68 results about "Bromosuccinimide" patented technology

The invention discloses a C60-BODIPY triplet photosensitizer as well as a preparation method and photodynamic antibacterial application thereof. In the preparation process, a fullerene pyrrole ring compound and a BODIPY molecule are connected together through a benzene bridge group, and two ends of a bridge bond are respectively connected to a C atom on a fullerene pyrrole ring and a 6th site of the BODIPY molecule; a BODIPY-C60 binary molecule is formed; the preparation method comprises the following steps: reacting 9-anthracene formaldehyde with 2, 4-dimethyl pyrrole to generate a boron-dipyrromethene molecule of which the meso position is substituted by 9-anthryl, brominating the boron-dipyrromethene molecule at the 6 position by N-bromosuccinimide, coupling the boron-dipyrromethene molecule with p-formylphenylboronic acid, and carrying out Prato reaction on the coupled boron-dipyrromethene molecule with C60 and N-methylglycine to prepare the BODIPY-C60 binary triplet photosensitizer. The triplet photosensitizer has excellent photodynamic activity and relatively high reactive oxygen quantum yield, and can effectively kill bacteria.

The invention relates to the field of coatings, and discloses a self-cleaning nano-coating glass plate and a preparation method and application thereof.The nano-coating is prepared from organic silicon resin, epoxy resin, modified nano titanium dioxide, long-chain alkyl methyl silicone oil, a curing agent and a diluent; the modified nano titanium dioxide is prepared by grafting a modified silane coupling agent and nano titanium dioxide, wherein the modified silane coupling agent is prepared by reacting a modified phosphorus-containing antibacterial monomer with vinyltriethoxysilane; the modified phosphorus-containing antibacterial monomer is prepared by reacting eugenol with N-bromosuccinimide, then reacting with 2-amino-4-methylthiazole, further reacting with diphenyl phosphinyl chloride, and reacting the obtained phosphorus-containing antibacterial monomer with 1, 1, 3, 3-tetramethyldisiloxane; the long-chain alkyl methyl silicone oil is prepared by using octamethylcyclotetrasiloxane, dodecyl methyl dimethoxy silane and hexamethyldisiloxane as raw materials, and the prepared nano coating has a super-hydrophobic surface and also has excellent antibacterial activity, wear resistance and flame retardance.

The invention provides a synthesis method of an OLED polycyclic fused thiophene compound, and relates to the technical field of material synthesis, and the synthesis method comprises the following steps: providing and mixing 2-naphthalene sulfonic acid and dichloromethane, dropwise adding an N-bromosuccinimide solution into the mixture under the protection of inert gas, and reacting to obtain an intermediate A; dissolving the intermediate A, then adding sodium hydroxide, 4-bromophenylboronic acid, water and tetrakis (triphenylphosphine) palladium, and reacting to obtain an intermediate B; dissolving the intermediate B, adding sulfonic acid and phosphorus pentoxide, and reacting to obtain an intermediate C; adding the intermediate C into tetrahydrofuran, dissolving, adding lithium aluminum hydride under inert gas, and reacting to obtain a target compound. According to the method, the chemical reaction efficiency of the intermediate C is high, and the yield and LC purity of a target product are relatively high.

The invention provides a thermo-sensitive triblock copolymer with a lateral group containing polyethylene glycol and a preparation method of the thermo-sensitive triblock copolymer, and relates to the field of polymer synthesis. The preparation method comprises the following steps: carrying out a reaction on hydroxyl-terminated polyether PAGE and single carboxyl-terminated polyethylene glycol monomethyl ether (mPEG-COOH) under the action of N-bromosuccinimide to prepare a polymer brush PAGE-g-mPEG; and reacting the polymer brush PAGE-g-mPEG with poly (N-isopropylacrylamide) to generate a thermo-sensitive triblock copolymer of which the side group contains polyethylene glycol. The thermo-sensitive triblock copolymer disclosed by the invention is endowed with good biocompatibility, hydrophilicity and low-temperature performance, has a good thermo-sensitive characteristic, and can be widely applied to the fields of drug-loaded controlled release, sewage treatment and nanoparticles; the invention also provides a preparation method of the thermo-sensitive triblock copolymer, which overcomes the defects of harsh reaction conditions and easy chain extension reaction, and realizes accurate control of the molecular weight of the prepared copolymer.

