124750-51-2Relevant articles and documents
Method for tubular reaction preparation of substituted benzylically brominated methyl biphenyl and reaction device of method
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Paragraph 0022-0029, (2018/06/15)
The invention discloses a method for tubular reaction preparation of substituted benzylically brominated methyl biphenyl and a reaction device of the method. According to the method, substituted methyl biphenyl is taken as a raw material and bromine is taken as a bromination reagent. The reaction materials are continuously fed into a high-efficiency mixer for mixing through a liquid conveying pump, and the formed mixture enters a reactor in a water bath for a reaction, after the reaction is finished, the reaction system enters a receiving tank, a reducing agent is added to the receiving tank for quenching, liquid separation is carried out, anhydrous sodium sulfate is added into the organic phase, suction filtration is performed, the organic phase is subjected to reduced-pressure concentration for solvent removal, a solvent is added for recrystallization, suction filtration is performed, and the filter cake is dried to obtain a pure product namely the substituted benzylically brominatedmethyl biphenyl. The method of the invention is simple and convenient to control, high in safety, less in generation of by-products and convenient for post-processing, a small trial process can be directly used for amplified production. The method meets the requirements of green chemistry and has a certain industrial application value.
Bacterial Peptide Deformylase Inhibition of Tetrazole-Substituted Biaryl Acid Analogs: Synthesis, Biological Evaluations, and Molecular Docking Study
Khan, Firoz A. Kalam,Patil, Rajendra H.,Patil, Manjiri,Arote, Rohidas,Shinde, Devanand B.,Sangshetti, Jaiprakash N.
, p. 934 - 943 (2016/12/09)
The synthesis and screening of tetrazole-substituted biaryl acid analogs 7a–l as bacterial peptide deformylase (PDF) enzyme inhibitors is reported. The compounds 7e (IC50 value = 5.50 μM) and 7g (IC50 value = 7.25 μM) showed good PDF inhibition activity. The compounds 7e (MIC range = 10.75–11.66 μg/mL) and 7g (MIC range = 8.91–12.83 μg/mL) also showed potent antibacterial activity when compared with the standard ciprofloxacin (MIC range = 25–50 μg/mL). Thus, the active derivatives were not only potent PDF enzyme inhibitors but also efficient antibacterial agents. In order to gain more insight into the binding mode of the compounds with the PDF enzyme, the most active compounds 7e and 7g, the moderately active compound 7k, and the least active compound 7h were docked against the PDF enzyme of Escherichia coli. The docking study of the most active compounds 7e and 7g against the PDF enzyme exhibited good binding properties. Hence, we believe our synthesized compounds 7a–l could serve as reservoir for bacterial PDF inhibitor development.
A process for the preparation of olmesartan
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, (2017/04/19)
The invention discloses a preparation method of Olmesartan Medoxomil. The method is used for synthesizing an important intermediate 4-[2-(2-triphenylmethyl tetrazole-5-yl) phenyl] benzyl bromide (a compound III) so as to prepare the compound Olmesartan Medoxomil. The method is high in yield, easy to separate and purify, simple to operate and suitable for industrial production.