26 results about "Phenacyl" patented technology

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

The application discloses a cannabidiol derivative and application thereof, and belongs to the technical field of medicinal chemistry. The structural general formula of the cannabidiol derivative is shown as formula (I): (I) R1 is selected from one of hydrogen, chlorine, bromine, a hydroxyl group, a cyano group, an acetoxy group, an acryloyloxy group, a benzoyl group, an acetamide group, an acrylamide group, a propiolamide group, an ethyl thiourea group, a 3-chloro-2,2-dimethylpropionyl group, a 2-ethylsulfonamide acetyl group, a 2-ethylsulfonamide-N-(2-amino-2-oxoethyl) acetyl group, a methylsulfonyl group, an ethylsulfonyl group, a vinylsulfonyl group, an alkyne propylsulfonyl group, a phenylsulfonyl group and a styrylsulfonyl group; and R2 is selected from one of C2-C5 alkyl groups. The cannabidiol derivative disclosed by the application has significantly improved anti-neuroinflammatory activity, significantly reduced cytotoxicity, and a generally improved treatment index of more than 10 times, or even more than 260 times, compared with cannabidiol.

This invention belongs to the field of pharmaceutical technology, specifically relating to novel substituted benzoylpyridinone compounds and their applications. These novel substituted benzoylpyridinone compounds have the general structural formulas shown in (Ⅰ), (Ⅱ), (Ⅲ), (Ⅳ), (Ⅴ), (Ⅵ), (Ⅶ), (Ⅷ), or (Ⅸ), and as antitumor drugs, they exhibit significant EZH2 histone methyltransferase inhibitory activity. This invention provides methods for preparing these compounds, as well as pharmaceutical compositions containing them and their uses. The novel substituted benzoylpyridinone compounds obtained by this invention possess more significant antitumor activity and safety, and are of great value, particularly as antitumor agents, in EZH2, PRC2, and EZH2 / PRC2-mediated diseases.

This invention discloses a synthetic chiral N -benzoyl- N The method for synthesizing dihexylamino-thio-phenyl sulfoxide imine belongs to the field of organic synthesis. Starting with sodium benzenesulfinate, a key intermediate, chlorosulfoxide imine, is obtained through a multi-step reaction. Then, the following steps are employed: A) an asymmetric chloro-fluorine exchange reaction at a hexavalent sulfur center yields an optically active fluorinated sulfoxide imine, which undergoes a nucleophilic substitution reaction with di-n-hexylamine to give the R-type product; B) using a bifunctional small organic molecule catalyst, 4-arylpyridine N-oxygenate, as the catalytic system, a nucleophilic substitution reaction is carried out with di-n-hexylamine to asymmetricly synthesize the S-type product. This method is characterized by mild conditions, simple steps, high overall yield, and chiral product. N -benzoyl- N Dihexylamino-thiophenyl sulfoxide imine exhibits micromolar levels of biological activity in human lung cancer cells.

The present invention belongs to the field of pharmaceutical chemistry, and relates to an N-(benzoyl)-phenylalanine compound used as an α4β7 integrin antagonist, including the pharmaceutical composition and the use, and in particular to a compound represented by general formula (1). The compound exhibits good α4β7 integrin binding inhibitory activity, can be used as a high-efficiency α4β7 integrin antagonist, and used for preventing and / or treating α4β7 integrin-related diseases such as autoimmune diseases and inflammatory diseases.

Described herein are 1,4-substituted piperidine compounds according to Formula I that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described 1,4-substituted piperidine compounds. Also described herein are methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the described 1,4-substituted piperidine compounds and synthetic intermediates useful in those syntheses.

The present application relates to a kind of photoinitiator and its preparation method and application, the photoinitiator includes 2,4,6-trimethyl benzoyl phenyl methyl phosphonate, the melting point of the photoinitiator is 53-57 ℃.The photoinitiator described in the present application has the characteristics of light color, low yellowness, little smell, good fluidity and high storage stability, and has good solubility in monomer, can also play the role of dispersant, the curing rate of the photo-curing system formed is fast, the adhesion on the surface of different plastic substrates is high, and the comprehensive performance is excellent.

Disclosed in the present invention is a process for preparing a key intermediate of fluopyram. The key intermediate is dimethyl [3-chloro-5-(trifluoromethyl)pyridin-2-yl]({[2-(trifluoromethyl)benzoyl]amino}methyl)malonate. The process comprises the following steps: in the presence of a solvent 1, reacting the compound potassium dimethyl 2-[3-chloro-5-(trifluoromethyl)pyridyl]malonate with the compound 1-D in a reaction container, and recovering the solvent 1 by means of distillation, so as to obtain the intermediate compound, wherein the solvent 1 is selected from acetic ester solvents having a boiling point range of 40-110°C at a normal temperature and a normal pressure. The process of the present invention 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 require any post-purification treatment, and can be directly used for the synthesis of fluopyram; and the process can be amplified, and is beneficial for cost reduction, efficiency improvement and commercial mass production.