The invention provides a synthetic method of a bromo-pyrazole intermediate for preparing loratinib, which comprises the following steps: 1, adding a solvent and a compound 19 into a reaction kettle, and then adding a bromination reagent N-bromo-succinimide in batches to synthesize a compound 14; 2, adding dichloromethane, the compound 14 and triethylamine into a reaction kettle, and then dropwise adding trifluoroacetic anhydride to synthesize a compound 15, namely the key intermediate bromo-pyrazole of the loratinib; according to the synthetic method of the bromo-pyrazole intermediate for preparing the loratinib, the adopted starting materials are low in price, the route is simple, the yield is high, the purity is good, the cost is reduced by 40% or above compared with an existing synthetic route, the production cost can be greatly reduced, and the industrial competitiveness is improved.

The invention belongs to the field of Velciguat synthesis, and particularly relates to a preparation method of Velciguat and an intermediate product thereof. The preparation method of the Velciguat comprises the following steps: (1) reacting aminomalononitrile with methyl chloroformate to generate an intermediate product I; (2) carrying out ring closing on the intermediate product I and formamidine under an alkaline condition to obtain an intermediate product II; (3) carrying out bromination reaction on the intermediate product II and N-bromosuccinimide to obtain an intermediate product III; (4) reacting the intermediate product III with bis (pinacolato) diboron under the action of a catalyst to obtain an intermediate product IV; and (5) carrying out a reaction on the intermediate product IV and 5-fluoro-1-(2-fluorobenzyl)-3-iodo-1H-pyrazolo [3, 4-b] pyridine to prepare the viriciguat. The method is simple to operate, low in cost and safe in production. The invention also provides the intermediate product obtained by the preparation method.

The invention relates to a preparation method of alpha-bromo-carboxylic acid. The method comprises the following steps: under the protection of nitrogen, dissolving a malonic acid substrate, N-bromosuccinimide (NBS) and pyridine in a reaction solvent, and reacting for 1 hour at 50 DEG C under the irradiation of blue light; and separating the crude reaction product through column chromatography or preparative plate chromatography to obtain the target delta-bromo-carboxylic acid compound. The method has the advantages of mild reaction conditions, simple operation, easily available raw materials, low cost, and good functional group compatibility and substrate universality. In the obtained product, due to high reaction activity of bromine atoms, the bromine atoms can be further derived into various alpha-heteroatom substituted carboxylic acids, and the product has application potential in the fields of synthetic chemistry, drug research and development and the like.

The present invention relates to the technical field of detection systems, in particular to a system for detecting the content of N-bromosuccinimide in sodium sugammadex. The system comprises a chromatograph main body for elution and separation and a mass spectrometer main body for detection, wherein a column oven is connected between the chromatograph main body and the mass spectrometer main body, and a chromatographic column for sample elution and separation is assembled in the column oven; a liquid inlet seat and a liquid outlet seat are provided in the column oven, respectively communicating with the chromatograph main body and the mass spectrometer main body, and the chromatographic column is positioned and assembled between the liquid inlet seat and the liquid outlet seat; a telescopic joint structure is provided at the end of the chromatographic column, the chromatographic column is connected to the liquid inlet seat and the liquid outlet seat via the joint structure, and a glass wool column can be positioned and loaded in the joint structure; a combined water bath structure is provided in the column oven based on an inner partition, and the assembled water bath structure can seal the chromatographic column main body structure; the present invention can achieve the purpose of improving the accuracy of content detection.

The method for manufacturing an intermediate compound for shikonin synthesis of the present invention comprises the steps of: reacting 1,5-dihydroxynaphthalene with dimethyl sulfate to prepare 1,5-dimethoxynaphthalene; reacting 1,5-dimethoxynaphthalene with N-bromosuccinimide (NBS) to prepare 1,5-dibromo -4,8-dimethoxynaphthalene; introducing a methoxy group into 1,5-dibromo-4,8-dimethoxynaphthalene using copper iodide (CuI) and 1,10-phenanthroline as a catalyst to prepare 1,4,5,8-tetramethoxynaphthalene; performing formylation of 1,4,5,8-tetramethoxynaphthalene using phosphoryl chloride (POCl3) to prepare 2-formyl-1,4,5,8-tetramethoxynaphthalene; and forming a boron complex using pinacolborane (HBpin) and 3,3-dimethylallyl bromide and reacting the boron complex with 2-formyl -1,4,5,8-tetramethoxynaphthalene to prepare a prenylated shikonin intermediate. Compared to conventional synthetic methods, the method of the present invention offers milder reaction conditions, shorter reaction time, and improved yield, thereby greatly enhancing the economic feasibility of shikonin synthesis.

