1023-67-2Relevant articles and documents
Borane-Catalyzed Chemoselective and Enantioselective Reduction of 2-Vinyl-Substituted Pyridines
Hu, Chen-Yu,Li, Xiang,Liang, Xin-Shen,Liu, Ning,Tian, Jun-Jie,Tu, Xian-Shuang,Wang, Xiao-Chen,Yang, Zhao-Ying
supporting information, p. 18452 - 18456 (2020/08/21)
Herein, we report that highly chemoselective and enantioselective reduction of 2-vinyl-substituted pyridines has been achieved for the first time. The reaction, which uses chiral spiro-bicyclic bisboranes as catalysts and HBpin and an acidic amide as reducing reagents, proceeds through a cascade process involving 1,4-hydroboration followed by transfer hydrogenation of a dihydropyridine intermediate. The retained double bond in the reduction products permits their conversion to natural products and other useful heterocyclic compounds by simple transformations.
2, 4-substituted pyrimidine derivative, preparation method thereof and application thereof in preparation of antitumor drugs
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Paragraph 0018-0021, (2020/04/22)
The invention belongs to the field of medical compounds, and particularly relates to a 2, 4-substituted pyrimidine derivative, a preparation method thereof and an application thereof in the preparation of antitumor drugs. The derivative has a structure sh
Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus
Kyei-Baffour, Kwaku,Mohammad, Haroon,Seleem, Mohamed N.,Dai, Mingji
supporting information, p. 1845 - 1854 (2019/03/28)
Antibiotic resistance remains a major global public health threat that requires sustained discovery of novel antibacterial agents with unexploited scaffolds. Structure-activity relationship of the first-generation aryl isonitrile compounds we synthesized led to an initial lead molecule that informed the synthesis of a second-generation of aryl isonitriles. From this new series of 20 compounds, three analogues inhibited growth of methicillin-resistant Staphylococcus aureus (MRSA) (from 1 to 4 μM) and were safe to human keratinocytes. Compound 19, with an additional isonitrile group exhibited improved activity against MRSA compared to the first-generation lead compound. This compound emerged as a candidate worthy of further investigation and further reinforced the importance of the isonitrile functionality in the compounds’ anti-MRSA activity. In a murine skin wound model, 19 significantly reduced the burden of MRSA, similar to the antibiotic fusidic acid. In summary, 19 was identified as a new lead aryl isonitrile compound effective against MRSA.
