Discovery of 4-[2-[(3-Ethyl-4-methyl-2-oxo-3-pyrrolin-1-yl)carboxamido]ethyl]benzenesulfonamide

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Preparation method of glimepiride intermediate (by machine translation)

The invention relates to a preparation method, namely a glimepiride intermediate compound I. Belong to bulk drug preparation technical field. The preparation method comprises the following steps: reacting a compound II with diphenyl carbonate under the catalysis of a base (cf. Synletlett, 28 (18), 2495 – 2498 2017; adatdatdatas) preparing the compound IX; adding a weak 4 – acid 2 – adding isopropanol, and heating 1:1 the reflux reaction. atimetimea feeding, adding of the weak acid and heating reflux reaction . the compound IX is prepared from the following steps. The invention provides a preparation method of a high-purity glimepiride intermediate. (by machine translation)

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Brief introduction of Methyl 10-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)-9-methoxy-3-oxo-3H-benzo[f]chromene-2-carboxylate

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Novel optimization of valmerins (tetrahydropyrido[1,2- a ]isoindolones) as potent dual CDK5/GSK3 inhibitors

An efficient synthetic strategy able to modulate the structure of the tetrahydropyridine isoindolone (Valmerin) skeleton was developed. A library of more than 30 novel final structures was generated. Biological activities on CDK5 and GSK3 as well as cellular effects on cancer cell lines were measured for each novel compound. Additionally to support the SAR, a docking study was performed. A potent GSK3/CDK5 dual inhibitor (37, IC50 CDK5/GSK3 35/7 nM) was obtained. Best antiproliferative effects were obtained on lung and prostate cell lines with IC50 Combining double low line 20 nM.

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Some scientific research about 4-[2-[(3-Ethyl-4-methyl-2-oxo-3-pyrrolin-1-yl)carboxamido]ethyl]benzenesulfonamide

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Method for promoting insulin secretion drug glimepiride intermediate preparation method (by machine translation)

The invention discloses a method for promoting insulin secretion drug glimepiride intermediate preparation method, the promoting insulin secretion drug glimepiride intermediate chemical name 2 – (3 – ethyl – 4 – methyl – 2 – oxo – 3 – pyrroline – 1 – carboxamido) ethyl benzene sulfonamide; the invention is directed to glimepiride midbody preparation, the preparation process is simple, short synthetic route, improves manufacturing efficiency, beneficial to the post to the glimepiride preparation, it is easy to realize the industrialized, reduces the production cost, is suitable for mass production, the search for new glimepiride preparation method of the midbody for glimepiride economic and technical is very meaningful. (by machine translation)

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Properties and Exciting Facts About Methyl 10-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)-9-methoxy-3-oxo-3H-benzo[f]chromene-2-carboxylate

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CINNAMOYL COMPOUND AND USE OF THE SAME

The present invention relates to a cinnamoyl compound represented by the formula (I):

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An Efficient and Practical Process for the Synthesis of Glimepiride

A novel and simple approach to the synthesis of glimepiride is reported. It involves the preparation of a carbamate of 3-ethyl-4-methyl-1 H -pyrrol-2(5 H)-one, followed by its reaction with 4-(2-aminoethyl)benzenesulfonamide to produce the intermediate sulfonamide. This sulfonamide, upon reaction with phenyl (trans -4-methylcyclohexyl)carbamate, gave glimepiride. This process avoids the use of phosgene, isocyanates, or chloroformates. Furthermore, sulfonation of the aryl group was eliminated, rendering the product free of the impurities reported in earlier processes.

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Properties and Exciting Facts About 4-[2-[(3-Ethyl-4-methyl-2-oxo-3-pyrrolin-1-yl)carboxamido]ethyl]benzenesulfonamide

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A preparation method of glimepiride (by machine translation)

The invention discloses a method for preparing for glimepiride, which belongs to the technical field of the synthesized compounds. The invention through N, N’ – carbonyl imidazole as the condensing agent, in order to compound I: N – 4 – [2 – (3 – ethyl – 4 – methyl – 2 – oxo – 3 – pyrroline – 1 – carboxamido) ethyl] – benzene sulfonamide and compound II: trans 4 – methyl cyclohexyl amine as the starting material, by condensation reaction, through simple purification processing, can get the glimepiride. Compared with the existing method, the method avoids the use of toxic of the triphosgene or phosgene, while avoiding preparation isocyanate or carbamate intermediate of the increase of the process route, the method has simple technique, the procedure is short, simple operation and the like. (by machine translation)

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2 – SUBSTITUTED HETEROCYCLIC COMPOUNDS AND ANTITUMOR COMPOSITION COMPRISING THE SAME

The present invention relates with 2-substituted heterocyclic compounds and antitumor composition comprising the same. The compound according to the present invention exhibits superior effect as telomerase inhibitor based on new mechanism (terlomere-terlomerase) which can resolve the problems occurring at the time of using chemotherapeutics, i.e side effects and cross resistance between related mechanism on using chemotherapeutics. In addition, the antitumor composition comprising the compound of the present invention exhibits superior effect in inhibiting the growth of cancer cell.

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Top Picks: new discover of 4-[2-[(3-Ethyl-4-methyl-2-oxo-3-pyrrolin-1-yl)carboxamido]ethyl]benzenesulfonamide

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A NOVEL PROCESS FOR PREPARATION OF SUBSTANTIALLY PURE GLIMEPIRIDE

The present invention discloses a novel process for purification of trans-4-methyl cyclohexylamine HC1 and 4-[2-(3-Ethyl-4-methyl-2-carbonyl pyrrolidine amido) ethyl] benzene sulfonamide used in the synthesis of 3-Ethyl-2,5-dihydro-4-methyl-N-[2-[4-[[[[(trans-4-methyl cyclohexyl)amino]carbonyl]amino]sulfonyl]phenyl]ethyl]-2-oxo-1H-pyrrole-1-carboxamide(I), popularly known as Glimepiride. The present invention also discloses a novel purification of Glimepiride Form I (I), having the undesired cis isomer below 0.15%. Glimepiride (I) is useful in the treatment of diabetes mellitus.

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Sulfonylureas as Concomitant Insulin Secretagogues and NLRP3 Inflammasome Inhibitors

Insulin-secretory sulfonylureas are widely used, cost-effective treatments for type 2 diabetes (T2D). However, pancreatic beta-cells are continually depleted as T2D progresses, thereby rendering the sulfonylurea drug class ineffective in controlling glycaemia. Dysregulation of the innate immune system via activation of the NLRP3 inflammasome, and the consequent production of interleukin-1beta, has been linked to pancreatic beta-cell death and multiple inflammatory complications of T2D disease. One proposed strategy for treating T2D is the use of sulfonylurea insulin secretagogues that are also NLRP3 inhibitors. We report the synthesis and biological evaluation of nine sulfonylureas that inhibit NLRP3 activation in murine bone-marrow- derived macrophages in a potent, dose-dependent manner. Six of these compounds inhibited NLRP3 at nanomolar concentrations and can also stimulate insulin secretion from a murine pancreatic cell line (MIN6). These novel compounds possess unprecedented dual modes of action, paving the way for a new generation of sulfonylureas that may be useful as therapeutic candidates and/or tool compounds in T2D and its associated inflammatory complications.

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Total synthesis of cis and trans-hydroxyglimepiride: Active metabolite of glimepiride

Syntheses of trans-hydroxyglimepiride 2b, a human metabolite of the blood glucose lowering agent glimepiride 1 and its corresponding cis-stereoisomer 2a, are described.

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