The invention belongs to the technical field of organic synthesis, and discloses a preparation method for trifluoromethylation of a 1, 6-enyne substrate. The preparation method comprises the following steps: in a protective gas atmosphere, mixing a 1, 6-eneyne substrate, NaSO2CF3, an oxidant, N-bromosuccinimide and an organic solvent, heating to react, cooling, separating an organic phase, drying and purifying to obtain a product after trifluoromethylation of the 1, 6-eneyne substrate, the organic solvent is selected from any one of dimethoxyethane and 1, 2-dichloroethane. The preparation method is mild in reaction condition, simple and convenient to operate, good in substrate applicability, good in substrate selectivity in reaction and high in target product yield, and a new way is provided for trifluoromethylation of the 1, 6-eneyne compound.

The application belongs to the technical field of organic synthesis, and provides a star structure carbazole derivative, a preparation method thereof and a carbazole conductive polymer. The application obtains an intermediate by mixing 10-phenyl-10H-phenothiazine, N-bromosuccinimide and a first organic solvent for reaction; obtains the star structure carbazole derivative by mixing the intermediate, 9H-carbazole-2-boronic acid pinacol ester, tetrakis(triphenylphosphine)palladium, an accelerator and a second organic solvent for reaction; and obtains the carbazole conductive polymer by mixing the star structure carbazole derivative and an electrolyte solution for cyclic voltammetry electrochemical polymerization. The method is simple, has few by-products, and the star structure carbazole derivative obtained by the method is a non-coplanar star structure, which is beneficial to the embedding and discharging of electrolyte ions, so that the carbazole conductive polymer has excellent electrochemical performance and energy storage properties, and the conductive polymer also has excellent electrochromic performance.

The invention discloses a preparation method of adamantyl triphenylamine, which comprises the following steps: 1, reacting o-aminobiphenyl with N-bromosuccinimide and an organic solvent to prepare an intermediate I; 2, adding 1-adamantanol and chlorobenzene into an organic solvent, and reacting under the action of strong acid to prepare an intermediate II; 3, adding the intermediate II, alkali and bis (pinacolato) diboron into an organic solvent, and reacting under the action of a palladium catalyst to prepare an intermediate III; and step 4, adding the intermediate III, the intermediate I, a palladium catalyst, alkali salt and tetrabutylammonium bromide into a mixed solution of toluene and deionized water, and carrying out Suzuki reaction to obtain adamantyl triphenylamine. The preparation method of adamantyl triphenylamine has the advantages of easily available raw materials, simple operation, high reaction yield in each step, high purity of the obtained product, and realization of industrialization.

This invention discloses a two-photon fluorescent dye, prepared as follows: 6-hydroxy-2-naphthaldehyde reacts with a dihaloalkane under alkaline conditions to obtain a monohaloalkane-based aryl ether, which is then reacted with an aqueous trimethylamine solution to prepare S1; diethyl 4-(4-tolyl)pyridine-2,6-dicarboxylate reacts with N-bromosuccinimide to obtain a brominated product, which is then reacted with triphenylphosphine to prepare S2. After intermediates S1 and S2 react under strongly alkaline conditions, the product is then hydrolyzed to prepare the target product. This dye exhibits good cell membrane permeability, good dispersion in the cytoplasm, preferentially targets organelles in the cytoplasm, is water-soluble, has very low toxicity, and a high two-photon absorption interface, making it suitable for two-photon fluorescence confocal microscopy imaging.

The application provides a kind of 3-bromofluorenone and preparation method thereof, it relates to the technical field of organic photoelectric material.The method is prepared by using 2-bromofluorenone and benzophenone imine under the condition of palladium catalyst to react 2-amino fluorenone, purification is convenient;Using 2-amino fluorenone and N-bromosuccinimide under ice water bath, the impurity can be controlled, purification is convenient, cost is controlled;Using with tert-butyl nitrite can obtain high purity 3-bromofluorenone compound target product;Using N-bromosuccinimide in ice water bath, accurately locate the 3 position of fluorenone, without the help of other catalysts, simplify the reaction;Using the way of dropping tert-butyl nitrite THF solution into the reaction system, can greatly improve the utilization rate of tert-butyl nitrite, finally improve the yield of the whole reaction.The preparation method provided by the application has the advantages of controllable impurity, easy purification and cost economy.

