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100 results about "Thianaphthene" patented technology

Thianaphthene may be used in the preparation of 2-thianapthenylphenyllith ium, via metalation by n-butyllithium. General description Reaction of ethyl diazoacetate with thianaphthene has been reported.

Preparation of covalent organic framework material containing methyl and thiophene and application of covalent organic framework material in production of hydrogen peroxide

The invention relates to preparation of a covalent organic framework material (COF) containing methyl and thiophene and application of the covalent organic framework material in production of hydrogen peroxide. Two thienyl covalent organic framework materials are prepared respectively, and the problem that the yield of hydrogen peroxide produced through photocatalysis of an existing covalent organic framework material is not high is solved. A solvothermal method is adopted for preparation, the preparation process is simple and efficient, the solvent consumption is low, the method is green and environmentally friendly, the yield is high, the problem that the energy utilization efficiency is too low due to mutual compounding of photon-generated carriers and electrons in the photocatalysis process is solved, and the efficiency of photocatalytic production of hydrogen peroxide is effectively improved. The BTTPa-2COF is applied to photocatalytic production of hydrogen peroxide, experimental results show that the BTTPa-2COF has excellent performance of photocatalytic production of hydrogen peroxide, and the performance of hydrogen peroxide production can reach 3680 [mu] molg <-1 > h <-1 > under visible light irradiation.
Owner:HARBIN UNIV OF SCI & TECH

Compound as well as preparation method and application thereof

The invention discloses a compound as well as a preparation method and application thereof, and belongs to the field of organic materials. The compound includes a first chain hydrocarbon group, a first phenyl group, a second phenyl group, a thieno [3, 2-b] thienyl group, and a second chain hydrocarbon group. The first chain alkyl is connected to one carbon atom of the first phenyl group, the other carbon atom of the first phenyl group is connected with one carbon atom of the second phenyl group through a first connecting bond, the other carbon atom of the second phenyl group is connected with one carbon atom of the thieno [3, 2-b] thienyl through a second connecting group, and the other carbon atom of the thieno [3, 2-b] thienyl is connected with the second chain alkyl. The first phenyl group has one or two first substituents which are F,-CF3 or-OCF3; the first and second chain hydrocarbon groups are linear alkyl groups, alkoxy groups, fluoroalkyl groups, alkenyl groups, alkenyloxy groups or difluorovinyl groups. The compound can be used as a liquid crystal monomer to improve birefringence, low-temperature stability, high-temperature stability and nematic phase temperature range of a liquid crystal material.
Owner:HUAWEI TECH CO LTD

Compound containing thiophene group, device and equipment

The invention relates to a compound containing a thiophene group, a device and equipment. In the structural formula of the compound, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are independently selected from hydrogen, halogen, cyano, trifluoromethyl, triphenylamine and derivatives thereof, methoxyl, aryl and derivatives thereof, cyanobiphenyl and naphthyl; the compound can be used for preparing a photovoltaic device and photovoltaic equipment and is used for improving the efficiency and stability of the photovoltaic device.
Owner:JIANGSU SHENGKAI NEW ENERGY TECH CO LTD +1

Boron coordination salicylhydrazone double-state emission fluorophore as well as preparation method and application thereof

The invention relates to the technical field of organic synthesis and the technical field of fluorescent materials, in particular to a boron coordination salicylhydrazone double-state emission fluorophore as well as a preparation method and application of the boron coordination salicylhydrazone double-state emission fluorophore. The structure of the boron coordination salicylazone double-state emission fluorophore is shown as I, II or III; wherein R1 is selected from one of H, halogen atoms, diethylamino and thienyl, R2 is selected from one of H, halogen atoms, diethylamino and thienyl, and R3 is selected from one of aryl, 9, 9 '-spirobifluorenyl, alkoxy and halogen atoms. The boron coordination salicylazone double-state emission fluorophore is diversified in structure and good in solubility, has excellent photophysical properties and extremely high quantum yield, and also shows excellent biocompatibility and remarkable liposome targeting property at the same time. Moreover, the preparation method of the boron-coordinated salicylazone double-state emission fluorophore adopts a one-pot two-step method, is simple and convenient, is high in yield, is green and environment-friendly, and has a wide application prospect.
Owner:ANHUI NORMAL UNIV

