19798-80-2Relevant articles and documents
Synthesis and biological evaluation of novel 4-(2-fluorophenoxy)-2-(1h- tetrazol-1-yl)pyridines bearing semicarbazone moieties as potent antitumor agents
Qin, Mingze,Liao, Weike,Xu, Chen,Fu, Baolin,Ren, Jianguo,Gu, Yucheng,Gong, Ping
, p. 840 - 850 (2013)
A series of 4-(2-fluorophenoxy)-2-(1H-tetrazol-1-yl)pyridines bearing semicarbazone moieties were synthesized and evaluated for their in vitro antitumor potency. Some of the compounds (10b, 10c, 10e-10h, 10m-10p, 10r, and 11b) exhibited moderate to excellent antitumor activity as compared to sorafenib and PAC-1, as well as low levels of toxicity toward the human fetal lung fibroblast cell line WI-38. The most promising compound 10p (IC50 = 0.08, 0.36, 0.97 μM) was 45.1-, 6.1-, and 2.4-fold more active than sorafenib (IC50 = 3.61, 2.19, 2.32 μM), and 17, 3.2, and 2.9 times better than PAC-1 (IC50 = 1.36, 1.17, 2.83 μM) against three cancer cell lines (HT-29, H460, and MKN-45), respectively. In addition, further studies examining enzymatic activity suggested that the marked pharmacological activity observed might be ascribed to an inhibitory action against CRAf kinase. A series of 4-(2-fluorophenoxy)-2-(1H-tetrazol-1-yl)pyridines bearing semicarbazone moieties were synthesized and evaluated for their cytotoxic activities in vitro. The most promising compound 10p was further examined for enzymatic activity, with the goal to investigate the molecular mechanisms of action.
Synthesis method of imidazopyridine or pyrimidine derivative
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Paragraph 0034-0036, (2021/05/29)
The invention belongs to the technical field of synthesis, and particularly relates to a synthesis method of an imidazopyridine or pyrimidine derivative. The imidazopyridine or pyrimidine compound is obtained by taking pyridine or pyrimidinecarboxylic acid as a synthon through amidation, Hofmann degradation and cyclization reaction, and the obtained imidazopyridine or pyrimidine derivative can be further converted to generate a functional product. The method has the advantages of easily available raw materials, simple operation, high reaction efficiency, convenient post-treatment, and diversity of functional groups.
Preparation method of 2-amino-4-fluoropyridine
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Paragraph 0008; 0020; 0022; 0024; 0026; 0028; 0030, (2018/09/12)
The invention discloses a preparation method of 2-amino-4-fluoropyridine, comprising the synthetic steps of 1, subjecting 2-pyridinecarboxylic acid as a raw material to reaction in the presence of thionyl chloride and a salt to obtain 4-chloropyridine-2-acyl chloride, and subjecting 4-chloropyridine-2-acyl chloride the presence of ammonia to obtain 4-chloropyridine-2-amide; 2, subjecting 4-chloropyridine-2-amide to Hofmann rearrangement reaction to obtain 2-amino-4-chloropyridine; 3, subjecting 2-amino-4-chloropyridine to halogen exchange to obtain 2-amino-4-fluoropyridine. The problems of theexisting preparation method, such as long synthetic path, operational complexity, high pollution of three wastes, poor atomic economy, low yield and high manufacture cost, are solved.
ANTIVIRAL DRUGS FOR TREATMENT OF ARENA VIRUS INFECTION
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Paragraph 0000228, (2013/08/28)
Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever