59 results about "Phenylsulfonamide" patented technology

The invention provides a six-membered sultam derivative as well as an electrochemical synthesis method and application thereof, and a 2-isoallylbenzenesulfonamide derivative and a hydroxyl-containing compound are electrified and reacted in an electrolyte to obtain the six-membered sultam derivative. The electrolyte comprises 2, 2, 6, 6-tetramethylpiperidine and an electrolyte tetrabutylammonium tetrafluoroborate; compared with the prior art, the sultam derivative can be obtained through reaction under the electrochemical condition, no oxidizing agent or reducing agent is needed in the reaction, no metal catalyst or high temperature is needed, synthesis steps are simple, side reactions are few, the yield of the target product is high, and the method can be used for industrial production.

The invention discloses a synthesis method of a Vinetoram key intermediate and Vinetoram, and relates to the technical field of organic synthesis.The synthesis method comprises the steps that 1-((4 '-chloro-5, 5-dimethyl-3, 4, 5, 6-tetrahydro-[1, 1'-biphenyl]-2-yl) methyl) piperazine hydrochloride and 2-((1H-pyrrolo [2, 3-b] pyridine-5-yl) oxy)-4-bromobenzoic acid methyl ester are used as reaction raw materials, a reaction is carried out, and the Vinetoram key intermediate and the synthesis method of the Vinetoram key intermediate are synthesized; the method comprises the following steps: carrying out a substitution reaction and a hydrolysis reaction to obtain a key intermediate of the Venotocork, and carrying out a condensation reaction on the intermediate and 3-nitro-4-((tetrahydro-2H-pyran-4-yl) methylamino) benzenesulfonamide to obtain the Venotocork. The synthesis method has the advantages of short process route, easily available raw materials, mild reaction conditions, high yield and purity of the intermediate and the Vinetoram, facilitation of the improvement of the yield and quality of the Vinetoram, and reduction of the production cost of the Vinetoram.

The application relates to a synthesis method of a phenothiazine derivative, and belongs to the technical field of synthesis in organic chemistry. A diaryl iodonium salt and N-(2-mercapto phenyl)-4-methyl benzene sulfonamide are used as starting materials, and chlorpromazine and perphenazine are obtained through a plurality of steps of substitution reaction, reduction reaction, addition reaction and deprotection reaction. In the application, the reaction raw materials are easy to obtain, the yield is high, and chlorpromazine and perphenazine can be successfully obtained.

The application discloses an amino benzene sulfonamide derivative and application thereof. The structural general formula of the amino benzene sulfonamide derivative is shown in the following formula. The amino benzene sulfonamide derivative has good pepsin inhibitory activity, can effectively block the adhesion and reactivation of pepsin in the pharyngeal mucosa, and has super high selectivity in the internal proteinase family compared with other non-specific protease inhibitors, thereby significantly reducing the off-target risk of normal physiological proteases in the human body. In addition, the compound is particularly suitable for local spray administration in the throat, can maintain a high concentration in the lesion site, and overcomes the defect of traditional oral antacid drugs in the insufficient effect on non-acid reflux, thereby providing a new solution for the treatment of throat reflux diseases.

The application belongs to the technical field of biomedicine, and particularly relates to a benzene sulfonamide derivative and application thereof in antidepressant drugs. The structural general formula of the compound is (I). The compound or a pharmaceutically acceptable salt thereof has agonistic activity on 5-hydroxytryptamine 2A type receptors. The compound is determined to have good antidepressant activity through a mouse tail suspension test model, an open field test model and a forced swimming test model, is a novel antidepressant compound with wide application prospect, has no hallucinogenic effect, and can be developed into an antidepressant therapeutic drug.

A method for preparing N-phenyl-N-trichloromethylthio phenyl sulfonamide by one-pot method, organic solvent, aniline and catalyst are added to phenylsulfonyl chloride, then slow addition of acid binding agent, incubation for 1-4 h to obtain a reaction solution containing intermediate N-phenyl phenyl sulfonamide; the system is cooled to 0-20℃, slow addition of per-chloromethylthio alcohol, after the end of feeding, continue to react for 1-4 h; then add water to separate the phases, add appropriate amount of water in the organic phase to distill the organic solvent, filter to obtain N-phenyl-N-trichloromethylthio phenyl sulfonamide. The method uses organic solvent as solvent, adopts two-step reaction one-pot method, the process is simple, improves the reaction conversion rate, effectively reduces the generation of by-products, the yield of the product is high, and the quality is good. The used organic solvent and acid binding agent can be recycled and used, which reduces the production cost and greatly reduces the three wastes, and is suitable for industrial production.

