140 results about "Phenylsulfonamide" patented technology

The invention provides a process for simply and efficiently preparing a selective cyclooxygenase-2 (COX-2) inhibitor 4-[3-trifluoromethyl-5-(4-methylphenyl)-1H-pyrazolyl]benzenesulfonamide (celecoxib, I). The process comprises the following steps: reacting an alkyl trifluoroacetate and 4-methylacetophenone which are initial raw materials under the action of an organic alkali solution, directly adding a dilute acid, an organic solvent and 4-aminosulfonylhydrazinobenzene or its acid salt to the resulting system, and heating to prepare the celecoxib. Above reaction adopts one kettle way, so the process has the advantages of mild condition, simple operation, high product yield and high product purity, and is suitable for industrialized production.

The invention discloses novel N-4-phenylsulfonamido--N'-1-desoxy-(2-desoxy-2-substituted-amino)-beta-D-glucopyransoylthiocarbamide compounds with the general formula disclosed in the specification, which have the activity of inhibiting carbonic anhydrase and further achieve the effect of resisting tumor metastasis and invasion. The compounds structurally have the three active segments sulfamine, substituted glucosamine and thiocarbamide, and the three active segments and Zn<2+> ions in the carbonic anhydrase form coordinate bonds, thereby inhibiting the catalytic activity of the enzyme and performing the function of resisting tumor metastasis and invasion. Thus, the compounds have application potential in the aspect of antitumor drugs. In the general formula, R is defined in the specification.

The invention discloses a triphosgene method for synthesizing benzene sulphanilamide, the intermediate of glimepiride, a drug for Type ii Diabetes Mellitus. Triphosgene is slowly dropped into a solution which contains phenethylamine and 3-ethyl-4-methyl pyrroline ketone, at a controlled temperature, so that N-[2-(3-ethyl-4-methyl-2-oxidation-3-pyrroline-1-formylamino)ethyl]-benzene (3) is obtained; the product reacts with chlorosulfonic acid to generate sulfonated product; the sulfonated product reacts with ammonia water to generate crude product benzenesulfonamide; the crude product is refined through solvent treatment to generate fine product; the reaction formula is show in the specification. The triphosgene method is simple in technology, simple in operation and high in yield; compared with the conventional method of phosgene, the solid phosgene (triphosgene) method is safer and is convenient to operate.

The invention provides a triazolopyrimidine sulfonamide compound and synthetic methods and application thereof, relating to a penoxsulam analog and a synthetic method and application thereof. The objective of the invention is to overcome the problems of great synthesis difficulty and high cost of conventional penoxsulam. The triazolopyrimidine sulfonamide compound has a structural formula described in the specification. The method 1 comprises the following steps: 1, preparing 2-methyl-3-chlorobenzenesulfonyl chloride; and 2 preparing a finished product so as to obtain 3-chloro-2-methyl-N-(5,8-dimethoxy-[1,2,4] triazolo[1,5-c]pyrimidine-2-yl) benzsulfamide. The method 2 comprises the following steps: 1, preparing 2-mercapto-3-trifluoromethylpyridine; and 2, preparing 3-trifluoromethylpyridine-2-sulfonyl chloride; and 3, preparing a finished product so as to obtain 3-trifluoro-methyl-N-(5,8-dimethoxy-[1,2,4] triazolo[1,5-c]pyrimidine-2-yl) pyridine sulfamide. The triazolopyrimidine sulfonamide compound is used as a herbicide in a rice field.

The invention relates to the technical field of fine chemical engineering, and discloses a method for preparing asymmetric disulfide. The preparation method comprises the following specific steps: taking 3-methylthio-N-phenylpropionamide and diphenyl disulfide as raw materials, taking N-fluorobisbenzenesulfonamide as an additive, and preferably carrying out a reaction in an acetonitrile solvent under a heating condition so as to obtain a target product, namely the symmetric disulfide N-phenyl-3-(phenyldithioalkyl)propionamide. The method is simple and convenient to operate and mild in reaction, 3-methylthio-N-phenylpropionamide and symmetric diphenyl disulfide are used as reaction raw materials, the asymmetric disulfide product is efficiently synthesized in one step, the use of a thiol rawmaterial with unpleasant smell or a transition metal catalyst is avoided, and the method has a potential application value.

The present invention relates to a method of treating cancer in a mammal and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a novel combination comprising the MEK inhibitor: N-{3-[3-cyclopropyl-5-(2-fluoro-4-iodo-phenylamino)6,8-dimethy; -2,4,7-trioxo-3,4,6,7-tetrahydro-2H-pyrido[4,3-d]pyrimidin-1-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, and the PI3 kinase inhibitor: 2,4-difluoro-N-{2-(methyloxy)-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl}benzenesulfonamide, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same, and methods of using such combinations in the treatment of cancer.

