- Visible-Light-Induced Radical Difluoromethylation/Cyclization of Unactivated Alkenes: Access to CF2H-Substituted Quinazolinones
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A mild and efficient visible-light-induced radical difluoromethylation/cyclization of unactivated alkenes toward the synthesis of substituted quinazolinones with easily accessible difluoromethyltriphenylphosphonium bromide has been developed. The transformation has the advantages of wide functional group compatibility, a broad substrate scope, and operational simplicity. The benign protocol offers a facile access to pharmaceutically valuable difluoromethylated polycyclic quinazolinones.
- Chen, Xiaoyu,Liu, Bo,Pei, Congcong,Li, Jingya,Zou, Dapeng,Wu, Yangjie,Wu, Yusheng
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supporting information
p. 7787 - 7791
(2021/10/20)
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- Pyrimidine hydrazone derivative and preparation method and application thereof
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The invention relates to pyrimidine hydrazone derivatives as shown in a chemical structural formula I or II, pharmaceutically acceptable salts and pharmaceutical compositions thereof, and an application of the pyrimidine hydrazone derivatives and the pharmaceutically acceptable salts and the pharmaceutical compositions in preparation of influenza virus neuraminidase inhibitors, wherein X is selected from: fluorine, chlorine, bromine, hydroxyl, dihydroxy, 2-hydroxy-3-methoxy, 2-hydroxy-4-methoxy, 2-hydroxy-5-C1-C2 alkoxy, 2-hydroxy-6-C1-C2 alkoxy, 3-hydroxy-2-C1-C2 alkoxy, 3-hydroxy-4-C1-C2 alkoxy, 3-hydroxy-5-methyl C1-C2 alkoxy , 3-hydroxy-6-C1-C2 alkoxy, 4-hydroxy-2-C1-C2 alkoxy, 4-hydroxy-3-C1-C2 alkoxy, 4-hydroxy-3, 5-diC1-C2 alkoxy, trihydroxy or 4-hydroxy-3,5-dimethyl; and Y is selected from: fluorine, chlorine, bromine, acetamido, hydroxyl or methoxy.
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Paragraph 0116-0120
(2020/11/23)
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- FXIa blood coagulation factor inhibitor as well as pharmaceutical composition and application thereof
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The invention relates to an FXIa blood coagulation factor inhibitor as well as a pharmaceutical composition and application thereof. Specifically, the invention discloses a compound shown as a formulaI or a pharmaceutically acceptable salt thereof. The invention also discloses a pharmaceutical composition containing the compound as shown in the formula I or pharmaceutically acceptable salt thereof, and application of the compound as shown in the formula I or pharmaceutically acceptable salt thereof. The compound disclosed by the invention is novel in structure and has good inhibitory activityon FXIa. .
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Paragraph 0206-0210
(2020/12/30)
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- BIARYL KINASE INHIBITORS
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The present disclosure is directed to biaryl compounds of formula (I) which can inhibit AAKl (adaptor associated kinase 1), compositions comprising such compounds and their use for treating e.g. pain, Alzheimer's disease, Parkinson's disease and schizophrenia.
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Page/Page column 288; 289
(2017/07/31)
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- Design, synthesis, and antifungal activities of new β-methoxyacrylate analogues
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Strobilurins have become one of the most important classes of agricultural fungicides. To search for new strobilurin derivatives with high activity against resistant pathogens, a series of new β-methoxyacrylate analogues containing substituted pyrimidine in the side chain with strobilurin pharmacophore were synthesized and their biological activities were tested. The compounds were confirmed and characterized by 1H-NMR, elemental analysis and mass spectroscopy. The bioassays indicated that most of the compounds 1 exhibited potent antifungal activities against Colletotrichum orbiculare, Botrytis cinerea Pers and Phytophthora capsici Leonian at a concentration of 50 μg mL-1. Notably, compound 1b (R = 2,5-dimethylphenyl) showed better antifungal activity against all the tested fungi than the commercial strobilurin fungicide azoxystrobin.
- Liu, Hui-Jun,Zhang, Xiang,Gao, Yong-Xin,Li, Jian-Zhong,Wang, Hui-Li
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- INHIBITORS OF STEAROYL-COA DESATURASE
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Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity.
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- PYRIMIDINE DERIVATIVES AND HERBICIDES CONTAINING THE SAME
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The present invention provides a pyrimidine derivative represented by the formula: wherein R1p and R1q are the same or different, and each represents (1)hydrogen, (2)halogen, (3) a C1-6alkyl group which may be substituted or (4) a C1-6alkoxy group, and so on, R2 is halogen, a C1-6alkyl group, cyano group, and so on, Ar is a phenyl group which may be substituted or is a condensed hetero ring which may be substituted, which has excellent selective herbicidal activity, and a herbicide containing the derivative.
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