the technical problem that a high-performance demethylation special reagent is lacked in the prior art is solved.

The invention belongs to the technical field of organic synthesis, and relates to a method and system for preparing p-hydroxyacetophenone through continuous high-temperature alkali fusion demethylation. A three-temperature-zone tubular reactor is matched with a falling film quench cooler, a spiral plate heat exchanger and other devices which are connected in series, p-methoxyacetophenone and a 30% sodium hydroxide solution with the molar ratio being 1: 2-1: 3 serve as raw materials, the raw materials are premixed through a static mixer and then enter the three-temperature-zone tubular reactor, a reaction is conducted for 15-30 min at a certain temperature and pressure, the temperature of a main reaction zone is 245-255 DEG C, and the reaction time is 30-50 min. And carrying out acidification crystallization on the reaction product after millisecond-level quenching. According to the method disclosed by the invention, the problems of incomplete demethylation, acetyl hydrolysis and the like in a traditional intermittent process are solved through processes such as short high-temperature retention time and a spiral turbulence enhanced mass transfer technology, the yield reaches 96.7%, and the purity is greater than 99%; meanwhile, an aluminum trichloride catalyst which is high in price and easy to cause environmental pollution is avoided, so that the method is green and environment-friendly, and the production cost is reduced by about 32%.

The embodiment of the present application discloses a preparation method of nor-tropine alcohol. The method comprises the following steps: performing demethylation reaction on tropinone and chloroethyl chloroformate in the presence of a solvent, performing vacuum concentration and evaporation, and obtaining demethyltropinone; performing reduction reaction on the demethyltropinone and lithium tri-t-butoxyaluminum hydride in the presence of a solvent, and obtaining the nor-tropine alcohol. The present application adopts a new type of reducing agent lithium tri-t-butoxyaluminum hydride, which is safe, not sensitive to air and water, and simple in post-treatment, thus avoiding safety hazards from the source. The present application avoids the use of dangerous Raney nickel and does not need to use an autoclave, so that the production capacity is greatly improved. The present application performs the reaction under low-temperature conditions, is low in energy consumption, can effectively reduce production cost, and is moderate in reaction conditions, safe and simple in operation, and is conducive to large-scale industrial production.

Provided is a controllable RNAm6A demethylation editing system comprising a targeting element and an editing element. The targeting element comprises an inactivated Cas13 protein, and the editing element comprises a methyltransferase domain of FTO and / or ALKBH5. The editing system can specifically perform m6A demethylation editing in tumor cells without affecting the m6A demethylation regulation of normal cells. In addition, the editing system does not require additional light or chemical inducers, thereby eliminating the side effects of inducers on cells and organisms.

The invention relates to a preparation method of a paliperidone palmitate key intermediate, which comprises the following steps: by taking formic acid as a solvent, carrying out reductive amination reaction on 3-methoxy-2-piperidone (SM1) and ammonium formate to obtain 3-methoxy-2-aminopiperidine, and then dehydrating the 3-methoxy-2-aminopiperidine and 3-acetyl-4, 5-dihydro-2 (3H)-furanone (ADHF) in the presence of p-toluenesulfonic acid to obtain an intermediate 2, 3-dimethoxy-2-piperidone. The preparation method comprises the following steps: carrying out a chlorination reaction on an intermediate 2 and oxalyl chloride to obtain an intermediate 3, and carrying out demethylation on the intermediate 3 in 48% HBr to obtain a target product 3-(2-chloroethyl)-9-hydroxy-2-methyl-6, 7, 8, 9-tetrahydro-4H-pyridine [1, 2-a] pyrimidine-4-ketone. According to the method, the production cost is remarkably reduced, the operation is simple, the reaction condition is mild, and the method is suitable for industrial production.

The invention belongs to the technical field of organic synthetic chemistry, and particularly relates to a fluorine-containing hydroxybenzoic acid compound and a preparation method thereof. The invention provides a brand-new synthesis route and method, which comprises the following steps: by taking 4-fluoro-3-methoxybenzonitrile as an initial raw material, firstly, carrying out specific demethylation reaction in a benzene or toluene solvent under the catalysis of anhydrous aluminum trichloride to obtain an intermediate 4-fluoro-3-hydroxybenzonitrile; then carrying out acidic hydrolysis reaction on the intermediate in a mixed medium of concentrated sulfuric acid and water to convert cyano into carboxyl to obtain a 3-hydroxy-4-fluorobenzoic acid crude product; finally, a high-purity product is obtained through directional recrystallization of an ethanol-water mixed solvent. Competitive bromination and Grignard reagent application of a traditional route are fundamentally avoided, and the method has the remarkable advantages of being simple in route, mild in condition, safe to operate, high in selectivity, environmentally friendly and easy to implement industrially.