Preparation method and application of thienyl metal organic framework material

The invention discloses a preparation method and application of a thienyl metal organic framework material, a 1, 2, 4, 5-tetra (5-bromothiophene) benzene intermediate is synthesized through a Steyler reaction and an NBS bromination reaction, the intermediate reacts with 4-methoxycarbonyl phenylboronic acid to obtain long-size 1, 2, 4, 5-tetra (2-(5-(4-carboxyphenyl)) thienyl) benzene with a large conjugated system, and the long-size 1, 2, 4, 5-tetra (2-(5-(4-carboxyphenyl)) thienyl) benzene has a large conjugated system. And self-assembling with Zr < 4 + > by adopting a solvothermal method to obtain the MOF with a stable structure and an excellent fluorescent property. The prepared fluorescence-enhanced metal organic framework material has excellent chemical and hydrothermal stability, the quenching rate and recognition sensitivity of the fluorescence-enhanced metal organic framework material to Fe < 3 + > and aromatic nitro compounds are kept at 95% and above 104 orders of magnitude, and the prepared MOF has good application in selective fluorescence detection of Fe < 3 + > and aromatic nitro compounds.
Owner:CHINA UNIV OF MINING & TECH

Terpyridyl fluorescent compound and application

The invention belongs to the field of fluorescent compound synthesis, and particularly relates to a terpyridyl fluorescent compound and application. The terpyridyl fluorescent compound is named as (E)-4-(5-((3, 2 ': 6', 3 '-tripyridyl)-4'-yl) styryl) thiophene-2-yl) morpholine in Chinese, the structural formula is # imgabs0, terpyridyl serves as a fluorophore, thiophene serves as a reaction site, morpholine is introduced to serve as an electron withdrawing group, a push-pull result is formed in a molecular structure, the reaction sensitivity is improved, and the fluorescent compound can be applied to the field of fluorescence detection. The Fe < 3 + > is coordinated with the empty orbital of the thiophenic sulfur element, so that the energy distribution of the probe is changed, the fluorescence intensity of the probe is changed, and finally the purpose of identifying the iron ions is achieved. Therefore, the invention also provides application of the terpyridyl fluorescent compound as a fluorescent probe in detection of Fe < 3 + >.
Owner:HENAN VINO BIOTECHNOLOGY CO LTD

Synthesis method of thioether ligand and palladium-catalyzed 2-aryl indole compound

The invention provides a synthesis method of a thioether ligand and a palladium-catalyzed 2-aryl indole compound, and designs an application of the biphenyl thioether ligand and a palladium catalyst in preparation of the 2-aryl indole compound. Indole and arylboronic acid are subjected to a reaction under the action of a palladium catalyst and a biphenyl sulfide ligand, and the structural formula of the biphenyl sulfide ligand is shown in the specification. Ar is phenyl, furyl, thienyl, naphthyl or phenyl substituted by one or more substituent groups; r1 is methyl, methoxyl, fluorine atom, chlorine atom, bromine atom or methyl ester group; r2 is the same or different and is methyl, ethyl, isopropyl, isobutyl, cyclohexyl, benzyl, n-butyl or n-hexyl; r3 is alkoxy, alkylthio, substituted amino or halogen; the palladium catalyst is a divalent palladium compound.
Owner:JIUZHOU PHARMACEUTICAL (HANGZHOU) CO LTD

Metal-organic framework materials, methods of making and use in methane adsorption

The application discloses two kinds of metal organic framework materials Zr-TTB-1 and Zr-TTB-2, a preparation method thereof and application thereof in methane adsorption. The preparation method comprises the following steps: firstly, synthesizing an organic ligand TTB containing a five-membered thiophene ring under specific and suitable conditions by taking 1,3,5-tri(thiophene-2-yl) benzene as a raw material; and then preparing stable two kinds of metal organic framework materials under specific and suitable conditions by combining the organic ligand TTB with a Zr6 metal cluster. The synthesis and preparation method route is simple, the operation is simple, the cost is low, and the method is suitable for efficient methane adsorption and storage.
Owner:ZJU HANGZHOU GLOBAL SCI & TECH INNOVATION CENT

Thiophene-containing tetraarylethene compound as well as preparation method and application thereof

