- High Chemo-/Stereoselectivity for Synthesis of Polysubstituted Monofluorinated Pyrimidyl Enol Ether Derivatives
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A novel intramolecular Smiles rearrangement of α-fluoro-β-keto-pyrimidylsulfones (usually used as a carbon nucleophile) was developed, providing a versatile avenue for synthesis of tri/tetra-substituted monofluorinated pyrimidyl enol ethers. Among these, diverse (Z)-monofluorovinylsulfones and sulfinates were efficiently assembled by adding extra electrophile and fine-tuning reaction conditions. The process is triggered by a keto-enol tautomerism from enol oxyanion to pyrimidine 2-carbon, completely different from the classical carbon nucleophilic addition reaction approach.
- Kang, Lei,Wang, Fang,Zhang, Jinlong,Yang, Huameng,Xia, Chungu,Qian, Jinlong,Jiang, Gaoxi
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supporting information
p. 1669 - 1674
(2021/03/08)
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- Propiconazole hapten as well as preparation method and application thereof
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The invention discloses a propiconazole hapten as well as a preparation method and application thereof. According to the propiconazole hapten, a de novo synthesis method is adopted, a connecting arm containing four C atoms is connected to a benzene ring of propiconazole, and a carboxyl group capable of being coupled with carrier protein is introduced to the tail end of the connecting arm. The monoclonal antibody prepared by using the hapten is high in sensitivity and strong in specificity. The sensitivity (IC50) measured by an indirect competitive enzyme-linked immunoassay (ic-ELISA) method is 2.33 [mu] g/L, and the detection range (IC10-IC90) is 0.26-21.28 [mu] g/L. The monoclonal antibody and the propiconazole analogue have no cross reaction (CR is less than 0.1%). In addition, the monoclonal antibody is used for preparing the propiconazole colloidal gold rapid detection test strip which is high in detection sensitivity, strong in specificity, simple, convenient, rapid and low in cost. The test strip can be used for detecting propiconazole residues in agricultural products, and the detection limit of the test strip reaches 5 [mu] g/L.
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Paragraph 0011; 0032; 0038-0039
(2021/11/27)
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- Novel arylimino thiazole compound, preparation method and uses thereof
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The present invention relates to a compound with antibacterial synergy activity, a preparation and uses thereof, particularly to a novel arylimino thiazole compound, a preparation method and uses thereof, and specifically discloses a class of compounds represented by a formula (I) or optical isomers, cis-trans isomers or pharmaceutically acceptable salts thereof, a preparation method and uses thereof. The invention further discloses a pharmaceutical composition containing the compound. The compound of the present invention can effectively enhance the antibacterial activity of antibiotics, andcan be used for treating antibiotic-resistant bacteria. The formula (I) is defined in the specification.
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Paragraph 0235; 0238; 0239; 0240
(2018/03/28)
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- Antibacterial synergist, preparation method and uses thereof
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The present invention relates to an antibacterial synergist, a preparation method and uses thereof, and specifically discloses a compound represented by a formula (I) and having antibacterial synergyactivity, or an optical isomer, a cis-trans isomer or a pharmaceutically acceptable salt thereof, and a preparation method thereof. The present invention further discloses a medical composition containing the compound, and uses thereof. According to the present invention, the compound can effectively enhance the antibacterial activity of polymyxin B against Acinetobacter baumannii and Klebsiella pneumoniae, and can be used for the antibacterial treatment of pathogenic bacteria insensitive to polymyxin or having low bacterial inhibition activity. The formula (I) is defined in the specification.
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Paragraph 0339; 0340; 0341; 0342
(2018/03/28)
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- PYRAZOLE DERIVATIVES USEFUL AS INHIBITORS OF FAAH
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The present invention is directed to certain imidazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and t
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Page/Page column 149
(2010/01/07)
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