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239 results about "Phenacyl" patented technology

In organic chemistry, a phenacyl group is an aromatic substituent that consists of a phenyl group attached to an acyl group. A molecule containing a phenacyl group has the formula RCH₂(CO)C₆H₅ and the structure shown to the right. Here, R denotes the remainder of the molecule; for instance, if R is Br, then the compound could be called "phenacyl bromide". Note however that in the standard IUPAC nomenclature this compound would instead be called "2-bromo-1-phenylethanone".

Active energy ray-curable inkjet printing ink composition

An active energy ray-curable inkjet printing ink composition satisfies requirements A to E below is provided: (A) the content of amine-modified oligomer is 1.0 to 20.0% by mass; (B) alkoxy group-containing (meth)acrylate monomers are contained by 2.0 to 20.0% by mass; (C) (meth)acrylate monomers having an alkyl group with 6 to 20 carbon atoms is contained by 2.0 to 25.0% by mass; (D) at least one type selected from the group that consists of 1,6-hexanediol diacrylate, 3-methyl-1,5-pentanediol diacrylate, dipropylene glycol diacrylate, 1,10-decanediol diacrylate, propoxylated(2)neopentyl glycol diacrylate, and hydroxypivalic acid neopentyl glycol diacrylate is contained by 30.0 to 60.0% by mass; (E) as photopolymerization initiators, ethoxy(2,4,6-trimethylbenzoyl)phenylphosphine oxide is contained by 3.0 to 15.0% by, and oligo(2-hydroxy-2-methyl-1-(4-(1-methylvinyl)phenyl)propanone) and / or 2-hydroxy-1-{4-[4-(2-hydroxy-2-methylpropionyl)phenoxy]phenyl}-2-methylpropanone is / are contained by 2.0 to 10.0% by mass, where the total content of photopolymerization initiators is 6.0 to 25.0% by mass.
Owner:SAKATA INX

Preparation method of 2-(2-amino-5-bromo-benzoyl) pyridine

The invention relates to a preparation method of 2-(2-amino-5-bromo-benzoyl) pyridine, which comprises the following steps: by taking 1, 2-diphenyl-1H-benzimidazole (I) as a starting material, oxidizing under the action of chromium trioxide and acetic acid to obtain N-[2-(2-pyridinecarbonyl) phenyl] benzamide (II), hydrolyzing the N-[2-(2-pyridinecarbonyl) phenyl] benzamide (II) under the action of sulfuric acid to obtain 2-(2-aminobenzoyl) pyridine (III), and reacting the 2-(2-amino-5-bromo-benzoyl) pyridine (III) with the 2-(2-amino-5-bromo-benzoyl) pyridine (III) to obtain the 2-(2-amino-5-bromo-benzoyl) pyridine. And (III) performing substitution reaction with NBS in DCM to obtain the target product 2-(2-amino-5-bromo-benzoyl) pyridine. The method has the advantages of mild reaction conditions, higher product purity, high yield, simplicity and convenience in operation, low cost and easiness in industrialization.
Owner:YICHANG TIANRUI BIOMEDICINE CO LTD +1

Process method for preparing fluopyram key intermediate

The invention discloses a process method for preparing a fluopyram key intermediate. The key intermediate is [3-chloro-5-(trifluoromethyl) pyridine-2-yl] ({[2-(trifluoromethyl) benzoyl] amino} methyl) dimethyl malonate, and the process method comprises the following steps: in the presence of a solvent 1, carrying out a reaction on a compound 2-[3-chloro-5-(trifluoromethyl) pyridyl] dimethyl malonate potassium salt and a compound 1-D in a reaction container, and distilling and recovering the solvent 1 to obtain the intermediate compound. Wherein the solvent 1 is selected from acetic ester solvents with the boiling point range of 40-110 DEG C at normal temperature and normal pressure. The process method is simple and convenient, the total yield is high, the solvent is easy to recover, and the product purity is high; the intermediate does not need purification post-treatment, can be directly used for synthesis of fluopyram, can be amplified, and is beneficial to cost reduction, efficiency improvement and commercial mass production.
Owner:YIFAN BIOTECHNOLOGY (SHANGHAI) CO LTD

