75907-82-3Relevant articles and documents
Preparation method of vonoprazan fumarate intermediate
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Paragraph 0051-0054, (2021/06/21)
The invention provides a preparation method of a vonoprazan fumarate intermediate, and particularly provides a preparation method of a compound shown as a formula I. The preparation method comprises the following steps: reacting o-fluorobenzonitrile with
Method for synthesizing thiobenzamide derivative through CO2 regulation and control of substituted benzonitrile
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Paragraph 0037; 0038; 0040; 0041; 0042, (2019/01/24)
The invention discloses a method for synthesizing a thiobenzamide derivative through CO2 regulation and control of substituted benzonitrile. The method comprises the following steps: taking the substituted benzonitrile as a raw material, an inorganic sulfide as a sulfur source and CO2 as an auxiliary agent for reacting in the presence of a reaction solvent, and concentrating and purifying a reaction solution to obtain the thiobenzamide derivative. The reaction system disclosed by the invention is relatively simple, other catalysts are not added outside a reactant and the inorganic sulfide, themethod is suitable for synthesis of high-additional-value thiobenzamide containing a plurality of substituent groups, the reaction is carried out at low temperature and low pressure, and the risk coefficient is reduced.
Synthesis, crystal structure, anti-HIV, and antiproliferative activity of new oxadiazole and thiazole analogs
Khan, Mahmood-ul-Hassan,Hameed, Shahid,Akhtar, Tashfeen,Al-Masoudi, Najim A.,Al-Masoudi, Wasfi A.,Jones, Peter G.,Pannecouque, Christophe
, p. 2399 - 2409 (2016/10/25)
A series of 2-adamantyl-5-arylthiazolyl-1,3,4-oxadiazoles 7a–x together with thiazoles 13 and 14 were synthesized. Compounds 7a–l, 13, and 14 were tested in vitro with the aim of identifying novel lead compounds active against human immunodeficiency virus type-1 and human immunodeficiency virus type-2 activity in MT-4 cells. Title compounds were also tested against representatives of Gram-positive and Gram-negative bacteria (Staphylococcus aureus, Salmonella spp.), various mycobacterial strains (Mycobacterium fortuitum and Mycobacterium smegmatis), yeast (Candida albicans), and mold (Aspergillus fumigatus). None of the compounds showed antiviral or antimicrobial activity, except compounds 13 and 14 exhibited anti-human immunodeficiency virus-1 activity with EC50 values of 1.79 and 2.39 μM with Selectivity index = 18 and 4, respectively. On the other hand, compounds 7a and 7j showed a marked cytotoxicity against the human CD4+ lymphocytes (MT-4). Therefore, 7a and 7j were evaluated for their antiproliferative activity against two solid tumor-derived cell lines, which exhibited IC50 values of 8.1 ± 0.10 μM and 4.8 ± 0.08 μM against Hep-G2 cell lines, respectively.
