35450-53-4

Usage

General Description

p-(2-acetamidoethyl)benzenesulphonyl chloride is a synthetic organic compound used in the pharmaceutical industry. It is a sulphonyl chloride derivative, which means it contains a sulphonyl group attached to a benzene ring. This particular compound also has an acetamidoethyl group attached to the benzene ring. The presence of the sulphonyl chloride functional group makes it a potent reagent for the synthesis of various pharmaceutical compounds, particularly those based on sulphonamides. Its reactivity and specificity make it a valuable tool in the production of sulphonyl-containing drugs, as well as in research and development of new pharmaceuticals. However, due to the reactivity of the sulphonyl chloride group, caution must be exercised in handling and using p-(2-acetamidoethyl)benzenesulphonyl chloride.

InChI:InChI=1/C10H12ClNO3S/c1-8(13)12-7-6-9-2-4-10(5-3-9)16(11,14)15/h2-5H,6-7H2,1H3,(H,12,13)

Upstream product

• 877-95-2 methyl-N-(benzyl-methyl)-formamide 
• 64-04-0 phenethylamine 

Downstream Products

• 112557-13-8 4-(β-Acetamidoethyl)benzene-N-<4-phenylenesulfamido-5-(2-ethyl-1,3,4-thiadiazolyl)>sulfonamide 
• 374632-73-2 4-[2-(acetylamino)ethyl]-N-(2-phenyl-2H-pyrazol-3-yl)benzenesulfonamide 
• 25862-65-1 1-<sulfonyl>-3-cyclohexyl-2-iminoimidazolidine dihydrochloride 
• 41176-98-1 4-(((((4-trans-methylcyclohexylamino)carbonyl)amino)sulfonyl)phenethylamine) 
• 35303-76-5 4-(2-aminoethyl)benzenesulfonamide 

Relevant academic research and scientific papers

Styrene sulfone NLRP3 inflammasome inhibitor, preparation method and application thereof

The invention relates to the field of styrene sulfone compounds and NLRP3 inhibitors, and particularly provides a styrene sulfone NLRP3 inflammasome inhibitor, a preparation method and application thereof, wherein the inhibitor is represented by a formula (1), n is selected from 0 and 1, X is selected from N and O, R1 is selected from different electron withdrawing or electron donating substituents, and R2 is selected from different fat or aromatic substituents. According to the invention, it is verified that the compounds represented by the general formula have NLRP3 inhibitory activity.

N - aryl sulfonamide compound, its pharmaceutical composition and its use (by machine translation)

The invention discloses a category represented by the following general formula I N - aryl sulfonamide compound, to the compound as the active ingredient of the pharmaceutical composition, and their preparation for treating Lp - PLA2 In the diseases related to the activity of the use. (by machine translation)

Preparation method of glimepiride impurity

The invention belongs to the technical field of medicinal chemistry and particularly relates to a preparation method of a glimepiride impurity. The preparation method comprises the following steps: dropwise adding acetic anhydride into a solution of 2-phenethylamine and an organic solvent with a low boiling point to be subjected to reaction to generate N-acetyl phenethylamine; dropwise adding chlorosulfonic acid into the N-acetyl phenethylamine at the temperature of lower than 20 DEG C to be subjected to chlorosulfonation reaction, and performing hydrolysis after the reaction is completed to remove excess chlorosulfonic acid; performing filtration and washing to obtain an impurity J benzenesulfonyl chloride; performing ammonolysis on the impurity J benzenesulfonyl chloride to obtain an impurity J benzene sulfonamide; in acetone, enabling the impurity J benzene sulfonamide to firstly react with a catalyst and then react with trans-p-methylcyclohexyl isocyanate to obtain an impurity J acetyl substance; enabling the impurity J acetyl substance and ethanol to be subjected to alcoholysis under the condition of the catalyst to generate an impurity J and ethyl acetate; and performing refining to obtain a high-purity impurity J. The purity of the glimepiride impurity J prepared by the method is high, the liquid phase content of the glimepiride impurity J is greater than 98.5%, the rawmaterials used in the method are easily available, the process parameters are controllable, and the reaction is mild.