A ternary insecticidal composition for insects, pests and mites

PCT designated stage expiredWO2025150071A1BiocideAnimal repellantsPhenacylEthyl group
The present invention relates to a ternary insecticidal composition of 3-[benzoyl(methyl)amino]-N-[2-bromo-4-(1,1,1,2,3,3,3-heptafluoropropan-2-yl)- 6-(trifluoromethyl)phenyl]-2-fluorobenzamide (Component A), 4-chloro-5-ethyl-2-methyl-N-[[4-(4-methylphenoxy)phenyl]methyl] pyrazole-3-carboxamide (Component B) and at least one insecticide (Component C) demonstrating an effective and synergistic broad spectrum control of insects-pests and mites with one shot application by developing delay in resistance of hard to kill and resistant towards insects-pests and mites Further, the ternary insecticidal composition provides residual control and increases yield of treated plants due to protection against insect-pests and mites. The ternary insecticidal composition of present invention increases overall health and plant vigor and is environmentally safe.
Owner:RAJDHANI PETROCHEMICALS PRIVATE LIMITED

UV (ultraviolet) viscosity-reduced film and preparation method thereof

The invention belongs to the technical field of UV visbreaking polymers, and particularly relates to a UV visbreaking film and a preparation method thereof. Wherein the UV viscosity-reducing film sequentially comprises a base film (1), a first viscosity-reducing adhesive layer (5), a second viscosity-reducing adhesive layer (4) and a release film (3) from bottom to top, the first viscosity-reducing adhesive layer (5) and the second viscosity-reducing adhesive layer (4) both comprise a photoinitiator, the photoinitiator in the first viscosity-reducing adhesive layer (5) is 1-hydroxy-cyclohexyl phenyl ketone, and the content of the photoinitiator in the formula of the adhesive layer is 0.1%-10% by mass; a photoinitiator in the second viscosity-reducing adhesive layer (4) is bis (2, 4, 6-trimethylbenzoyl) phenyl phosphine oxide, and the content of the photoinitiator in the adhesive layer formula is 0.1-10% by mass; in the preparation method, ultraviolet irradiation precuring is carried out, so that the UV viscosity-reducing film has light selectivity and high cohesion strength, and the residual adhesive is remarkably reduced.
Owner:HUBEI INST OF AEROSPACE CHEMOTECHNOLOGY +1

Spinosad derivatives as insecticides and preparation methods and uses thereof

ActiveCN115785180BPhenacylNematode
The present invention discloses spinosad derivatives or their salts, stereoisomers, and tautomers, which have a structure as shown in Formula I, indicating that the single bond or double bond X is selected from O, S, and N; Y is selected from O, S, and N; A is selected from a covalent bond, hydrogen, substituted alkyl, substituted or unsubstituted heterocycloalkyl, alkoxy, substituted carbonyl, substituted benzoyl, substituted aromatic heteroformyl, and substituted phenylacetyl; and B is selected from hydrogen, substituted alkyl, substituted or unsubstituted heterocycloalkyl, substituted carbonyl, substituted benzoyl, substituted aromatic heteroformyl, and substituted phenylacetyl. The present invention also discloses the use of spinosad derivatives in the preparation of insecticides for controlling plant diseases and insect pests. The spinosad derivatives of the present invention show comparable or higher activity to natural spinosad products against insects of the Noctuidae and Pyralidae families, arachnids, and / or nematodes, and can be used in the agricultural and animal health markets.
Owner:利民化学有限责任公司