The application provides a multi-omics gene mining technology-based method for detecting and regulating rice grain length GW5 The application relates to the technical field of biology, and relates to application of gene promoter methylation in regulation of rice grain length. The application is based on a pan-genome micro-core germplasm population, integrates multi-dimensional omics data such as genomes and epigenomes, constructs an epigenome atlas of rice, and uses stable methylation polymorphic markers in the atlas to combine with a rice grain width phenotype to perform multi-omics correlation analysis, successfully mines a new epiallele of a gene, discovers GW5 a new epiallele of a gene, and discovers GW5 that a high-methylation and low-methylation epigenetic state exists in an upstream promoter region of the gene in different rice germplasm backgrounds, and that after demethylation editing is performed on the region, a phenotype of significantly increased grain length is exhibited. Therefore, according to GW5 a methylation level of a promoter of the gene, detection of a rice grain length trait can be realized, and by regulating GW5 a methylation level of a promoter of the gene, regulation of a rice grain length trait can be realized.

This invention relates to the field of organic synthesis technology, and particularly to a dual-fluorescent probe for Bodipy and NBD, its synthesis method, and its application. The method includes: first, synthesizing NBD coumarin compound 6; then, using nitrobenzaldehyde f and dimethylpyrrole as starting materials, undergoing a four-step one-pot cascade reaction with catalytic amounts of trifluoroacetic acid, DDQ oxidation, and excess triethylamine and Lewis acid boron trifluoride diethyl ether to obtain the fluorescent compound Bodipy h; finally, subjecting the fluorescent compound Bodipy h to reduction and acylation to obtain Bodipy fluorescent probe 8; and finally, after lithium hydroxide demethylation of Bodipy fluorescent probe 8 to obtain a carboxylic acid, which is then amidated with the deBoc-protected NBD compound 6 by trifluoroacetic acid to obtain the target product, dual-fluorescent probe 9. This invention anticipates that the fluorescence of coumarin and naphthalimide, through this dual quenching process, can efficiently achieve the quenching strategy, and can be applied to the simultaneous detection of H2S and hNQO1 in vivo or in vitro.

The invention relates to a lignin demethylation method based on nucleophilic activation reinforcement, and belongs to the technical field of biomass high-value utilization. The core of the method is to construct a composite catalytic system composed of sodium sulfite and a nucleophilic activation auxiliary agent. The nucleophilic attack ability and efficiency of sulfite ions on methoxyl groups in lignin macromolecules are remarkably enhanced by introducing small molecular additives such as urea, guanidine hydrochloride, betaine or glycine and utilizing the weak coordination effect of the small molecular additives with sodium ions and the hydrogen bond activation synergistic effect on the sulfite ions. According to the method, the reaction is carried out by taking the mixed solution of the sodium hydroxide aqueous solution and the organic alcohol as a medium under the mild conditions of 80-160 DEG C and normal pressure, the process operation is simple, and the raw material cost is low. The methyl removal rate of the finally obtained demethylated lignin is as high as 71-94%, the phenolic hydroxyl group content is increased to 33-87%, the condensation side reaction is effectively inhibited, the reaction activity is remarkably enhanced, and the demethylated lignin can be used as a high-quality substitute of phenol for preparing phenolic resin, polyurethane and other high polymer materials. The method successfully overcomes the defects of low efficiency, heavy pollution and high cost of the traditional demethylation method, and provides a green, efficient and easy-to-industrialize new path for high-value utilization of lignin.

The invention provides a sulfuryl quaterphenyl [3] arene sulfate macrocyclic compound as shown in a formula IV as well as a preparation method and an application of the sulfuryl quaterphenyl [3] arene sulfate macrocyclic compound. The preparation method of the compound comprises four steps of reaction: Suzuki coupling, cyclization, demethylation and sulfation, the process is simple, the total yield is high, and the yield of each step of reaction is superior to 70%. The compound has excellent water solubility and biocompatibility and can form a stable host-guest inclusion complex with an anti-cancer drug terpyridyl ruthenium through hydrogen bonds, pi-pi accumulation and other supramolecular acting forces, and the binding constant of the compound is as high as (3.59 + / -1.48) * 10 < 6 > M <-1 >. A cytotoxicity experiment shows that the half inhibitory concentration (IC50) of the inclusion complex to human colon cancer cells HCT116 is 2.95 mu M, and compared with a free terpyridyl ruthenium drug (IC50 = 64.93 mu M), the anticancer activity of the inclusion complex is improved by about 22 times. The invention provides an efficient and convenient new strategy for drug delivery, the bioavailability and the treatment effect of the drug can be remarkably improved without covalent modification of drug molecules, and the drug delivery system has a good industrialization prospect.