The application discloses a five-membered double-spiro indoline derivative and a preparation method and application thereof, and a structure formula of the five-membered double-spiro indoline derivative is shown as formula (III); wherein, R 1 is selected from hydrogen, an alkyl group or halogen; R 2 is selected from hydrogen, an alkyl group, an allyl group, a benzyl group or a benzoyl group; R 3 is selected from a phenyl group, a naphthyl group, a biphenyl group, a thienyl group, a furanyl group, an alkylphenyl group, a halogenphenyl group, an alkoxyphenyl group, a nitrophenyl group or a trifluoromethylphenyl group; R 4 is selected from an alkylphenyl group, a halogenphenyl group or a nitrophenyl group. The five-membered double-spiro indoline derivative of the application is synthesized by a one-step method, high atom economy and high yield, not only simplifying a synthesis route, but also reducing production cost, and because of the green chemical characteristics, reducing the influence on the environment. The five-membered double-spiro indoline derivative is found to have an antifungal and antibacterial effect.

The present invention relates to a chemical process for the synthesis of the compound 8-[(2-hydroxybenzoyl)amino]octanoic acid or a derivative thereof useful in the process of making sodium 8-[(2-hydroxybenzoyl)amino]octanoate (SNAC), a delivery agent used in solid pharmaceutical compositions. The invention provides an efficient synthesis using less hazardous chemicals and / or a reproducible process that is easier to handle on production scale.

The application discloses a kind of UV solidification degradable polyester acrylate pressure-sensitive adhesive and preparation method thereof, belong to adhesive technical field.The pressure-sensitive adhesive with acryloyl ε-caprolactone, lactide and triethylene carbonate ring-opening random copolymer as prepolymer, with bio-based castor oil acrylate active diluent, conventional acrylate active diluent, multi-functional acrylate as active crosslinking diluent, phenyl bis (2, 4, 6-trimethyl benzoyl) phosphine oxide and 1-hydroxycyclohexyl phenyl ketone etc. are prepared into UV solidification as photoinitiator.The pressure-sensitive adhesive mass fraction is composed of: degradable polyester acrylate accounts for 50-75wt%;Castor oil-based acrylate accounts for 5-30wt%;Active diluent accounts for 0.5-20wt%;Photoinitiator accounts for 1-5wt%.The pressure-sensitive adhesive has high adhesion, and is suitable for bonding performance requirement is high, degradable occasion.

The present application provides a novel organic compound and an organic ionic compound having excellent light absorption properties. The organic compound of an embodiment of the present application has a structure represented by the following formula (1). In formula (1), R 1 represents at least one selected from a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, and a substituted or unsubstituted phenyl group; R 2 represents at least one selected from a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, an alkylcarbonyl group having 1 to 4 carbon atoms, a substituted or unsubstituted phenyl group, a substituted or unsubstituted benzoyl group, and a carboxymethyl group; and X represents an organic group having a heterocyclic skeleton containing at least one oxygen atom, nitrogen atom, or sulfur atom in the ring.

The application discloses a 2-benzoylindole compound shown in a formula I and application of the 2-benzoylindole compound. The 2-benzoylindole compound can be used as a selective estrogen receptor downregulator (SERD) and is used for preparing a medicine for preventing and / or treating diseases mediated or dependent on an estrogen receptor in a living body.

This invention belongs to the field of polyurethane elastomer synthesis technology, specifically relating to a method for synthesizing a multifunctional polyurethane elastomer, comprising the following steps: adding polytetrahydrofuran to a four-necked flask, then adding dicyclohexylmethane-4,4'-diisocyanate, and stirring the mixture under a nitrogen atmosphere for 1 hour; finally, adding the catalyst dibutyltin dilaurate and prepolymerizing the mixture for 3 hours to obtain a prepolymer PM-NCO; adding a polymerization inhibitor and tetrahydrofuran to the obtained prepolymer PM-NCO, followed by adding N-(hydroxymethyl)acrylamide until the -NCO peak disappears in the FTIR spectrum to obtain PMN; cooling the reaction to room temperature under a nitrogen atmosphere, and then placing the obtained PMN, lipoic acid, phenylbis(2,4,6-trimethylbenzoyl)phosphine oxide, and diethylaluminum hypophosphite into a vacuum degasser and stirring thoroughly to obtain PMNSx-n; the method for synthesizing a multifunctional polyurethane elastomer provided by this invention can fundamentally solve the contradiction between flame retardant modification and intelligent self-healing properties.

This invention belongs to the field of gel preparation technology, specifically relating to a self-gelling powder with a dehydration-induced highly entangled dual-network structure and its preparation method. The invention uses carboxymethyl chitosan, acrylamide, genipin, N,N'-methylenebisacrylamide, and the photoinitiator 2,4,6-trimethylbenzoyldiphenylphosphine oxide as raw materials. After photo-initiated polymerization and thermal dehydration treatment, a highly entangled carboxymethyl chitosan / polyacrylamide dual-network gel is obtained. This gel is then freeze-dried and pulverized to obtain a self-gelling powder with a dehydration-induced highly entangled dual-network structure. The freeze-dried powder of this invention can rapidly rebuild a stable three-dimensional network after absorbing water, exhibiting rapid self-gelling ability. Simultaneously, it greatly improves the storage stability of the material, extends its shelf life, and solves the storage problems of liquid or semi-solid gel products.