Method for producing polyetherketoneketone

PendingUS20250297056A1BenzenePolymer science
A process for manufacturing a polyether ketone ketone, involving: placing an aromatic ether or a mixture of aromatic ethers, including at least 50 mol % of 1,3-bis(4-phenoxybenzoyl)benzene, 1,4-bis(4-phenoxybenzoyl)benzene or a mixture thereof, relative to the total number of moles of aromatic ether(s), in contact with an acyl chloride or a mixture of acyl chlorides, and a Lewis acid, in all or part of a reaction solvent, so as to form a reaction mixture, the 1,3-bis(4-phenoxybenzoyl)benzene and / or 1,4-bis(4-phenoxybenzoyl)benzene essentially not being dissolved in the reaction solvent at the end of the step of placing in contact; and, polymerizing the reaction mixture, the polymerization being performed, at least in part, at a temperature Tp greater than or equal to 50° C.; the process including a step of gradual heating of the reaction mixture until acceleration of the polymerization reaction is achieved.
Owner:ARKEMA FRANCE SA

Preparation method of 2, 4, 6-tri (4 '-butoxy-2'-hydroxyphenyl)-triazine

The invention provides a preparation method of 2, 4, 6-tri (4 '-butoxy-2'-hydroxyphenyl)-triazine, and belongs to the technical field of sun-screening agent preparation. The preparation method of the 2, 4, 6-tri (4 '-butoxy-2'-hydroxyphenyl)-triazine comprises the following steps: carrying out substitution reaction on a compound in a formula I to obtain a compound in a formula II; performing hydrolysis reaction on the compound in the formula II to obtain a compound in a formula III; and carrying out Friedel-Crafts reaction on the compound shown in the formula III and cyanuric chloride to obtain a compound shown in a formula IV. The preparation method comprises the following steps: reacting benzoic acid-3-hydroxyphenyl ester with n-butyl bromide to obtain benzoic acid-3-(butyloxy) phenyl ester, removing benzoyl from the benzoic acid-3-(butyloxy) phenyl ester to obtain 3-(butyloxy) phenol, and reacting 3-(butyloxy) phenol with cyanuric chloride to obtain 2, 4, 6-tri (4 '-butoxy-2'-hydroxyphenyl)-triazine, so that the yield of 2, 4, 6-tri (4 '-butoxy-2'-hydroxyphenyl)-triazine is increased, and the yield of 2, 4, 6-tri (4 '-butoxy-2'-hydroxyphenyl)-triazine is increased. The yield of the 2, 4, 6-tri (4 '-butoxy-2'-hydroxyphenyl)-triazine is increased, and the production cost of the yield of the 2, 4, 6-tri (4 '-butoxy-2'-hydroxyphenyl)-triazine is reduced.
Owner:CHONGQING WERLCHEM FINE CHEM

1, 4-bis (4-fluorobenzoyl) benzene production waste utilization process

The invention discloses a 1, 4-bis (4-fluorobenzoyl) benzene production waste utilization process, which belongs to the technical field of 1, 4-bis (4-fluorobenzoyl) benzene production, and comprises the following steps: dissolving waste leftovers in a solvent, and adsorbing and removing pigments and solid particles in the leftovers by activated carbon; carrying out dehalogenation and hydrogenation on the pretreated leftovers in the presence of a hydrogenation catalyst and an alkaline substance to produce 1, 4-biphenyl acyl benzene; and carrying out separation and purification on the hydrogenation product in a solution crystallization manner to obtain 1, 4-biphenyl acyl benzene with the purity of more than or equal to 99.75%. The waste leftovers are used for producing the 1, 4-biphenyl acyl benzene, so that the utilization rate of the raw materials is increased, the discharge of hazardous wastes is reduced, and the method is green and environment-friendly.
Owner:SHANDONG ORIENT HONGYE CHEM +1

Synthesis process of 1,4-bis(4-phenoxybenzoyl)benzene

The present invention belongs to the technical field of organic synthesis, and specifically relates to a synthesis process of high-yield 1,4-bis(4-phenoxybenzoyl)benzene. The process is mainly prepared by using excess diphenyl ether and terephthaloyl chloride as reaction raw materials, using o-dichlorobenzene as reaction solvent, and under the catalytic action of aluminum chloride. The synthesis process of 1,4-bis(4-phenoxybenzoyl)benzene provided by the present invention successfully overcomes many challenges existing in traditional synthesis methods, such as many side reactions, low yield, and purification difficulties, by optimizing key parameters such as reaction conditions, solvent selection, catalyst dosage, and sample addition order. It is not only easy to operate, but also significantly improves the yield of the target compound, and also ensures the high purity and low impurity content of the product.
Owner:SHANDONG KAISHENG NEW MATERIALS