The invention relates to the field of drug synthesis, in particular to an amine compound for fungi drugs and a preparation method of the amine compound. Comprising the following steps: 1) adding N-bromosuccinimide (NBS) into 4-iodobenzene serving as an initial raw material in an acetonitrile solvent in the presence of benzoyl peroxide serving as a catalyst, and reacting to obtain a 1-bromomethyl-4-iodobenzene compound II; 2) adding N-methylacetamide into the compound II in a tetrahydrofuran solvent by using potassium carbonate as alkali, and reacting to obtain an N-(4-iodobenzyl)-N-methylacetamide compound III; and 3) heating the compound III in a sodium hydroxide solution for deacetylation to obtain the compound IN-methyl-1-(4-iodophenyl) methylamine. The invention aims to provide a preparation process of the N-methyl-1-(4-iodophenyl) methylamine compound I, which is simple, convenient, green, environment-friendly and suitable for industrial production.

The invention discloses a preparation method and application of a liquid reaction type bromine flame retardant, and belongs to the technical field of flame retardant preparation, and the preparation method comprises the following steps: mixing polypropylene glycol, tetrahydrofuran, N-bromosuccinimide, azodiisobutyronitrile and tetrahydrofuran for reaction, and performing post-treatment to obtain a brominated polyether polyol flame retardant; according to the invention, the prepared brominated polyether polyol flame retardant is also used in thermosetting resin to prepare a flame-retardant resin composition; according to the brominated polyether polyol flame retardant, the balance of high bromine content, high reaction activity and excellent synergism is realized; as a reactive flame retardant, the flame retardant not only can improve the flame retardant property of thermosetting resins such as polyurethane, but also can better retain the inherent physical and mechanical properties of a resin matrix.

The invention discloses a method for synthesizing 3-bromine-9-ethyl carbazole through reactive extrusion. The method comprises the following reaction steps: (1) adding uniformly mixed 9-ethyl carbazole, N-bromosuccinimide and a solid diluent into a solid feeding bin of a double-screw extruder; (2) adjusting the feeding speed and the screw rotating speed of the double-screw extruder, and dropwise adding auxiliary liquid through a peristaltic pump; and (3) collecting the product, dissolving, filtering, evaporating to remove the solvent and the like to obtain the 3-bromine-9-ethyl carbazole. According to the present invention, the double-screw extruder is adopted to efficiently prepare the 3-bromo-9-ethyl carbazole through the reaction extrusion, such that the use amount of the toxic and harmful solvent is substantially reduced, the product yield is improved, and the good application prospect is provided.

The application belongs to the technical field of pesticide intermediate preparation, and discloses a preparation method and application of 4-chloro-2,6-dimethylbromobenzene. The method uses 3,5-dimethylphenol as a starting material, and first reacts with p-toluenesulfonyl chloride under alkaline conditions to obtain 3,5-dimethylphenyl p-toluenesulfonate, then performs selective bromination with N-bromosuccinimide in the presence of a free radical initiator to obtain 4-bromo-3,5-dimethylphenyl p-toluenesulfonate, and finally performs a substitution reaction with a chlorine source such as concentrated hydrochloric acid or lithium chloride to obtain the target product 4-chloro-2,6-dimethylbromobenzene; the product can be used for synthesizing pesticides such as methoxypiperidine acetate and dispiro. The method realizes high-selectivity halogenation by regulating the electron cloud distribution of the benzene ring through functional group transformation, has mild reaction conditions, simple operation, avoids high-risk reagents and processes, has high yield, less waste, low cost, and is suitable for industrial production.

The application belongs to the field of vixepiromide synthesis, and particularly relates to a preparation method of vixepiromide and intermediate products thereof. The preparation method of vixepiromide comprises the following steps: (1) reacting aminopropandinitrile with methyl chloroformate to generate an intermediate product one; (2) ring closing the intermediate product one with formamidine under alkaline conditions to generate an intermediate product two; (3) performing bromination on the intermediate product two with N-bromosuccinimide to generate an intermediate product three; (4) reacting the intermediate product three with pinacol diboron under the action of a catalyst to generate an intermediate product four; and (5) reacting the intermediate product four with 5-fluoro-1-(2-fluorobenzyl)-3-iodo-1H-pyrazolo[3,4-b]pyridine to generate vixepiromide. The application has the advantages of simple operation, low cost and safe production. The application further provides the intermediate products generated in the above preparation method.

The present invention discloses a method for synthesizing α-bromosulfone compounds. Using a mixed solvent and N-bromosuccinimide as the bromination reagent, the alkynyl sulfone compounds are converted into the corresponding α-bromosulfone compounds under alkaline conditions. The reaction is controlled by the equivalent ratio of N-bromosuccinimide and the base as well as the reaction time, realizing the selective synthesis of α-bromosulfone compounds. The method of the present invention has mild reaction conditions, simple operation, excellent yield and good functional group tolerance.