This invention relates to the field of organic compound synthesis technology, specifically to a spirocyclooxanthone compound, its preparation method, and its applications. 2-[4-(dihexylamino)-2-hydroxybenzoyl]benzoic acid is reacted with 4-bromo-3-methylphenol under concentrated sulfuric acid catalysis. The reaction product is post-treated to obtain a crude product, which is then separated and purified to obtain 2'-bromo-6'-(dihexylamino)-3'-methyl-3H-spiro[isobenzofuran-1,9'-xanthones]-3-one. This one-pot acid-catalyzed tandem cyclization method efficiently and selectively constructs complex spirocyclooxanthone skeletons in one step, solving key problems in traditional multi-step synthesis such as cumbersome steps, low yield, harsh conditions, and difficulty in controlling regioselectivity. It achieves the preparation of spirocyclooxanthone derivatives with high yield, high purity, and a simple process.

This invention relates to the field of polyvinyl chloride resin technology, and discloses a β-diketone PVC auxiliary heat stabilizer, its preparation method, and its application. The β-diketone PVC auxiliary heat stabilizer has a structure as shown in Formula I or Formula II. This invention designs a type of furanyl group with stronger electron-withdrawing properties to replace the stearoyl group in SBM or the benzoyl group in DBM. The β-diketone produced has increased electron-withdrawing properties of the furan ring, and the hydrogen atom of the methylene group between the two formyl groups is more easily freed. The furan β-diketone is more reactive and can participate better in the heat stabilization reaction of various PVCs, resulting in better heat stabilization effect.

The application belongs to the field of chemical synthesis, and particularly relates to a preparation method of 5-benzoyl dihydrofuran-2(3H)-one and derivatives thereof. The preparation method is as follows: five-membered ring, six-membered ring aromatic and heterocyclic compounds, and substituted glutaric anhydride are used as raw materials, aluminum chloride is used as a catalyst, a solvent is simply distilled out, and phenyl dihydrofuran-2(3H)-one and derivatives are prepared by one-pot method with iodobenzene acetate as an oxidant. The reaction condition is simple, the reaction temperature is 40-60 DEG C, no noble metal catalyst is used in the scheme disclosed in the application, no heavy metal residue is caused, the raw materials used are commercial products, the oxidant and the catalyst are relatively inexpensive and easy-to-obtain substances, the reaction operation is simple, and the reaction product is easy to purify and the post-treatment is convenient.

The application discloses a kind of 1,4-di (4-fluorobenzoyl) phenol production waste utilization process, it belongs to 1,4-di (4-fluorobenzoyl) phenol production technical field, including the following steps, waste scraps are dissolved in solvent and active carbon adsorption is removed pigment and solid particles in scrap material;The pretreated scrap material is subjected to dehalogenation hydrogenation under the condition of hydrogenation catalyst and alkaline substance, and 1,4-biphenyl acyl benzene is produced;The hydrogenation product is separated and purified using solution crystallization, and 1,4-biphenyl acyl benzene with a purity of 99.75% or more is obtained.The application uses waste scraps to produce 1,4-biphenyl acyl benzene, improves the utilization rate of raw materials, reduces the amount of hazardous waste emissions, and is green and environmentally friendly.

This invention discloses an N-aryl(2-acylaminobenzoyl)aminoamide compound, its preparation method, and its uses. This compound is generated by reacting Boc-amino acids and aromatic amines in dichloromethane under the action of EDCI, DMAP, and triethylamine. The N-Boc-aminobenzoyl compound is then acid-hydrolyzed with trifluoroacetic acid to obtain an aminobenzoyl compound. Next, the aminobenzoyl compound is reacted with indomethacin anhydride in acetonitrile under the action of potassium carbonate to generate a diamide compound. Finally, the diamide compound is reacted with an acyl halide in the action of triethylamine to obtain the N-aryl(2-acylaminobenzoyl)aminoamide compound. The raw materials used in the synthesis are inexpensive and readily available, and the synthesis method is simple. This compound exhibits good inhibitory activity against crop pathogens, particularly against Sclerotinia sclerotinia, Phytophthora blight, Fusarium head blight, rice blast fungus, gray mold, sheath blight, and rot fungus.

The application discloses a method for synthesizing 1,4-di(4-fluorobenzoyl)benzene by using ultrasonic waves, and belongs to the technical field of Friedel-Craft reaction. In the method, trifluoromethanesulfonic acid compounds are used as catalysts, fluorobenzene and terephthaloyl chloride are catalyzed to synthesize 1,4-di(4-fluorobenzoyl)benzene under the action of ultrasonic waves; the trifluoromethanesulfonic acid compounds are selected from any one of Bi(OTf)3, La(OTf)3, Sn(OTf)2 and TfOH. In the method, trifluoromethanesulfonic acid compounds are used as catalysts, the catalysts are separated by filtering and rectifying, and a large amount of acidic waste liquid is avoided; meanwhile, the reaction time is shortened, the reaction yield is improved, and the production cost is reduced by combining with ultrasonic wave intensification.