Synthesis method of saflufenacil

PendingCN119613347Ahigh puritySimplified purification stepsOrganic chemistryChemical synthesisSaflufenacil
The invention provides a synthesis method of saflufenacil, and belongs to the field of chemical synthesis. The preparation method comprises the following steps: reacting N-(2-chloro-4-fluoro-5-aminobenzoyl)-N '-isopropyl-N'-methyl sulfonamide serving as a raw material with chloroformate in a strong polar solvent, then directly adding alkali and ethyl 3-amino-4, 4, 4-trifluoro-2-butenoate into the reaction material, and carrying out cyclization reaction, so as to obtain the N-(2-chloro-4-fluoro-5-aminobenzoyl)-N '-isopropyl-N'-methyl sulfonamide. And carrying out methylation reaction on the cyclization reaction material and a methylation reagent to obtain saflufenacil. The selected reaction solvent is relatively single and easy to recover, so that the reaction operation is simple, the product yield is improved, and the method is suitable for industrial large-scale production and has a wide application prospect.
Owner:YONGNONG BIOSCI

A system for the sustainable synthesis of novel hydrazinylthiazoles via biomass-derived furfural

ActiveDE202025100143U1PhenacylThiazole
A system (100) for the synthesis of hydrazinyl thiazoles from furfural obtained from biomass, wherein the system (100) comprises: configured to deliver 5.0 mmol of hydroxylmethylfurfural (HMF), 5.0 mmol of thiosemicarbazide, and 5.0 mmol of phenacyl tosylate; a grinding unit (104) connected to the reactant delivery unit (102) and configured to grind the reactants under ambient conditions for 5 minutes; a reaction monitoring unit (106) comprising thin-layer chromatography (TLC) and connected to the milling unit (104) and configured to monitor the reaction of the reactants during milling; and a purification unit (108) connected to the reaction monitoring unit (106) and configured to isolate the crude compound, followed by recrystallization using a mixture of ethyl acetate and ethanol.
Owner:BHOSALE LALIT DHANANJAY RATNAGIRI +3

Preparation of N-alkoxyamine HALS from corresponding hydroxylamines

A process for the preparation of a compound of the sterically hindered alkoxyamine class is described, the process comprises the step of alkylating a sterically hindered hydroxylamine compound to a corresponding sterically hindered alkoxyamine by reacting said sterically hindered nitroxyl compound with a compound capable of producing a carbon-central alkyl radical, typically a territorial or secondary alkyl radical, the compounds capable of generating carbon-center alkyl radicals are selected from thermal radical initiators that form radical species in the temperature range of 40 DEG C to 200 DEG C, and from photoinitiators that undergo light excitation when irradiated with UV light or visible light in the range of 180 to 700 nm, in particular UV light in the range of 180 to 380 nm, the compounds capable of generating carbon center alkyl radicals are typically selected from the class of organic peroxides, azo compounds, benzoyl derivatives, benzophenone derivatives, thioxanthone derivatives, benzoin derivatives, benzoyl phosphine oxide derivatives, and the like. The invention relates to a peroxide, for example, selected from the group consisting of diacyl peroxides of formula (A), peracid esters of this formula (A), and oxalic acid peracid esters of formula (D) R-CO-O-O-Z-R (A), r-Z ''-X-CO-CO-O-O-Z''-R (D) wherein each R independently represents a primary or secondary alkyl or cycloalkyl group, preferably comprising from 1 to 15 carbon atoms, and X is oxygen-O-or peroxy-O-O-, Z represents CO or an alkylene group bonded to a quaternary carbon atom, the quaternary carbon atom being an alkylene group of formula (C) R '-C-R' (C), wherein each R'is selected from alkyl groups having 1 to 15 carbon atoms, and Z "represents the alkylene group bonded to a quaternary carbon atom having the formula (C). The described process produces the corresponding O-alkylated derivatives of the sterically hindered hydroxylamines, typically compounds of the class referred to as N-O-alkyl HALS, with very high selectivity and conversion and without the need for the use of catalysts, in particular metal catalysts.
Owner:GENE CHEMISTRY CO LTD