The application belongs to the field of pharmaceutical chemical industry, and particularly relates to a preparation method of a ticagrelor intermediate (1R, 2S)-2-(3, 4-difluorophenyl)cyclopropylamine, which comprises the following steps: taking compound II as raw material, and reacting with N-bromosuccinimide and sodium acetate to prepare target intermediate compound I. Compared with the prior art, the reaction has the advantages of mild reaction condition, simple operation, high safety, simple post-treatment, and safety and environmental protection. It is determined that the yield of the product prepared by the technical scheme disclosed in the application can reach more than 88%, and the purity is more than 99%.

This invention discloses a eutectic solvent and its preparation, a metal leaching agent, and a metal leaching method. The eutectic solvent is prepared by mixing choline chloride and a sulfonamide compound in a specific ratio; the sulfonamide compound is sulfonamide, 4-amino-N-(aminoiminomethyl)benzenesulfonic acid, or p-aminobenzenesulfonamide. This invention provides a metal leaching agent containing the aforementioned eutectic solvent, which is a transparent liquid prepared from the eutectic solvent and an auxiliary agent. The auxiliary agent is at least one selected from 1,3-dibromo-5,5-dimethylhydantoin, 1,3-dichloro-5,5-dimethylhydantoin, N-chlorosuccinimide, N-bromosuccinimide, chloramine T, and sodium hypochlorite. The eutectic solvent of this invention is an environmentally friendly compound, and the metal leaching agent system containing this eutectic solvent possesses both good oxidizing and coordinating abilities, enabling the leaching of gold and palladium with rapid leaching speed and high extraction rate.

The invention relates to the technical field of compound synthesis, in particular to a preparation method of N, N '-bis (2, 4, 6-trimethoxyphenyl) oxamide. The preparation method comprises the following steps: S1, bromination reaction: mixing dichloromethane, 1, 3, 5-trimethoxybenzene and triethylene diamine, adding NBS (N-bromosuccinimide) or dibromohydantoin, and reacting to obtain 1-bromo-2, 4, 6-trimethoxybenzene; s2, amination reaction: mixing an organic solvent, an acid binding agent, 1-bromo-2, 4, 6-trimethoxybenzene, a cuprous compound and a catalyst, and reacting to obtain 2, 4, 6-trimethoxyaniline hydrochloride; and S3, condensation reaction: mixing the 2, 4, 6-trimethoxyaniline hydrochloride with dichloromethane, adding triethylamine, and dropwise adding oxalyl chloride to obtain the N, N '-bis (2, 4, 6-trimethoxyphenyl) oxamide. The invention provides a preparation method of N, N '-bis (2, 4, 6-trimethoxyphenyl) oxamide, and aims to solve the problems of relatively slow reaction speed, incomplete reaction conversion, generation of impurities, poor product purity and low yield in a synthetic method in related technologies.

This invention discloses a method for preparing deuterated 1,2-dibromoethane, comprising the following steps: (1) adding tetradeuterium glycol, N-bromosuccinimide, and solvent into a reaction vessel; (2) controlling the temperature inside the reaction vessel at -5 to 20°C, and then adding a mixture of triphenylphosphine and solvent dropwise into the reaction vessel; (3) after the dropwise addition is completed, restoring the reaction vessel to room temperature, and controlling the reaction time to 0.5 to 1.5 h to obtain a product containing deuterated 1,2-dibromoethane. The reaction temperature of this invention is at room temperature, the reaction operation is simple, it meets the requirements of green chemistry, and it can be industrialized. Furthermore, the purity of deuterated 1,2-dibromoethane is above 98 wt%, and the yield of deuterated 1,2-dibromoethane is above 60 wt%.