Structure-Guided Discovery of Novel, Potent, and Orally Bioavailable Inhibitors of Lipoprotein-Associated Phospholipase A2

Lipoprotein-associated phospholipase A2 (Lp-PLA2) is a promising therapeutic target for atherosclerosis, Alzheimer's disease, and diabetic macular edema. Here we report the identification of novel sulfonamide scaffold Lp-PLA2 inhibitors derived from a relatively weak fragment. Similarity searching on this fragment followed by molecular docking leads to the discovery of a micromolar inhibitor with a 300-fold potency improvement. Subsequently, by the application of a structure-guided design strategy, a successful hit-to-lead optimization was achieved and a number of Lp-PLA2 inhibitors with single-digit nanomolar potency were obtained. After preliminary evaluation of the properties of drug-likeness in vitro and in vivo, compound 37 stands out from this congeneric series of inhibitors for good inhibitory activity and favorable oral bioavailability in male Sprague-Dawley rats, providing a quality candidate for further development. The present study thus clearly demonstrates the power and advantage of integrally employing fragment screening, crystal structures determination, virtual screening, and medicinal chemistry in an efficient lead discovery project, providing a good example for structure-based drug design.

Product-Derived Bimetallic Palladium Complex Catalyzes Direct Carbonylation of Sulfonylazides

A novel product-derived bimetallic palladium complex catalyzes a sulfonylazide-transfer reaction with the σ-donor/π-acceptor ligand CO, and is advantageous given its broad substrate scope, high efficiency, and mild reaction conditions (atmospheric pressure of CO at room temperature). This methodology provides a new approach to sulfonylureas, which are present in both pharmaceuticals and agrochemicals. The synthesis of Glibenclamide on a gram scale further revealed the practical utility of this procedure. Mechanistically, the generation of a bridged bimetallic palladium species derived from the product sulfonylurea is disclosed as the crucial step for this catalytic cycle.

Synthesis process of glibenclamide intermediate 4-Acetamidobenzenesulfonamide

The invention aims at providing a synthesis process of glibenclamide intermediate 4-Acetamidobenzenesulfonamide. The synthesis process is characterized by comprising the following steps that 1, a crude acetyl phenethylamine acyl compound product is prepared, namely phenethylamine and acetic anhydride perform acylation reaction; 2, acetylamino-benzenesulfonyl chloride is prepared, namely an acetyl phenethylamine acyl compound and chlorosulfonic acid perform chlorosulfonation reaction; 3, the 4-Acetamidobenzenesulfonamide is prepared, namely the acetylamino-benzenesulfonyl chloride and ammonia water perform reaction; The synthesis process has the advantages that by changing the proportion of reactants and reaction conditions, the yield of the glibenclamide intermediate 4-Acetamidobenzenesulfonamide is improved, and further the glyburide yield is improved.

SUBSTITUTED DIAMINOPYRIMIDYL COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH

Provided herein are diaminopyrimidyl Compounds having the following structures: wherein X, L, R1, and R2 are as defined herein, compositions comprising an effective amount of a Diaminopyrimidyl Compound, and methods for treating or preventing PKC-theta-mediated disorders, or a condition treatable or preventable by inhibition of a kinase, for example, PKC-theta.

MTH1 INHIBITORS FOR TREATMENT OF CANCER

A compound of formula I, (I) or a pharmaceutically-acceptable salt thereof. The compound is useful in the treatment of cancer.

MTH1 INHIBITORS FOR TREATMENT OF INFLAMMATORY AND AUTOIMMUNE CONDITIONS

A compound of formula (I), or a pharmaceutically acceptable salt thereof, for use in the treatment of autoimmune diseases and inflammatory conditions.

Synthesis and biological evaluation of sulfonylurea and thiourea derivatives substituted with benzenesulfonamide groups as potential hypoglycemic agents

A novel class of sulfonylurea and thiourea derivatives substituted with benzenesulfonamide groups were designed and synthesized. The target compounds were assayed for the effects on the insulin release of isolated rat pancreatic islets and the glucose transport in adipocytes of rats. Some of them exhibited high potency. Compound 10 also had potent antiplatelet activity and showed an excellent property to protect collagen-epinephrine-induced mice mortality as well as plasma glucose-lowering activity in vivo. The preliminary pharmacological profile of compound 10 showed that it might be useful in the treatment of diabetics with cardiovascular and nephropathy complications.