A method for the synthesis of benzoyl modified nucleosides

The application relates to the technical field of organic synthesis, and discloses a synthesis method of a benzoyl modified nucleoside, which comprises the following steps: dissolving or suspending a substrate in a solvent, adding N-chlorosuccinimide, reacting at a certain temperature, generating a corresponding N-chloroamine intermediate, then adding a certain equivalent of benzaldehyde, and generating a final product under the joint action of an oxidant and a catalyst. According to the method, the hydroxyl group on the sugar ring does not need to be protected, and is directly reacted with the amino group on the base, so that the side reaction is less, the obtained product is high in purity, and the yield is high.
Owner:NANJING AIMEITE BIOTECHNOLOGY CO LTD

Trifluoromethyl alkyl quinoline compounds, synthetic methods and antitumor applications thereof

The application discloses a trifluoromethyl alkyl quinoline compound, a synthesis method and anti-tumor application in the field of organic synthesis and medicinal chemistry, which is synthesized from trifluoropropylene quinoline or N-benzoyl pyrrole (A) and redox active ester (B) as raw materials, dimethyl sulfoxide as a solvent, dihydropyridine as an electron donor, and under visible light irradiation, a trifluoromethyl alkyl quinoline and analogues (C) are synthesized at a high yield. The specific reaction formula is as follows: The compounds provided by the application all have excellent anti-tumor activity and low toxicity to normal cells, and therefore have application prospects for preparing anti-tumor drugs.
Owner:ZUNYI MEDICAL UNIVERSITY

Synthesis method of 2-(2-amino-5-bromo-benzoyl) pyridine

The invention provides a synthetic method of 2-(2-amino-5-bromo-benzoyl) pyridine, and belongs to the technical field of medicine synthesis. A one-pot boiling method is adopted, 2-cyanopyridine and 4-bromaniline are used as raw materials, BCl3 is used as a catalyst, dichloromethane is used as a solvent, a heat preservation reaction is performed for 5-25 hours at the temperature of-10 DEG C to 40 DEG C, and the product 2-(2-amino-5-bromo-benzoyl) pyridine is obtained through ethyl acetate extraction, anhydrous sodium sulfate drying and dichloromethane and petroleum ether recrystallization. According to the preparation method of the 2-(2-amino-5-bromo-benzoyl) pyridine, provided by the invention, butyl lithium with extremely high dangerousness does not need to be used, the reaction steps are simple, the yield is stable, the treatment is easy, and the yield is high.
Owner:WEINAN NORMAL UNIV

Production process of cellulose acetate fiber fabric containing natural fragrance

The invention discloses a production process of a cellulose acetate fiber fabric containing natural fragrance, a solvent formed by mixing a modified polymer, 2, 4, 6-trimethylbenzoyl-diphenyl phosphine oxide, a modified microcapsule and dimethylformamide is subjected to dry spinning to prepare the cellulose acetate fiber fabric, and the weight part ratio of the modified polymer to the modified microcapsule is (70-80): (6-8). The preparation method comprises the following steps: by taking an isocyanate group on excessive hexamethylene diisocyanate as a reaction site, firstly reacting with an intermediate containing dihydroxyl, and then reacting with cellulose acetate containing free hydroxyl, so as to prepare the modified polymer. The halamine structure on the molecular chain can destroy cell membranes, enzyme systems or genetic materials through oxidation. The modified capsule has a lavender essential oil and cinnamon essential oil double-component double-capsule-wall structure, the fragrance durability can be improved, the copper sulfide nanoparticles and quaternized chitosan structures can destroy the bacterial cell structure, and the antibacterial performance of the material is improved.
Owner:ZHEJIANG ALICE DYEING & FINISHING CO LTD

Optically switched supramolecular fluorescent polymers, their preparation methods, and their anti-counterfeiting applications in water.