The invention relates to the technical field of organic synthesis, and particularly provides a thiophene-containing tetraarylethene compound as well as a preparation method and application thereof. According to the invention, two phenyl groups of tetraphenylethylene are replaced by methyl formate thiophene groups, and the substituted tetraarylethylene compound has more remarkable photochromic and mechanochromic dual functions through the interaction of a specific substituent group at the position 2 of thiophene and a large conjugated group formed by four aromatic rings; and light-operated double-color display in a polymer mechanism can be realized. The mechanochromism of the compound does not depend on ultraviolet light, when the compound is subjected to mechanical force, the molecular accumulation mode and conjugate planarity are changed, and the color change can be directly observed by naked eyes. Different from traditional tetraphenyl ethylene force-induced discoloration recessive fluorescence change, the dominant color change can be used in the fields of visual stress monitoring, anti-counterfeiting marks, inkless writing materials, safe ink and the like in ultraviolet-free environments (such as indoor and closed spaces), and the application prospect is wide.
Owner:HEBEI UNIV OF SCI & TECH

A compound containing a triphenylamine skeleton, and a preparation method and application thereof

This application relates to a terphenylamine skeleton compound, its preparation method, and its application, belonging to the field of chemical synthesis technology. The preparation method of the terphenylamine skeleton compound of this application includes the following steps: dissolving 2,4,6-triphenylaniline with thiazole-4-carboxaldehyde or thiophene-3-carboxaldehyde in a solvent, conducting a reductive amination reaction under reducing agent conditions, quenching, extraction, washing, concentration to remove solvent, and purification to obtain the terphenylamine skeleton compound. This application provides a simple and mild synthetic method for the natural active products 5'-phenyl-N-(thiazol-4-ylmethyl)-[1,1':3',1''-terphenyl]-2'-amine and 5'-phenyl-N-(thiophene-3-ylmethyl)-[1,1':3',1''-terphenyl]-2'-amine, which can only be extracted from the secondary metabolites of the marine fungus Aspergillus sp. Furthermore, this method utilizes widely available raw materials, which is beneficial for large-scale industrial production of these natural active products.
Owner:HAINAN UNIV

2-cyanopyrrole compound as well as preparation method and application thereof

The invention relates to a 2-cyanopyrrole compound as well as a preparation method and application thereof. The structural formula of the 2-cyanopyrrole compound is as follows: # imgabs0 #, in the formula, R1 is selected from any one of phenyl, 4-methylphenyl, 4-chlorphenyl, 2, 4-dichlorophenyl, cyclopropyl or tert-butyl, and R2 is selected from any one of phenyl, 4-methylphenyl, 4-chlorphenyl, 2, 4-dichlorophenyl, cyclopropyl or tert-butyl; r1 is selected from any one of phenyl, 3-fluorophenyl, 4-methoxyphenyl, 2-thienyl or 2-naphthyl, and R2 is selected from any one of phenyl, 3-fluorophenyl, 4-methoxyphenyl, 2-thienyl or 2-naphthyl. Compared with the prior art, the method has the advantages of simple and easily available raw materials, simple reaction operation, environmental friendliness and the like. The 2-cyanopyrrole compound synthesized by the method disclosed by the invention has a wide application prospect in the related fields of organic synthesis, medicinal chemistry and the like.
Owner:SHANGHAI UNIV

A method for preparing a dihydroquinazoline compound

The application provides a preparation method of a dihydroquinazoline compound and belongs to the technical field of organic synthesis. 1 comprises hydrogen, methyl, tert-butyl, methoxy or halogen; R 2 comprises phenyl; R 3 comprises phenyl; R 4 comprises phenyl, p-tolyl, p-methoxyphenyl, o-tolyl, p-fluorophenyl, p-chlorophenyl, naphthyl, pyridyl or thienyl; Ar comprises phenyl, naphthyl or pyridyl; R 5 comprises phenyl, cyclopropyl, cyclohexyl or [1,1'-biphenyl]-4-yl. The preparation method provided by the application has the advantages of short reaction route, no need to add a transition metal catalyst, good functional group compatibility, high yield, high production efficiency and green environmental protection.
Owner:YUNNAN UNIV

A thiophene-substituted aza-fluoroboron dipyrrole compound, nanoparticles of the compound, and their preparation method and application

