895-45-4Relevant academic research and scientific papers
Preparation method of 2-(p-trifluoromethyl thiophenyl)benzoate
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Paragraph 0015; 0016; 0017; 0018; 0019; 0020; 0021, (2017/09/29)
The invention provides a preparation method of 2-(p-trifluoromethyl thiophenyl)benzoate. The 2-(p-trifluoromethyl thiophenyl)benzoate is obtained by reacting thiosalicylic acid serving as a starting raw material with p-trifluoromethyl chlorobenzene. Compared with the prior art, the preparation method mainly has the advantages: (1) an organic solvent obtained by post-treatment can be recycled, so that the emission of waste water, waste gas and waste solid is reduced, and the production cost is lowered; (2) a water phase obtained by post-treatment can also be recycled, and sodium chloride in the water phase can be recycled after repeated use, so that wastewater is recycled, water resources are saved, and the atom economy is increased; (3) the 2-(p-trifluoromethyl thiophenyl)benzoate content of a synthesized flupentixol intermediate can be 90 percent or more, the highest content can be up to 93 percent, and the content of the 2-(p-trifluoromethyl thiophenyl)benzoate obtained by an original process method is only about 85 percent. The whole process meets the technical requirements of environment-friendly synthesis and clean production, and is suitable for large-scale industrial production.
Novel dengue virus NS2B/NS3 protease inhibitors
Wu, Hongmei,Bock, Stefanie,Snitko, Mariya,Berger, Thilo,Weidner, Thomas,Holloway, Steven,Kanitz, Manuel,Diederich, Wibke E.,Steuber, Holger,Walter, Christof,Hofmann, Daniela,Wei?brich, Benedikt,Spannaus, Ralf,Acosta, Eliana G.,Bartenschlager, Ralf,Engels, Bernd,Schirmeister, Tanja,Bodem, Jochen
supporting information, p. 1100 - 1109 (2015/03/05)
Dengue fever is a severe, widespread, and neglected disease with more than 2 million diagnosed infections per year. The dengue virus NS2B/NS3 protease (PR) represents a prime target for rational drug design. At the moment, there are no clinical PR inhibitors (PIs) available. We have identified diaryl (thio)ethers as candidates for a novel class of PIs. Here, we report the selective and noncompetitive inhibition of the serotype 2 and 3 dengue virus PR in vitro and in cells by benzothiazole derivatives exhibiting 50% inhibitory concentrations (IC50s) in the low-micromolar range. Inhibition of replication of DENV serotypes 1 to 3 was specific, since all substances influenced neither hepatitis C virus (HCV) nor HIV-1 replication. Molecular docking suggests binding at a specific allosteric binding site. In addition to the in vitro assays, a cell-based PR assay was developed to test these substances in a replication-independent way. The new compounds inhibited the DENV PR with IC50s in the low-micromolar or submicromolar range in cells. Furthermore, these novel PIs inhibit viral replication at submicromolar concentrations.
