- Borane-Catalyzed Chemoselective and Enantioselective Reduction of 2-Vinyl-Substituted Pyridines
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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.
- Hu, Chen-Yu,Li, Xiang,Liang, Xin-Shen,Liu, Ning,Tian, Jun-Jie,Tu, Xian-Shuang,Wang, Xiao-Chen,Yang, Zhao-Ying
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supporting information
p. 18452 - 18456
(2020/08/21)
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- Iron complex containing diphosphine meta-position carborane ligand as well as preparation method and application of same
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The invention relates to an iron complex containing a diphosphine meta-position carborane ligand as well as a preparation method and application of the same. The iron complex is prepared by the following method: reacting n-BuLi with m-carborane m-C2B10H12, then adding halogenated phosphine for continuous reaction, then adding FeCl2 into a reaction system for continuous reaction, after the reactionis finished, separating the reaction product to obtain an iron complex containing a diphosphine m-carborane ligand, and applying the iron complex to catalytic synthesis of a trans-2-alkenyl azaarenecompound. Compared with the prior art, the method shows efficient catalytic activity in synthesis of the trans-2-alkenyl aza-aromatic hydrocarbon compound through direct condensation reaction of 2-methyl aza-aromatic hydrocarbon and aromatic aldehyde, is low in catalyst dosage, mild in reaction condition, high in reaction rate and relatively high in yield, and has a wide application prospect in industry.
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Paragraph 0032; 0036-0037; 0040
(2020/10/14)
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- 2, 4-substituted pyrimidine derivative, preparation method thereof and application thereof in preparation of antitumor drugs
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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
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Paragraph 0018-0021
(2020/04/22)
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- [2+2] Photodimerization of Stilbazoles Promoted by Oxalic Acid in Suspension
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In this study, a very simple technique to perform efficiently photodimerization of some vinylpyridines is reported. By irradiating a stirred mixture of several stilbazoles with solid oxalic acid dihydrate dispersed in a nonpolar (i.e., cyclohexane) or moderately polar (benzene, dichloromethane, dioxane) solvent, the corresponding dimeric cyclobutane adducts were obtained in high yields and excellent regio- and stereoselectivities. The strategy could also be applied successfully to oily, waxy, or even insoluble stilbazoles. Moreover, the oxalic acid loading could be lowered to substoichiometric amounts. When further optimizations were needed, our strategy was found to be highly flexible to identify other oligocarboxylic acids as alternative additives to improve, or even overturn, the regioselectivity. Oxalic acid and other oligocarboxylic acids were found to be capable of orienting more than 50 stilbazoles toward photodimerization under these conditions.
- Nguyen, Thanh Binh,Nguyen, Tuan Minh,Retailleau, Pascal
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supporting information
p. 4682 - 4689
(2020/04/15)
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- Styryl pyridine compound containing pyridine structure, preparation method and application of styryl pyridine compound in preparation of antitumor drugs (by machine translation)
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The invention belongs to the field, and particularly relates to a styryl pyridine compound containing a pyridine structure, a preparation method and an application of the styryl pyridine compound in preparation of anti-tumor drugs, wherein the compound is a compound as shown in the formula I. The compound of the general formula I has good inhibitory activity on non-small cell lung cancer A549 and liver cancer cell HepepepG2, can be used for preparing antitumor drugs, and is especially suitable for cancers, kidney cancer, lung cancer, thyroid cancer, colon cancer and other tumors. (by machine translation)
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Paragraph 0021-0024
(2019/09/05)
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- Second-generation aryl isonitrile compounds targeting multidrug-resistant Staphylococcus aureus
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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.
- Kyei-Baffour, Kwaku,Mohammad, Haroon,Seleem, Mohamed N.,Dai, Mingji
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supporting information
p. 1845 - 1854
(2019/03/28)
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- CHARACTERISTIC FEATURES OF THE CONDENSATION OF PICOLINE BORON TRIFLUORIDE COMPLEXES WITH AROMATIC ALDEHYDES
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The formation of complexes 2- and 4-picolines with BF3 results in a significant activation of their methyl groups.This makes it possible to carry out condensations with aromatic aldehydes under mild conditions.The reaction of 2-picoline with 4-(dimethylamino)benzaldehyde in acetic anhydride solution results in the splitting of the pyridine ring with formation of an unstable product.
- Vasil'ev, A. N.,Mushkalo, L. K.
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p. 1718 - 1720
(2007/10/02)
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