The invention belongs to the technical field of lithium ion battery diaphragms, and particularly relates to a preparation method and application of a modified polyphenyl ether (PPO)-based coated polyolefin diaphragm. The preparation method comprises the following steps: (1) bromination treatment: preparing brominated polyphenyl ether (BPPO), dissolving PPO in a chlorobenzene solution, adding bromosuccinimide to carry out electrophilic substitution reaction, and taking azodiisobutyronitrile as an initiator; (2) preparing a three-layer composite diaphragm: preparing a membrane casting solution by adopting a non-solvent phase inversion method, taking N-methyl pyrrolidone as a solvent and taking polyethylene glycol as a pore-forming agent, forming BPPO coatings on double surfaces of a PE diaphragm by a blade coating process, and curing by a water / ethanol double-component coagulating bath; and (3) carrying out surface functionalization treatment: carrying out in-situ amination reaction on 3-aminopropyltrihydroxysilane, and constructing a cross-linked structure in the BPPO coating. Compared with the prior art, the coating diaphragm provided by the invention takes the cross-linked brominated PPO material as the diaphragm coating layer for the first time, the stability of the material is enhanced through molecular design, the thermal shrinkage rate is remarkably improved compared with that of a PE base material, and meanwhile, the coating diaphragm has a flame-retardant characteristic.

This invention discloses a method for preparing bromobenzothiophene, relating to the field of organic synthesis. In the preparation of bromobenzothiophene, N-bromosuccinimide is first purified by recrystallization; benzo[b]thiophene is mixed evenly with acetonitrile, and then the purified N-bromosuccinimide is added in batches while stirring. Finally, deionized water is added to the reaction solution, followed by stirring, filtration, washing, and drying to obtain 3-bromobenzo[b]thiophene. The method for preparing bromobenzothiophene provided by this invention reduces the generation of toxic byproducts due to solvent substitution, resulting in a higher yield of bromobenzothiophene. Furthermore, the preparation method provided in this application can be carried out at a lower temperature, saving energy.

This invention discloses a berberine-dimethylaniline photosensitizer, its preparation method, and its application, belonging to the field of biomedical technology. The method involves sequentially reacting berberine with magnesium methyl bromide via Grignard addition, followed by bromomethylation with N-bromosuccinimide, and basic condensation with dimethylaminobenzaldehyde, then demethylating under high temperature and vacuum to obtain the active berberine-dimethylaniline. Finally, it undergoes weakly alkaline treatment to obtain the inactivated berberine-dimethylaniline. This invention introduces the electron-donating group dimethylaniline onto the berberine backbone, constructing an electron push-pull structure that red-shifts the absorption wavelength, facilitating deeper tissue penetration. Furthermore, this photosensitizer maintains high activity in the weakly acidic microenvironment of tumors while remaining inactive under normal physiological conditions, thereby achieving intelligent "on-off" regulation based on pH differences, improving the safety and precision of photodynamic therapy for tumors.

The invention discloses a method for continuously synthesizing 5, 5 '-dibromo-2, 2'-bithiophene through twin-screw extrusion, which comprises the following reaction steps: (1) adding 2, 2 '-bithiophene, N-bromosuccinimide and a solid diluent which are uniformly mixed into a feeding bin of a twin-screw extruder; (2) adjusting the feeding speed and the screw rotating speed of the double-screw extruder; and (3) collecting the product, dissolving, filtering, evaporating to remove the solvent and the like to obtain the 5, 5 '-dibromo-2, 2'-bithiophene. According to the present invention, the solvent-free continuous efficient preparation of 5, 5 '-dibromo-2, 2'-bithiophene is achieved by using the twin-screw extrusion technology, the method is green and environmentally friendly, the product yield is increased, and the method has good application prospects.

The present invention provides a method for synthesizing an OLED polycyclic fused thiophene compound, which relates to the field of material synthesis technology. The method comprises the following steps: providing 2-naphthalenesulfonic acid and dichloromethane and mixing them, adding a solution of N-bromosuccinimide dropwise thereto under inert gas protection to obtain intermediate A; dissolving intermediate A, and then adding sodium hydroxide, 4-bromophenylboric acid, water, and tetrakis(triphenylphosphine)palladium thereto to obtain intermediate B; dissolving intermediate B, adding sulfonic acid and phosphorus pentoxide to obtain intermediate C; adding intermediate C to tetrahydrofuran and dissolving it, and then adding lithium aluminum tetrahydride under inert gas to obtain the target compound. The chemical reaction efficiency of intermediate C in this method is high, and the yield and LC purity of the target product are relatively high.

The invention relates to a method of administering radiotherapy to a patient. The method involves producing a radiolabeled aryl drug compound by reacting the aryl boronic acid compound (II) Ar—Y, or a salt thereof, wherein Y is a borono group (—B(OH)2) or an ester group thereof, with a radionuclide selected from 123I, 124I, 125I and 131I, in the presence of an oxidizing agent selected from N-bromosuccinimide and N-chlorosuccinimide, in water, and administering the radiolabeled aryl drug compound to the patient.