This invention discloses a photosensitive supramolecular fluorescent polymer, its preparation method, and its anti-counterfeiting application in water, using trifluoroethyl methacrylate, hexafluorobutyl acrylate, 4-(acryloyloxy)butyl4-(2-methyl-3-(2-(2-methylbenzo[b]thiophen-3-yl)-4-oxo-5,6-2H-4H-thiaran[2,3-)b]thiaran-3-yl)benzo[b]thiophen-6-yl)-4-oxobutyrate, 4 This polymer was prepared by a simple one-step free radical copolymerization method using 1,1-(acryloyloxy)butyl3-(3,3,4,4,5,5-hexafluoro-2-(2-methyl-1,1-dioxide benzo[b]thiophene-3-yl)cyclopent-1-en-1-yl)-2-methylbenzo[b]thiophene-6-carboxylate 1,1-dioxide and phenylbis(2,4,6-trimethylbenzoyl)phosphine oxide (photoinitiator-819) as raw materials. The polymer exhibits excellent multicolor light-switching performance, high stretch ratio, high self-healing efficiency, strong substrate adhesion, and antifouling properties, especially demonstrating excellent stability under strong acid, strong alkali, and high salt environments. The synthetic route is simple, and it has great application potential in underwater anti-counterfeiting and encryption technologies.
Owner:HUNAN UNIV OF SCI & TECH

Calcipotriol compound, difunctional integrated hydrogel for treating psoriasis as well as preparation and application of difunctional integrated hydrogel

The invention relates to a calcipotriol nano-composite, difunctional integrated hydrogel for treating psoriasis as well as preparation and application of the difunctional integrated hydrogel. The preparation method comprises the following steps: loading calcipotriol on amino-modified mesoporous silica, and then carrying out a one-pot reaction on the amino-modified mesoporous silica, methacrylated gelatin, dopamine methacrylamide, sodium pirolinate carboxylate and phenyl (2, 4, 6-trimethylbenzoyl) lithium phosphate to obtain the difunctional integrated hydrogel. The hydrogel disclosed by the invention is UV-responsive drug-loaded hydrogel, can be quickly cross-linked and adhered to the surface of skin after being irradiated by UV, has the properties of high light transmission, drug sustained release, moisture retention and stable structure, and meets the clinical requirements of synchronous and integrated drug treatment and UV irradiation while remarkably improving the bioavailability of an externally applied drug; organic combination and mechanism complementation of two treatment modes are realized, so that the psoriasis is treated more efficiently.
Owner:THE SEVENTH MEDICAL CENTER OF PLA GENERAL HOSPITAL

Small molecule probe based on imidazo [1, 5-a] pyridine skeleton, preparation method and application

The invention discloses a small molecular probe based on an imidazo [1, 5-a] pyridine skeleton, a preparation method and application, and belongs to the field of activatable small molecular fluorescent probes. The preparation method of the small molecular probe based on the imidazo [1, 5-a] pyridine skeleton comprises the following steps: dissolving 2-benzoylpyridine and ammonium acetate in acetic acid, adding salicylaldehyde, heating and stirring to generate a compound 3; and dissolving the compound 3 in dichloromethane, adding pyridine, stirring, adding 4-bromobutyryl chloride, and continuously stirring to obtain a compound 1, namely the small molecule probe. The small molecule probe can be used for detecting hydrazine in a biological system or drinking water.
Owner:GENERAL HOSPITAL OF NUCLEAR IND

Method for producing macrolide compound

Disclosed are a method for producing pladienolide D that includes a step that reacts a compound represented by formula (A1) with a compound represented by formula (B1) in the presence of a metal catalyst to obtain a compound represented by formula (C1) (in the formulas, X means hydrogen, optionally substituted boryl, optionally substituted stannyl, or optionally substituted silyl, R4 is hydrogen, etc., R5 is optionally substituted benzoyl, etc., and R1 and R2 each independently are hydrogen, etc.) and crystals of a solvate of pladienolide D.
Owner:EISAI R&D MANAGEMENT CO LTD

