- Method for synthesizing 2-acetyl-4-chlorothiophene
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The invention provides a method for synthesizing 2-acetyl-4-chlorothiophene, which comprises the following steps: dissolving 2-acetylthiophene in a solvent, adding a chlorinating agent and a Lewis acid, and reacting to obtain the 2-acetyl-4-chlorothiophene, wherein the chlorinating agent is N-chlorosuccinimide. The method is simple to operate, the synthesized 2-acetyl-4-chlorothiophene is high inyield and purity which can reach 99.66%, the raw material conversion rate is high, and few byproducts are produced. Meanwhile, the solid N-chlorosuccinimide is used as the chlorinating agent in the synthesis process of the method, and the chlorinating agent is low in cost, environmentally friendly, convenient to use and easy to control in dosage. Therefore, the method for synthesizing the 2-acetyl-4-chlorothiophene also has the advantages of low cost and environmental friendliness, is suitable for industrial large-scale production, and has a good market prospect.
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Paragraph 0008; 0027-0032
(2020/05/14)
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- Synthesis method of 4-chlorothiophene-2-carbonyl derivative
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The invention discloses a synthesis method of a 4-chlorothiophene-2-carbonyl derivative. A thiophene-2-carbonyl derivative is used as a raw material and reacts with symclosene and aluminum trichloride, and liquid separation and concentration are performed to obtain the 4-chlorothiophene-2-carbonyl derivative. The synthesis method adopts one-step reaction, the yield is not lower than 80%, the production process is decreased while the yield is improved, and the cost is reduced; the used raw materials and reagents are easy to obtain, reaction conditions are mild, post-treatment and purification is easy to operate, and large-scale production can be achieved.
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Paragraph 0035-0037
(2019/03/08)
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- Combining structure- and property-based optimization to identify selective FLT3-ITD inhibitors with good antitumor efficacy in AML cell inoculated mouse xenograft model
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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.
- Heng, Hao,Wang, Zhijie,Li, Hongmei,Huang, Yatian,Lan, Qingyuan,Guo, Xiaoxing,Zhang, Liang,Zhi, Yanle,Cai, Jiongheng,Qin, Tianren,Xiang, Li,Wang, Shuxian,Chen, Yadong,Lu, Tao,Lu, Shuai
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p. 248 - 267
(2019/05/21)
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- Pyrrole inhibitors of S-nitrosoglutathione reductase as therapeutic agents
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The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
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Page/Page column 304-305
(2015/11/16)
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- INHIBITORS OF Akt ACTIVITY
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Invented are novel thiophene compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
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Page/Page column 141
(2010/11/27)
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- Herbicidal Thienylureas, I
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Syntheses of the title substances as potential herbicides are described by a modified Curtius degradation of corresponding thiophene carboxylic acids, obtained in turn by haloform reaction of appropriate acetyl thiophenes.Regioselective substitution reactions of thiophenes were key steps for the construction of desired substitution patterns.Structure-activity considerations show that especially the 3-thienyl ureas 36 and 38 exhibit significant herbicidal activity comparable with commercial products. - Keywords: Curtius degradation; Herbicides; Thiophenes; Ureas; Urethanes
- Stanetty, Peter,Puschautz, Erhard,Friedbacher, Gernot
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