The invention discloses a novel fluorocyclopentenone preparation method and a product thereof. The novel fluorocyclopentenone preparation method is characterized by comprising the following step: methyl tert-butyl ether, enynic ester, gold (acetonitrile)[(2-biphenyl)di-tert-butylphosphine] hexafluoroantimonate (I) and N-fluorobenzenesulfonimide are added to react, so that fluorocyclopentenone is obtained. The novel method for preparing a fluorocyclopentenone compound which is provided by the invention ensures that an enynic ester compound can be converted into the fluorocyclopentenone compound. The whole reaction is carried out under normal temperature and normal pressure, conditions are mild, and energy consumption is low. The whole reaction is carried out by utilizing a one-pot method, operation is easy, yield is high, and the purity of the product is 98 percent or more. The reaction substrate range is wide, and not only the simple enynic ester compound but also complex compounds containing natural product groups are applicable. The developed fluorocyclopentenone compound has potential bioactivity, and can become a drug by subsequent testing or modification.

The invention relates to an N-gallic amide-pyrimidine phenyl sulfonamide compound as well as a preparation method and an application of the compound in preparation of medicines for resisting bacteria and promoting the growth of cartilage cells. The N-gallic amide-pyrimidine phenyl sulfonamide compound and a water soluble salt thereof have certain bacteriostatic action on staphylococcus aureus, escherichia coli, pseudomonas aeruginosa, acinetobacter, proteusbacillus vulgaris, pulmonary tuberculosis and the like in vitro, and have an obvious promotion effect on proliferation of bone cells, and synthesis of total protein and glycosaminoglycan in chondrocyte, the gene levels of proteoglycan, II collagen and SOX9 gene can also be regulated upwards, the gene level of I collagen can be inhibited, secretion and synthesis of extracellular matrix of the cartilage can be promoted, and the compound can be applied to preparation of the medicines for treating osteoarthritis.

The invention relates to a heterocyclic benzene sulfonamide compound with a structure as shown in a formula (I) which is described in the specification and an application of the heterocyclic benzene sulfonamide compound in preparation of a ZAK inhibitor. The heterocyclic benzene sulfonamide compound can be used for effectively and highly selectively inhibiting ZAK protein kinase and further regulating the activation of downstream JNK/SAPK, p38, ERK and other pathways. The compound can be used for preparing medicines for preventing and treating various diseases related to ZAK kinase, such as myocardial hypertrophy, myocardial fibrosis, angina pectoris, coronary heart disease, heart failure, myocardial infarction and inflammation, and has the characteristics of better pharmacokinetics, low toxicity and higher druggability.

The present invention relates to a process for preparing storage-stable solid herbicide formulations which comprise herbicidally active compounds from the group of the sulfonamides and their salts, in particular phenylsulfonamides, such as phenylsulfonylaminocarbonyltriazolinones or phenylsulfonylureas, heteroarylsulfonamides and other sulfonamides and their salts.

The invention relates to application of an alkylene phenylsulfonamide compound with a structure of formula (I) (shown in the description) or pharmaceutically acceptable salt thereof or stereisomer thereof or a prodrug molecule thereof in preparation of a ZAK inhibitor. The alkylene phenylsulfonamide compound is capable of effectively and selectively inhibiting ZAK protein kinase and further regulating the activation of multiple routes such as downstream JNK/SAPK, p38 and ERK, can be used for preparing drugs for preventing and treating several ZAK kinase relevant diseases such as myocardial hypertrophy, myocardial fibrosis, stenocardia, coronary heart disease, cardiac failure and myocardial infarction and has the characteristics of relatively good pharmacokinetics, low toxicity and relatively high druggability.

The invention discloses a preparation method for celecoxib isomer, which includes the steps: firstly, preparing a crude product of 4, 4, 4-trifluoro-3-methoxyimino-1-(4-cresyl)-1-butanone from 4, 4, 4-trifluoro-1-(4-cresyl)-1, 3-butanedione with methoxylamine hydrochloride serving as ammoniation protective reagent; and secondly, adding p-amino sulfonyl phenylhydrazine hydrochloride into the prepared crude product, dissolving with ethyl acetate and acetic acid, obtaining a crude product after heating and backflow, and recrystallizing to obtain a pure product of 4-[3-(4-methylphenyl)-5-(trifluoromethyl)-1H-pyrazolyl] benzene sulfonamide, namely, the celecoxib isomer, which is white or almost white crystalline powder in appearance. The preparation method has the advantages of low cost, simplicity in post-processing, high yield and high selectivity.

The invention relates to a fast and efficient method for synthesizing sulfanilamide from acetanilide and the sulfanilamide, and belongs to the field of sulfanilamide synthesis. The method comprises the following steps that acetanilide and chlorosulfonic acid are mixed in carbon tetrachloride; heating is performed to 50 to 60 DEG C; sulfonation reaction is performed for 40 to 60min to obtain sulfonated liquid; under the irradiation effect of ultraviolet light, mixed liquid of the sulfonated liquid and thionyl chloride is heated to 70 to 80 DEG C; chlorination reaction is performed for 40 to 60min to obtain chloridized liquid; liquid materials are atomized in chlorination reaction; p-acetamido benzene sulfonyl chloride obtained through chloridized liquid crystallization is sequentially subjected to amination reaction and hydrolysis reaction. The operation is convenient; the synthesis efficiency is high. The sulfanilamide is prepared by the method; the production is fast; the purity is high.