A benzimidazole amine derivative, a preparation method thereof and use thereof as a beta2-adrenergic receptor allosteric modulator

The application belongs to the field of pharmaceutical chemistry, and specifically discloses a benzimidazole amine derivative, a preparation method thereof and application of the benzimidazole amine derivative as a beta2-adrenergic receptor allosteric antagonist. In the benzimidazole amine derivative, R1 is a hydrogen atom or a bromine atom; and R2 is a substituted benzoyl group or a substituted benzyl group. Pharmacological results show that the benzimidazole amine derivative has good antagonistic activity on beta2AR and can negatively allosterically regulate the functional activity of isoprenaline (ISO).
Owner:CHANGZHOU UNIV

Crystals of N-(benzoyl)-phenylalanine compounds, their pharmaceutical compositions, preparation methods, and uses.

The present invention relates to crystals of N-(benzoyl)-phenylalanine-based compounds, pharmaceutical compositions thereof, preparation methods and uses. Specifically, as shown in Formula (I) and Formula (II), the crystals of the compound of Formula (I) have crystal form A, and the crystals of the compound of Formula (II) have crystal form B. The two crystal forms have good stability, high reproducibility of the preparation method, high operability, and important application value in the prevention and / or treatment of diseases related to α4β7 integrin. [Chemical formula 1] TIFF2025518346000014.tif44156
Owner:HANGZHOU APELOA MEDICINE RES INST CO LTD +1

Preparation method of olaparib intermediate

The invention discloses a method for preparing an olaparib key intermediate compound as shown in a formula (1). The method comprises the following steps: (a) reacting a compound as shown in a formula (2) with a compound as shown in a formula (3) to generate a compound as shown in a formula (4); (b) carrying out intramolecular cyclization on the compound as shown in the formula (4) under the catalysis of acid to generate a compound as shown in a formula (5); (c) hydrolyzing the compound as shown in the formula (5) in an alkali solution, and acidifying to obtain a compound as shown in a formula (1); wherein in the compounds as shown in the formula (3), the formula (4) and the formula (5), R is formyl, acetyl, propionyl, butyryl, benzoyl, methoxycarbonyl, ethoxycarbonyl, t-butyloxycarbonyl, methylsulfonyl, benzenesulfonyl or p-toluenesulfonyl. The invention also discloses a compound shown in a formula (4) or a formula (5). The method is high in yield, mild in reaction condition, easy to purify and suitable for industrial large-scale production. # imgabs0 #
Owner:SHANGHAI BIOBOND PHARMA

Method for preparing dronedarone intermediate

The invention belongs to the technical field of medicine synthesis, and particularly relates to a method for preparing a dronedarone intermediate. According to the preparation method, 2-butyl-5-nitrobenzofuran-3-carboxylic acid is taken as a starting material and reacts with phenol, then rearrangement is carried out, the dronedarone intermediate 2-n-butyl-3-(4-hydroxybenzoyl)-5-nitrobenzofuran is obtained, the route is simple, convenient and efficient, the obtained product is high in yield and purity, and the preparation method is green, environmentally friendly and suitable for industrial production. The use of various metal Lewis acid catalysts can be effectively avoided, and the method is suitable for industrial production.
Owner:SHANDONG NEW TIME PHARMA CO LTD