The present invention discloses a thiophene-substituted aza-fluoro-boron-dipyrrole compound, nanoparticles of the compound, and their preparation methods and applications. The thiophene-substituted aza-fluoro-boron-dipyrrole compound designed and synthesized by the present invention, the introduction of the thiophene group can significantly red-shift the absorption spectrum of aza-fluoro-boron-dipyrrole, successfully red-shifting to the 810nm near-infrared region, which is more conducive to its application in vivo and in photothermal therapy. Nanoparticles prepared with this compound as the core can be effectively distributed to visceral adipose tissue after local intraperitoneal administration, selectively targeting visceral adipose tissue, have good biocompatibility and high photothermal conversion efficiency, can achieve temperature regulation by adjusting its concentration and 808nm laser power, and can be used for photothermal treatment of obesity.
Owner:ANHUI UNIV

A high-impact material prepared by recycling polypropylene and its preparation method

ActiveCN119570160BPlastic recyclingChlorobenzeneThiothixene
The invention discloses a kind of recycling polypropylene to prepare high-impact material and preparation method thereof, relate to the field of materials. When the present invention uses recycling polypropylene to prepare high-impact material, first, polypropylene is grafted with vinyl diphenylphosphine, then reacted with 1-(3-chlorophenyl)-2-propyn-1-ol, and then reacted with 6-(methyl formate) pyridine-3-boric acid to obtain modified polypropylene; Secondly, calcium carbonate pretreated with 3-aminopropyltrimethoxysilane and 3-thiophene carboxaldehyde are reacted, and thiophene, 6-(thiophene-2-yl) pyridine-2-carboxylic acid, and 6-(3-thienyl) pyridine-2-carboxaldehyde are polymerized on the surface of calcium carbonate to obtain modified calcium carbonate; Finally, recycled polypropylene, modified polypropylene, modified calcium carbonate, sodium cyanide, and bismaleimide are melt-blended, and then extrusion granulation is performed to obtain high-impact material; The high-impact material prepared by the present invention has good impact resistance, anti-aging performance and antibacterial performance.
Owner:肇庆市合亚科技有限公司

S-fluoroalkyl substituted amino acid, polypeptide and preparation method of S-fluoroalkyl substituted amino acid and polypeptide

The invention provides S-fluoroalkyl substituted amino acid, polypeptide and a preparation method of the S-fluoroalkyl substituted amino acid, and belongs to the technical field of fluorinated amino acid. The chemical structural formula of the compound is shown in the specification. Wherein Ar is 4-phenyl phenyl, 4-acetyl phenyl, 4-methoxycarbonyl phenyl, 4-acetoxyphenyl, 4-cyano phenyl, 4-(N, N-dicarboxamide) phenyl, 4-(N, N-dicarboxamide) phenyl, 4-(N, N-dicarboxamide) phenyl, 4-(N, N-dicarboxamide) phenyl, 4-(N, N- Ar'is phenyl, 4-iodophenyl, 4-bromophenyl, 3-methoxycarbonyl phenyl, 2-naphthyl or 3-thienyl, and R1 and R2 are methyl or H. According to the preparation method of the S-fluoroalkyl substituted amino acid and polypeptide, the adopted raw materials are low in cost, simple and easy to obtain, glassware cannot be corroded like other methods, and the tedious and functionalization steps are omitted in the preparation method.
Owner:SHENZHEN BAICHUAN HONGPEI BIOTECHNOLOGY CO LTD

Compounds, preparation method therefor, and use thereof

Compounds, a preparation method therefor, and the use thereof, belonging to the field of organic materials. Each of the compound comprises a first chain hydrocarbyl group, a first phenyl group, a second phenyl group, a thieno[3,2-b]thienyl group, and a second chain hydrocarbyl group. The first chain hydrocarbyl group is linked to a carbon atom of the first phenyl group, another carbon atom of the first phenyl group is linked to a carbon atom of the second phenyl group by means of a first linking bond, another carbon atom of the second phenyl group is linked to a carbon atom of the thieno[3,2-b]thienyl group by means of a second linking group, and another carbon atom of the thieno[3,2-b]thienyl group is linked to the second chain hydrocarbyl group. The first phenyl group has one or two first substituents which are F, -CF3 or -OCF3. The first and second chain hydrocarbyl groups are straight-chain alkyl groups, alkoxyl groups, fluoroalkyl groups, alkenyl groups, alkenyloxy groups, or difluorovinyl groups. The compounds can be used as liquid crystal monomers and can improve the birefringence, low-temperature stability, high-temperature stability and the nematic phase temperature range of liquid crystal materials.
Owner:HUAWEI TECH CO LTD

