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Chemical Research Letters, May 2021. Catalysts allow a reaction to proceed via a pathway that has a lower activation energy than the uncatalyzed reaction.Quality Control of Methyl benzo[b]thiophene-2-carboxylate, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 22913-24-2, Name is Methyl benzo[b]thiophene-2-carboxylate, molecular formula is C10H8O2S

FLT3 mutation is among the most common genetic mutations in acute myeloid leukemia (AML), which is also related with poor overall survival and refractory in AML patients. Recently, FLT3 inhibitors have been approved for AML therapy. Herein, a series of new compounds with pyrazole amine scaffold was discovered, which showed potent inhibitory activity against FLT3-ITD and significant selectivity against both FLT3-ITD and AML cells expressing FLT3-ITD. Compound 46, possessing the most promising cellular activity, blocked the autophosphorylation of FLT3 pathway in MV4-11 cell line. Furthermore, the apoptosis and downregulation of P-STAT5 were also observed in tumor cells extracted from the MV4-11 cell xenografts model upon compound 46 treatment. Compound 46 was also metabolically stable in vitro and suppressed tumor growth significantly in MV4-11 xenografts model in vivo. Compound 46 showed no toxicity to the viscera of mice and caused no decrease in body weight of mice. In conclusion, the results of this study could provide valuable insights into discovery of new FLT3 inhibitors, and compound 46 was worthy of further development as potential drug candidate to treat AML.

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The present invention provides novel imidazolyl-benzothiophenes and derivatives thereof which are useful as thromboxane A2 (TXA2) synthetase inhibitors and as such represent potent pharmacological agents.

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Sun lamp illuminated alkoxycarbonylation of aryl, heteroaryl, and vinyl halides was performed under atmospheric pressure of CO in the presence of a cobalt catalyst in situ generated from Co(OAc)2.Illunination through a Pyrex flask was sufficient to catalyze the reaction.This process avoids the use of Co2(CO)8 and excess CH3I, which were required in the earlier procedure.A SRN1 mechanism is proposed.

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A series of 4-substituted (benzo[b]thiophene-2-carbonyl)guanidines was synthesized and evaluated for the NHE-1 inhibitory activity and cardioprotective efficacy both in vitro and in vivo. Several analogs exhibited a strong inhibition on NHE-1, and which was generally well correlated with their cardioprotective efficacy. Especially the 4-nitro 20 and cyano 50 compounds excellently improved the cardiac function and reduced infarct size against ischemia/reperfusion injury.

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Organic thioether compounds had found extensive applications in the field of medicine, biology, agriculture, optical material and so on. The protocols synthesizing thioethers have always been an attractive interest to researchers. So far, various preparation methods involving diverse catalysts and promote reagents have been reported. A wide scope of newly published vital articles referring reactions of organic halides, alkenes, arenes, heteroaromatics and organic borides with sulfur source thiols, thiophenols, thioamides, potassium xanthate, potassium thiocyanate, elemental sulfur, sodium thiomethoxide, sodium sulfide, carbon disulphide, disulfides, sulfonyl hydrazides, AgSCF3, CuSCF3 with transition metal complexes catalyzation or with metal free method are comprehensively summarized in this review.

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A general method for the synthesis of structurally diverse N-arylpyrazoles from readily available cyclopropanols and aryldiazonium salts is disclosed. The reaction was conducted at room temperature within minutes with a broad substrate scope and excellent regioselectivity.

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The invention relates to ruthenium catalytic ester derivative selective dehydrogenation boron reaction new method, including falling to six coordination of borneol diene (NBD) ligand of ruthenium complex as catalyst, in order to methyl ester derivatives and joint frequency which mellow boron ester is the reaction substrate, the reaction under mild conditions, the high-efficient catalytic ester derivative in an oxygen atom ortho-methyl-hydrogen bond selectively generating boron reaction, to obtain the corresponding methyl ester borate product. At present, in the ester derivatives on the oxygen atom ortho-methyl hydrogen bond of boron selective dehydrogenation reaction has not yet been reported. The invention realized for the first time the occurrence of the oxygen atom of the ester derivative selective ortho-methyl of the dehydrogenation boron reaction, as the organic ester borate such organic synthetic intermediates preparation provides a new response strategies. (by machine translation)

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An SeO2-mediated one-pot method was established for the synthesis of 3-cyanofurans from 3-oxo-3-arylpropanenitriles and substituted acetaldehydes. The generality of the reaction was explored, and a plausible mechanism is proposed.

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A Ni-catalyzed decarbonylative methylation of aromatic esters was achieved using methylaluminums as methylating agents. Dimethylaluminum chlorides uniquely worked as the methyl source. Because of the Lewis acidity of aluminum reagents, less reactive alkyl esters could also undergo the present methylation. By controlling the Lewis acidity of aluminum reagents, a chemoselective decarbonylative cross-coupling between alkyl esters and phenyl esters was successful.

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A facile and selective palladium-catalyzed domino procedure has been developed for the preparation of 2-carbonylbenzo[b]thiophene derivatives from 2-gem-dihalovinylthiophenols. This protocol involves intramolecular C-S coupling/intermolecular carbonylation cascade sequences and allows access to various highly functionalized benzo[b]thiophenes in moderate yields.

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