Synthesis method of 2-butyl-3-(4-hydroxybenzoyl) benzofuran

The invention discloses a synthesis method of 2-butyl-3-(4-hydroxybenzoyl) benzofuran, and relates to the technical field of amiodarone intermediates.The synthesis method comprises the following steps that 2-bromoanisole and 1-hexene-2-alcohol are dissolved in a first solvent, and a first catalyst is added for a reaction; cooling to 25 DEG C, adjusting the pH value to 9-10, adding a catalyst II for reaction, and removing impurities after the reaction is completed, so as to obtain 2-butylbenzofuran; 2-butylbenzofuran and a catalyst III are added into a solvent II, vacuumizing is performed after nitrogen replacement, carbon dioxide is introduced to 0.02-3 MPa for a reaction, impurity removal treatment is performed after the reaction is completed, and 2-butyl-3-(4-hydroxybenzoyl) benzofuran is obtained; compared with a synthetic route in the prior art, the synthetic method has the advantages that the reaction steps are shortened into two steps, the synthetic steps are simplified, the synthetic efficiency is improved, the process cost is reduced, meanwhile, the conversion efficiency is higher, the total yield reaches 70% or above, and the yield is improved by 15% or above compared with the yield in the prior art.
Owner:合肥菁科生物科技有限公司

Pyrimidine derivative containing thiosemicarbazide structure and application thereof

The invention discloses a pyrimidine derivative containing a thiosemicarbazide structure and application of the pyrimidine derivative, and relates to the technical field of medicines, the compound has good oxidation resistance and alpha-glucosidase resistance activity, and the compound is 2-(4, 4 '-difluorophenyl)-2-(4, 4'-difluorophenyl)-2-(4, 4 '-difluorophenyl)-2-(4, 4' The IC50 values of the compound 2-(4, 6-dimethyl pyrimidine-2-yl)-N-methylhydrazine-1-methylsulfamide on DPPH (1, 1-diphenyl-2-picrylhydrazyl) scavenging activity and ABTS (2, 2, 6-dimethyl pyrimidine-2-yl)-N-methylhydrazine-1-methylsulfamide are 3.96 mu g / mL and 2.01 mu g / mL respectively, the IC50 value of the compound 2-(4, 6-dimethyl pyrimidine-2-yl)-N-methylhydrazine-1-methylsulfamide on alpha-glucosidase inhibitory activity is 38.62 mu g / mL, the effect is best, and the compound 2-(4, 6-dimethyl pyrimidine-2-yl)-N-methylhydrazine-1 The pyrimidine derivative containing the thiosemicarbazide structure has a general formula shown in the specification, and is superior to control medicaments such as vitamin C, vitamin E and acarbose.
Owner:KAILI UNIV

Synthesis method of N-protected 2-benzoyl-3-aryl azo indole

The invention discloses a synthesis method of N-protected 2-benzoyl-3-aryl azo indole, which is characterized in that CuNPs (at) HKUST-1 is used as a catalyst, the use of noble metal is abandoned, the use amount is extremely small, and the economical efficiency and the greenness are improved; the synthesis of the 2-aroyl indole compound is efficiently and highly regioselectively realized by using the guiding advantage of the azo substrate of the 2-aroyl indole compound under the nitrogen atmosphere with an equivalent amount of oxidizing agent. The N-protected aryl azo indole which is wide in source and extremely high in research value is used as a raw material, the benzoylformic acid which is rich in reserve is used as an acyl source, and synthesis of the 2-aroyl indole compound is achieved. The raw materials used in the invention are all industrial commodities, and the raw materials are simple to prepare, wide in source, low in price and stable in structure; reaction pollution is small, environmental protection is achieved, and operation is easy.
Owner:XINJIANG UNIVERSITY

The invention relates to a 2-(4apos; continuous synthesis method of-pentylbenzoyl) benzoic acid

The invention provides a continuous synthesis method of 2-(4 '-pentylbenzoyl) benzoic acid, and relates to the field of synthesis of 2-(4'-pentylbenzoyl) benzoic acid. The continuous synthesis method of the 2-(4 '-pentylbenzoyl) benzoic acid comprises the following steps: continuous catalytic reaction and post-treatment. The continuous synthesis method of the 2-(4 '-pentylbenzoyl) benzoic acid can effectively realize continuous and stable synthesis of the 2-(4'-pentylbenzoyl) benzoic acid on the premise of reducing the dosage of the traditional aluminum trichloride catalyst, improves the yield and purity of the continuously prepared 2-(4 '-pentylbenzoyl) benzoic acid, and reduces by-products.
Owner:SHANDONG MORIS TECH +1