A synthesis scheme and procedures for preparing a SIK3 inhibitor and intermediates thereof

The present invention relates to a new scheme and process for the preparation of one specific SIK3 inhibiting compound known as (and described herein as) “E9”. Compound E9 has previously been described by the present applicant to show surprisingly superior drug-like properties, such as in respect of target-potency / specificity and ADMET / PK properties, compared to other prior art SIK3 inhibiting compound. The present invention also relates to novel intermediates used in such process of preparing compound E9, as well as to a new methodology used within the process of producing a characteristic key thiophene-based amino intermediate that is used to produce compound E9, and other related aspects as disclosed herein.
Owner:IOMX THERAPEUTICS AG

Method for detecting hydrogen peroxide based on naphthalimide fluorescent probe

The invention provides a method for detecting hydrogen peroxide based on a naphthalimide fluorescent probe, the chemical name of the probe is (E)-(5-(((2-(2-mercaptoethyl)-1, 3-dioxo-2, 3-dihydro-1H-benzo [de] isoquinoline-6-yl) imino) methyl) thiophene-2-yl) boric acid, and the structural formula of the probe is shown in the description. Thiophene plays an important role in constructing a fluorescent probe based on naphthalimide. The fluorescence of the probe is changed into yellow green fluorescence from blue before and after reaction, and the probe has excellent sensing performance on hydrogen peroxide, including quite excellent selectivity and detection limit as low as 38.5 nM. Besides, on the basis of a reaction product aggregation phenomenon induced by cellulose, an (E)-(5-(((2-(2-mercaptoethyl)-1, 3-dioxo-2, 3-dihydro-1H-benzo [de] isoquinoline-6-yl) imino) methyl) thiophene-2-yl) boric acid / cellulose probe is further developed, and it is proved that the probe is higher in hydrogen peroxide detection speed, higher in sensitivity and capable of being used for detecting hydrogen peroxide. And the detection limit is as low as 4.0 nM.
Owner:XINJIANG TECH INST OF PHYSICS & CHEM CHINESE ACAD OF SCI

Chiral bis-thiophene-bis-nitrogen oxide ligands, methods for their preparation and use in asymmetric catalysis

The application discloses chiral bis-thiophene-bis-nitrogen-oxygen ligands BbTh-2NO and BTh-2NO. The ligands comprise bis-thiophene groups and nitrogen-oxygen groups (sulfur atoms of the bis-thiophene and oxygen atoms of the nitrogen-oxygen groups belong to electron-rich coordination sites), can form six-membered ring coordination with Lewis acid soft metal palladium, thereby generating chiral ligand metal palladium complexes, and are applied as chiral ligands in asymmetric catalytic reactions. Therefore, the application has important application value in the field of asymmetric catalytic synthesis, and a synthesis method thereof is very economical and simple. The application also has good air stability, wide applicability and good compatibility for various substituents.
Owner:GUIZHOU UNIV

Preparation method of brexpiprazole

PendingCN121914088AOrganic chemistryQuinolineChloroacetaldehyde
The invention belongs to the technical field of medicine synthesis, and particularly relates to a preparation method of brexpiprazole. The preparation method comprises the following steps: by taking a compound 4-amino benzo [b] thiophene and chloroacetaldehyde as starting materials, carrying out substitution reaction to prepare an intermediate 2, 2 '-(benzo [b] thiophene-4-yl azane diyl) diacetaldehyde, and then carrying out reductive amination reaction on the intermediate 2, 2'-(benzo [b] thiophene-4-yl azane diyl) diacetaldehyde and 7-(4-amino butoxy) quinoline-2 (1H)-ketone to construct a piperazine ring, thereby preparing the target product bupremizole I, the product obtained by the process has high yield and purity, and is suitable for industrial production.
Owner:LUNAN PHARMA GROUP CORPORATION