The application relates to a method for preparing an eight-membered selenium-containing benzazepine compound, which comprises the following steps: taking an N-(but-3-en-1-yl)-4-methyl-N-(2-(1-phenylvinyl)phenyl)benzenesulfonamide compound as a substrate, generating a selenyl radical through anodic oxidation of a selenide under electrochemical driving, and obtaining the eight-membered selenium-containing benzazepine compound through radical coupling-cyclization of the selenyl radical and the substrate. The method steps have the advantages of green simple operation, use of traceless electrons instead of an external oxidizing and reducing agent, avoidance of use of a metal catalyst and an external oxidizing and reducing agent, economy, simple and easy-to-prepare raw materials, wide substrate range and the like.

The invention provides a method for synthesizing celecoxib by a one-pot aqueous phase method. The preparation method comprises the following steps: firstly, directly reacting p-methylacetophenone and ethyl trifluoroacetate in one pot under the action of N, N-dimethyl butylamine to obtain a beta-diketone intermediate; in the other pot, p-chlorobenzenesulfonamide and hydrazine hydrate are used as raw materials, a p-hydrazinobenzenesulfonamide solution is generated under the action of N, N-dimethyl butylamine, and the operation is carried out in the two pots at the same time; and finally, adding the p-hydrazinobenzenesulfonamide solution into the beta-diketone intermediate material liquid, combining in two pots, adjusting the acid, heating for reaction, and cooling for crystallization to obtain celecoxib. According to the method disclosed by the invention, the p-hydrazinobenzenesulfonamide aqueous solution is creatively used for participating in the synthesis reaction of the celecoxib, and solid p-hydrazinobenzenesulfonamide hydrochloride does not need to be independently used for participating in the reaction, so that the use of a large amount of acid and the generation of high-temperature acid waste liquid during the production of the p-hydrazinobenzenesulfonamide hydrochloride are avoided. The method does not need any post-treatment operation and high-temperature salt forming link, and is more suitable for industrial production.

The application provides a 4-quinazolinone derivative containing a benzene sulfonamide piperazine ketone and a preparation method and application thereof. The derivative has the structure shown in the following general formula I. The application further relates to a preparation method of a compound containing the structure of formula I and application of the compound as an HIV-1 / HIV-2 capsid protein regulator in preparation of an anti-AIDS drug.

The invention provides a benzenesulfonamide derivative, a preparation method thereof and application of the benzenesulfonamide derivative in preparation of PARP1 inhibitors and antitumor drugs, and belongs to the technical field of medicines. The invention synthesizes a novel benzenesulfonamide derivative, namely a compound N, 4-dimethyl-N-(7H-pyrrolo [2, 3-d] pyrimidine-4-yl) benzenesulfonamide, and the benzenesulfonamide derivative provided by the invention can inhibit PARP1 enzyme activity in a targeted manner so as to inhibit DNA repair, activate a p53-mediated DDR signal channel, inhibit DNA repair and inhibit the expression of a p53-mediated DDR signal channel. The benzenesulfonamide derivative can induce apoptosis of lung cancer tumor cells and influence the cycle of the lung cancer tumor cells, has remarkable antitumor activity, and is simple in synthesis method, easy in raw material obtaining, high in synthesis route yield, environment-friendly and simple and convenient in operation process. The PARP1 inhibitor disclosed by the invention is simple in preparation process, high in drug purity, high in yield, stable in quality and easy for large-scale production. The compound disclosed by the invention has a wide prospect in the aspects of development and application of antitumor drugs.

A benzene sulfonamide compound of formula I or one of its addition salts with pharmaceutically acceptable acids, for use in a method of treating a pathology related to an excessive effect of TNF and for use in a method of treating the human or animal body.

