- Synthetic method of decoquinate
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The invention discloses a synthetic method of decoquinate, and belongs to the technical field of pharmaceutical engineering. The synthetic method takes o-hydroxyphenyl ethyl ether as a raw material to prepare decoquinate via the processes of coupling, reduction, condensation, etherification, cyclization and the like. The process of reduction in the method adopts environment-friendly hydrazine hydrate as a reducer to reduce an azo-compound and introduce an amino group, so that the synthetic method is good in selectivity, and environmentally friendly, and beneficial for reducing environmental pollution problems; BTC is adopted as a cyclization reagent in the process of cyclization, so that the condition is mild, the requirement on equipment is lowered, and the cost is reduced.
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Paragraph 0018; 0023; 0029
(2018/03/01)
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- Preparation method of decoquinate
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The invention discloses a preparation method of decoquinate. Industrialized 2-hydroxyphenylacetic acid phenetole serves as starting materials, and a product with better quality is obtained through diazo coupling, sodium dithionite reduction, condensation, etherificationa and superstrong solid acid SO4/Fe2O3 and sodium bisulfate cyclization. Part intermediate of a synthetic route of the decoquinate does not need to be purified, used solvent is single, aftertreatment of the intermediate and use of organic solvent are reduced, the cost is reduced, the whole process route is short, extremely high temperature or highly corrosive liquid acid is not needed, requirement to equipment is low, operation is easy and convenient, the production cycle is short, produced three wastes are fewer, the production yield is high, the quality is good, and the preparation method of the decoquinate is suitable for industrial production.
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Paragraph 0026
(2017/01/19)
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- Synthesis and anticoccidial activities of Quinoline Carboxylate derivatives with Methyl (E)-2-(3-methoxy)acrylate moiety
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A series of novel quinoline carboxylate derivatives with methyl (E)-2-(3-methoxy) acrylate group were designed and synthesized as anticoccidial medicines. The structures were confirmed by 1H NMR, IR and HR-MS spectra. The biological activities were primarily evaluated according to the anticoccidial index method. The results indicated that these compounds (7c, 7d, 7e, 7g) exhibited anticoccidial activities against Eimeria tenella. In particular, the anticoccidial index of 6-decyloxy-7-ethoxy-4-{6-[2-(2-methoxy-1-methoxycarbonyl- vinyl)phenoxy]pyrimidin-4-yloxy}- quinoline-3-carboxylic acid ethyl ester (7e) was 168.7, which indicated that the compound has a good anticoccidial activity.
- Liu, Yuan,Weng, Ya-Biao,Chen, Zhao-Bing,Wang, Yu-Liang
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p. 8509 - 8512
(2013/11/06)
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- Synthesis and anticoccidial activity of ethyl 6-substitutedbenzyloxy-7- alkoxy-4-hydroxyquinoline-3-carboxylates
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A series of novel ethyl 6-substitutedbenzyloxy-7-alkoxy-4-hydroxyquinoline- 3-carboxylates have been designed and synthesised from 4-nitro-2-alkoxyphenol. Their structures have been characterised by 1H NMR, HRMS and IR spectra. Anticoccidial activities of
- Zou, Yan,Yan, Chun-Rong,Weng, Ya-Biao,Li, Juan,Wu, Kai-Qun,Wang, Yu-Liang,Wang, Yu-Zhong
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experimental part
p. 252 - 254
(2009/12/03)
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- NPY ANTAGONISTS, PREPARATION AND USES
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The present invention concerns novel compounds, their preparation and their uses, therapeutic uses in particular. More specifically it concerns derivative compounds having at least two aromatic cycles, their preparation and their uses, in particular in the area of human or animal health. These compounds have an affinity for the biological receptors of neuropeptide Y, NPY, present in the central and peripheral nervous systems. The compounds of the invention are preferably NPY antagonists, and more particularly antagonists of sub-type NPY Y1, and can therefore be used for the therapeutic or prophylactic treatment of any disorder involving NPY. The present invention also concerns pharmaceutical compositions containing said compounds, their preparation and their uses, as well as treatment methods using said compounds.
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Page/Page column 84
(2009/09/28)
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- Metabolism of fungicide diethofencarb in grape (Vitis vinifera L.): Definitive identification of thiolactic acid conjugated metabolites
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The metabolic fate of diethofencarb (isopropyl 3,4-diethoxycarbanilate) separately labeled with 14C at the phenyl ring and 2-position of the isopropyl moiety was studied in grape (Vitis vinifera L.). The acetonitrile solution of 14C-diethofencarb at a rate of 500 g a.i. ha -1 was once applied topically to fruits or leaves at the maturity stage of fruits (PHI 35 days), and the plants were grown in the greenhouse until harvest. In the grape plants, diethofencarb was scarcely translocated to the untreated portion and was degraded more in the fruit as compared to the leaf. For the fruit, diethofencarb primary underwent O-deethylation at the 4-position of the phenyl ring to form the phenolic derivative, isopropyl 3-ethoxy-4-hydroxycarbanilate (0.9% of the total radioactive residue, TRR). This metabolite was successively transformed via conjugation with glucose at the phenolic hydroxy group (8.1-18.1% TRR) or with thiolactic acid at the 5-position of the phenyl ring (1.5-1.7% TRR). The thiolactic acid conjugate was further metabolized mainly to two different types of glucose conjugates at the 4-position of the phenyl ring (8.7-13.5% TRR) and the hydroxy group in the thiolactic acid moiety (6.4-7.3% TRR), as evidenced by 1H NMR and atmospheric pressure chemical ionization-liquid chromatography-mass spectrometry together with cochromatographies with synthetic standards.
- Fujisawa, Takuo,Ichise-Shibuya, Keiko,Katagi, Toshiyuki,Ruzo, Luis O.,Takimoto, Yoshiyuki
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p. 5329 - 5336
(2007/10/03)
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