Preparation method of key intermediate epoxide of Lubabbegron

The invention discloses a preparation method of a key intermediate epoxide of rubaburon, and belongs to the technical field of organic synthesis. The method comprises the following steps: (1) adding a solvent, 2-(2-bromophenyl) thiophene and a basic catalyst into a reaction container, dropwise adding glycidol while stirring, and continuously reacting after dropwise adding until the 2-(2-bromophenyl) thiophene is completely reacted; and (2) cooling and filtering to remove salt, concentrating filtrate to be dry, adding methanol, heating and dissolving, cooling and crystallizing, filtering and drying to obtain the 2-((2-thiophene-2-yl) phenoxy) methyl) ethylene oxide. According to the invention, new raw materials and a new synthetic route are selected to prepare the key intermediate epoxide of the rubaburon, the production process is simple, and the key intermediate epoxide of the rubaburon, which is higher in yield, less in side reaction and lower in cost, is obtained.
Owner:JIANGSU TIANHE PHARMA CO LTD

Thienyl oxazole formylhydrazine Al < 3 + > fluorescent probe and preparation method thereof

The invention relates to a thienyl oxazole formylhydrazine Al < 3 + > fluorescent probe and a preparation method thereof. The preparation method comprises the following steps: reacting thiophene-2-carbonyl chloride with ethyl isocyanoacetate to generate a cyclic compound, so as to obtain an intermediate 1; carrying out acylation reaction on the intermediate 1 and hydrazine hydrate to obtain a compound SON; oxidizing 2, 6-bis (hydroxymethyl)-p-cresol to obtain an intermediate 2; the intermediate 2 and a compound SON are subjected to an amine-aldehyde condensation reaction, and the thienyl oxazole formylhydrazine Al < 3 + > fluorescent probe is prepared. The thienyl oxazole formylhydrazine Al < 3 + > fluorescent probe is high in preparation yield, high in sensitivity and high in specific recognition capability, is suitable for pH detection in a natural environment and a water body, can generate strong blue fluorescence after being combined with metal Al < 3 + >, can realize naked eye recognition, can also be used for rapid monitoring of Al < 3 + > in the natural environment and a biological cell system, and has wide application prospects. The method has important practical application and expansion values.
Owner:NANCHANG HANGKONG UNIVERSITY

A pharmaceutical composition of avibactam sodium and a preparation method thereof

The application belongs to the technical field of pharmaceutical preparations, and particularly relates to a pharmaceutical composition of avibactam sodium and a preparation method thereof. The pharmaceutical composition comprises the following components: avibactam sodium, 2-(5-(2-oxoazetidin-1-yl)thiophene-2-yl)benzo[d]thiazole-6-carboxylic acid; the mass ratio of the avibactam sodium and the 2-(5-(2-oxoazetidin-1-yl)thiophene-2-yl)benzo[d]thiazole-6-carboxylic acid is 1:(2-3). The pharmaceutical composition has a significant synergistic antibacterial effect.
Owner:HARBIN PHARMA GROUP TECH CENT +1

Substituted thienyl-5-fluoro-1h-pyrazolopyridine compound and use thereof

The present invention relates to a substituted thienyl-5-fluoro-1H-pyrazolopyridine compound and a use thereof. The present invention specifically relates to a compound as shown in a formula (I), a preparation method for the compound, a pharmaceutical composition and a combination product containing the compound, and a use of the compound, the pharmaceutical composition or the combination product in preparation of drugs for treating and / or preventing diseases such as heart failure.
Owner:ACADEMY OF MILITARY MEDICAL SCIENCES

A method for the synthesis of a key intermediate for the synthesis of tianeptine

PendingCN122301832ACyclohexanoneCyclohexanecarboxylic acid
This invention relates to the field of pharmaceutical synthesis technology, specifically to a method for synthesizing key intermediates of telexamine, aiming to solve the problems of expensive raw materials, high pollution, high safety risks, and unsuitability for industrial production in existing telexamine intermediate synthesis processes. The key intermediates of this invention are 2-(2-thienyl)cyclohexanone and 2-bromo-2-(2-thienyl)cyclohexanone. The synthesis method uses thiophene and cyclohexanecarboxylic acid as starting materials, and obtains 2-(2-thienyl)cyclohexanone through a solvent-free condensation reaction mediated by polyphosphoric acid, followed by bromination with a brominating reagent and purification in an alcohol phase to obtain 2-bromo-2-(2-thienyl)cyclohexanone. This invention uses inexpensive and readily available raw materials, operates under mild conditions, is simple to operate, is environmentally friendly and safe, and achieves a target product yield of up to 73% and an HPLC purity of up to 98.22%, significantly reducing the synthesis cost of telexamine and making it suitable for large-scale industrial production.
Owner:NANJING ANYIHE PHARM TECH CO LTD