The invention discloses a ruthenium complex of targeted carbonic anhydrase as well as a preparation method and application of the ruthenium complex. The complex takes ruthenium (Ru < 2 + >) as a central metal ion, is formed by coordinating a bidentate ligand (An-en) containing an anthracene structure, a pyridine derivative ligand (N-ABS) containing a benzenesulfonamide group and a ruthenium precursor, and has the capability of accurately targeting tumor cell carbonic anhydrase IX (CAIX); the complex is low in dark toxicity and excellent in curative effect in an anoxic environment, the defects that a traditional ruthenium complex is high in dark toxicity and poor in anoxic curative effect can be effectively overcome, and an efficient and low-toxicity new strategy is provided for anoxic tumor treatment.

The invention discloses an application of N-(4-methoxyphenyl)-4-(4-methoxyphenyl) benzenesulfonamide in preparation of drugs for treating allergic diseases, and belongs to the technical field of biological medicines. The invention discloses a new pharmaceutical application of N-(4-methoxyphenyl)-4-(4-methoxyphenyl) benzenesulfonamide for the first time, and the N-(4-methoxyphenyl)-4-(4-methoxyphenyl) benzenesulfonamide serving as an anti-allergic antagonist can effectively inhibit phospholipase C activity of stimulated cells and mediated calcium mobilization thereof in vitro. And the effective dose of the desloratadine, which is a positive drug, is lower in vivo to generate a comparable anti-allergic effect with the desloratadine. Meanwhile, in animal models of allergic rhinitis and atopic dermatitis, compared with a positive drug desloratadine, the compound can effectively inhibit the pathological progress of diseases at a lower dosage. Therefore, the compound has a definite effect of inhibiting in-vitro and in-vivo anaphylaxis, and can be effectively applied to the development of drugs for treating allergic diseases.

The invention provides an aggregation-induced emission (AIE) ionic probe (E)-4-(2-(5-(4-(diphenylamino) phenyl) thiophene-2-yl) vinyl)-1-(4-sulfanilamide acyl benzyl) quinoline-1-onium hexafluorophosphoric acid (V) salt of a targeted golf apparatus, namely a fluorescent probe TTQ-GA, a preparation method of the fluorescent probe TTQ-GA and application of the fluorescent probe TTQ-GA in the aspect of detection. The benzenesulfonamide group of the probe can be selectively combined with a Golgi apparatus protein cyclooxygenase 2 (COX-2) inhibitor SC-558 to realize Golgi apparatus targeting; due to the hydrophobic triphenylamine part and the hydrophilic quinoline cation part of the probe, the probe has amphipathy; the probe does not emit fluorescence in an aqueous solution, and can emit strong fluorescence when molecular movement is limited and excited, so that no-wash marking of the Golgi apparatus is realized; the probe generates a large amount of ROS under light excitation, promotes local lipid peroxidation increase of Golgi apparatus, and promotes cancer cell apoptosis.

The application provides a synthesis method of 2-(phenyl sulfonamide)-3-oxo-3-heterocyclic propionic acid ester compounds and belongs to the technical field of organic synthesis. The preparation method comprises the following steps: adding heterocyclic formyl acetic acid ethyl ester compounds, sulfonamide compounds and a photosensitizer into a solvent to configure a reaction solution, performing reaction under blue light irradiation, and preparing a target product after the reaction is completed. The application avoids the problem of a large amount of by-products caused by various oxidants in a traditional method; the organic photosensitizer 4CzIPN is used as a catalyst, the reaction time is greatly shortened, the reaction can be completed in only 10 minutes, the reaction efficiency is improved, and the product does not have metal residues; the reaction condition is mild, and the reaction can occur at room temperature in an air atmosphere.

The invention discloses a small-molecule inhibitor based on lactic dehydrogenase targeted design and application thereof, and belongs to the field of biological medicine, the small-molecule inhibitor is a benzenesulfonamide compound or pharmaceutically acceptable salt thereof, and the structure of the small-molecule inhibitor is shown in the specification. The lactic dehydrogenase inhibitor is suitable for treating and / or preventing diseases mediated by lactic dehydrogenase.

The present inventors have shown that specific benzene sulfonamide thiazole compounds (I) have the ability to induce an early endoplasmic reticulum stress. These compounds also lead to cancerous cells growth inhibition and death.