Efficient synthesis method of brexpiprazole

The invention belongs to the technical field of medicine synthesis, and particularly relates to an efficient synthesis method of brexpiprazole. The invention provides a novel preparation method of bupreprazole, which comprises the following steps: by taking 1-(benzo [b] thiophene-4-yl)-4-(4-bromobutyl) piperazine as a starting material, carrying out substitution reaction on the 1-(benzo [b] thiophene-4-yl)-4-(4-bromobutyl) piperazine and 7-hydroxy-2H-benzopyran-2-ketone to prepare an intermediate 7-(4-(4-(benzo [b] thiophene-4-yl) piperazin-1-yl) butoxy)-2H-benzopyran-2-ketone; according to the present invention, with the process, the use of the noble metal catalyst and the generation of the related dimer and the heterotopic substitution impurity can be effectively avoided, and the product obtained through the process has characteristics of high yield and high purity, and is suitable for industrial production.
Owner:SHANDONG NEW TIME PHARMA CO LTD

Method for preparing propionate through ethylene hydrogen esterification reaction

The invention discloses a method for preparing propionate through ethylene hydrogen esterification reaction, which is characterized in that raw materials ethylene, carbon monoxide and low-carbon alcohol are subjected to hydrogen esterification reaction in the presence of a catalyst by taking propionate as a solvent to synthesize propionate, the catalyst is composed of a palladium compound, a naphthyl bidentate phosphine ligand and an acidic auxiliary agent, and the structure of the naphthyl bidentate phosphine ligand is shown in the following formula. Wherein m is 0 or 1, and n is 1 or 2; r1 is selected from phenyl, tertiary butyl, cyclohexyl, 2-pyridyl, 2-thienyl or 2-furyl, and R2 is selected from tertiary butyl, cyclohexyl, 2-pyridyl, 2-thienyl or 2-furyl. According to the method, the naphthyl bidentate phosphine is used as the ligand, the product propionate is used as the reaction solvent, the catalyst activity is high, the yield of the target product propionate is high, and byproducts are few.
Owner:NANJING CHENGZHI CLEAN ENERGY CO LTD

Salt and crystal form of at2r agonist and use thereof in pharmaceutics

PCT designated stageWO2026175343A1CarbamateAcyl group
The present invention relates to a salt and crystal form of an AT2R agonist and use thereof in pharmaceutics, and specifically relates to a salt and crystal form of methyl ((4-fluoro-5-isobutyl-3-(4-((2-(trifluoromethyl)-1H-imidazol-1-yl)methyl)phenyl)thiophen-2-yl)sulfonyl)carbamate (a compound represented by formula (I)) and use thereof in pharmaceutics.
Owner:HUBEI BIO PHARMACEUTICAL INDUSTRIAL TECHNOLOGICAL INSTITUTE INC

Multifunctional naphthalene derivative as well as preparation method and application thereof

The invention belongs to the technical field of organic synthesis, and provides a multifunctional naphthalene derivative as well as a preparation method and application thereof. In the structural formula of the multifunctional naphthalene derivative, R2 is alkyl, phenyl, 2-naphthyl, 1-naphthyl, 2-thienyl, an aromatic ring connected with an electron withdrawing group or an aromatic ring connected with an electron donating group, and the electron withdrawing group and the electron donating group comprise methyl, methoxyl, trifluoromethyl or halogen; r3 is H, methyl or methoxyl; r4 is H, methyl, phenyl or alkynyl. According to the preparation method, a 1, 6-diyne-3-alcohol compound is taken as a raw material, [2-(di-tert-butylphosphine) biphenyl] gold chloride (I) and silver tetrafluoroborate are taken as catalysts, intramolecular 6-endo-dig cyclization, 3, 3-Claisen rearrangement and aromatization reaction are performed, and finally, deacylation reaction is performed to obtain the multifunctional naphthalene derivative with phenyl, phenylethynyl and naphthalene ring structures. The method has application value in multiple fields.
Owner:ZHEJIANG NORMAL UNIV