The application provides a benzene sulfonamide piperazine ketone glycine derivative and a preparation method and application thereof. The derivative has a structure shown in the following general formula I. The application also relates to a preparation method of a compound containing the structure of formula I and application of the compound as an HIV-1 / 2 capsid protein regulator in preparation of an anti-AIDS drug.

A compound of Formula (I) is provided: (I) Salts and crystalline forms of the compound of Formula (I) are also provided. The compound of Formula (I) and crystalline forms thereof can be used for the treatment of several conditions linked to the inhibition of SGK-1, such as a cardiovascular disease selected from the group consisting of Long QT syndrome, heart failure, arrhythmia, ischemic injury, ischemic infarction, inflammatory and fibrotic diseases, cardiac fibrosis, vascular proliferation, restenosis, dilated cardiomyopathy, and stent failure; cancer; epilepsy; Parkinson's disease; and Lafora disease.

The application discloses a series of 4-piperazine thiourea phenyl sulfonamide-1,8-naphthalimide derivatives with various structures and a preparation method of the derivatives. Test results show that some target compounds have good inhibitory activity on CA IX, and can be used for preparing drugs for inhibiting carbonic anhydrase IX enzyme activity and / or overexpression. Some target compounds have good antitumor activity on various tumor cell strains, and are expected to be used for preparing antitumor drugs.

The invention relates to a preparation method of 4 '-chloro-2-aminobiphenyl, and relates to the technical field of organic synthesis.The preparation method comprises the following steps that p-dichlorobenzene, a sulfur trioxide-pyridine compound and thionyl chloride are subjected to a reaction, and 2, 5-dichlorobenzene sulfonyl chloride is obtained; the preparation method comprises the following steps: reacting 2, 5-dichlorobenzenesulfonyl chloride, aniline hydrochloride and a sodium bicarbonate solution to obtain 2, 5-dichloro-N-phenylbenzenesulfonamide; the preparation method comprises the following steps: reacting 2, 5-dichloro-N-phenylbenzenesulfonamide, cysteine, a titanium dioxide nanotube and a hydrogen peroxide solution to obtain 2-chloro-6H-dibenzothiazine dioxide; the preparation method comprises the following steps: reacting 2-chloro-6H-dibenzothiazine dioxide, zinc powder and glacial acetic acid to obtain an intermediate; and mixing the intermediate, p-toluenesulfonic acid and a solvent, and carrying out microwave-assisted hydrolysis to obtain 4 '-chloro-2-aminobiphenyl. The method has the effects of improving the yield and purity of the product, and meanwhile, the environmental protection property and economical efficiency of the process are improved.

This invention discloses a benzamide / benzenesulfonamide compound containing an aryl butanone structure, its preparation method, and its application, belonging to the field of medicinal chemistry. The structure of the benzamide compound containing the aryl butanone structure is as follows: R1 is hydrogen, halogen, alkyl, or alkoxy; R2 is tert-butyl, tert-pentyl, tert-octyl, adamantyl, or α,α-dimethylbenzyl; R3 is hydrogen, halogen, alkyl, alkoxy, fused ring, or aryl; R4 is hydrogen, alkyl, or aryl. The structure of the benzenesulfonamide compound containing the aryl butanone structure is as follows: R1 is hydrogen, halogen, or alkyl; R2 is tert-butyl, tert-pentyl, or tert-octyl; R3 is hydrogen, halogen, alkyl, or fused ring. The advantages of this invention are that some of the prepared compounds exhibit strong inhibitory effects on MCF-7 and HCT-116, and can be used as lead compounds for the subsequent preparation and development of antitumor drugs.

Compounds of Formulae I and II are disclosed: I II In compounds of formula I, R 1 is -OH or -NHC(=O)R10. The compounds of formula I are therefore benzenesulfonic acids or N-(phenylsulfonyl)carboxamides. The compounds of formula II are benzenesulfonamides. All of the compounds of formula I are MGAT2 inhibitors and are useful to treat obesity and metabolic dysfunction-associated steatotic liver disease (MASLD). All of the compounds of formula II are useful as intermediates in synthesizing N-(phenylsulfonyl)carboxamides of formula II, and a subset of compounds of formula II are also MGAT2 inhibitors and are useful to treat obesity and metabolic dysfunction-associated steatotic liver disease (MASLD).

Compounds are provided that act as potent antagonists of the CCR(9) receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR(9). The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR(9)-mediated diseases, and as controls in assays for the identification of CCR(9) antagonists.

The present disclosure relates to processes for the fluorination of molecules. One aspect provides a process for incorporating a fluorine atom into a molecule, said process comprising converting a compound of formula X-SG into a compound of formula X-F, wherein G is an optionally substituted C1-C6 alkyl group, an optionally substituted aryl group, or an optionally substituted heteroaryl group, and X is an organic group; and wherein the SG group is attached to a secondary or tertiary carbon atom in the organic group X; said process comprising treating said compound of formula X-SG with (i) an activator compound selected from the group consisting of N-halosuccinimides, N-halobenzenesulfonimides, N-halobenzenesulfonamides, dialkylaminodihalosulfinium salts, heterocyclylaminodihalosulfinium salts, dialkylaminosulfur trihalides, XeF2, difluoroiodotoluene, di- and tri-bromoisocyanuric acids, bromine, chlorine, hypervalent iodine compounds with I2; and other sources of Br+, Cl+, F+, I+, bromonium, iodonium, or chloronium; and (ii) a source of fluoride. Uses of the process in the preparation of various fluorinated molecules as well as uses of certain compounds as intermediates in the processes of the present disclosure are also provided.

The present disclosure provides a novel salt of 5-chloro-2-fluoro-4-((4-fluoro-2-(methyl(2-(methylamino)ethyl)amino)phenyl)amino)-N-(thiazol-4-yl)benzenesulfonamide and a method for preparing the same. The mesylate salt of 5-chloro-2-fluoro-4-((4-fluoro-2-(methyl(2-(methylamino)ethyl)amino)phenyl)amino)-N-(thiazol-4-yl)benzenesulfonamide, which may be prepared using methanesulfonic acid and, without wishing to be bound by theory, can exhibit reduced hygroscopicity and improved physicochemical stability and solubility. In some aspects, the present disclosure provides a pharmaceutical composition for preventing or treating a sodium channel blocker-related disease, comprising the mesylate salt of 5-chloro-2-fluoro-4-((4-fluoro-2-(methyl(2-(methylamino)ethyl)amino)phenyl)amino)-N-(thiazol-4-yl)benzenesulfonamide.

The invention discloses a benzenesulfonamide triazole derivative as well as a preparation method and application thereof, and is characterized in that the benzenesulfonamide triazole derivative has a structural formula shown as a formula I and a formula II or pharmaceutically acceptable salt, ester or solvate of the benzenesulfonamide triazole derivative with the structural formula shown as the formula I and the formula II, x is a carbonyl group, a sulfonyl group or a sulfuryl group; r1 is o-fluorophenyl, p-trifluoromethoxyphenyl, o-methoxyphenyl, o-methoxyanilino, p-methoxyphenyl, pyrimidine, thiazole, oxazole, methylthiophene, amino and methylamino, and the compound has the advantages that the compound can effectively inhibit CDK, the selectivity to CDK1 is higher than that of other subtype and / or eukaryotic tumor cell proliferation, and tumors are prevented and / or treated.

The invention belongs to the technical field of medicinal chemistry, and particularly relates to phenyl sulfanilamide para-triazole derivatives, a preparation method and application of the phenyl sulfanilamide para-triazole derivatives in resisting carbonic anhydrase. The structural general formula of the derivative is as shown in formula I, the invention provides a brand-new phenyl sulfanilamide para-triazole derivative and pharmaceutically acceptable salt, the inhibition activity of the derivative on human carbonic anhydrase is obviously superior to that of traditional inhibitors acetazolamide and methazolamide, and the derivative has selective binding capacity on different human carbonic anhydrase subtypes and has the potential to be developed into a novel carbonic anhydrase inhibition drug.

The invention is directed to the use of carbonic anhydrase V inhibitors for treatment of neurological and psychiatric disorders. In one aspect, the disclosure provides compositions for treating or preventing a neurological or psychiatric disease or disorder comprising a mitochondrial carbonic anhydrase V (CA-V) inhibitor. In various embodiments, the mitochondrial CA-V inhibitor selectively inhibits at least one or more of CA-VA and CA-VB. In some embodiments, the chemical compound is 4-phenylacetamidomethyl-benzenesulfonamide (4ITP), derivative, and analogs thereof.