- Synthesis of novel azabicyclo derivatives containing a thiazole moiety and their biological activity against pine-wood nematodes
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To explore a new skeleton with nematicidal activity, a series of novel azabicyclo derivatives containing a thiazole moiety were designed, synthesized and evaluated for their nematicidal activities. The bioassay results against pine-wood nematodes (Bursaphelenchus xylophilus) showed that most of the title compounds displayed nematicidal activity at a concentration of 40 mg/L. Especially, the title compounds2-((8-methyl-8-azabicyclo[3.2.1]octan-3-yl)oxy)-4-(4-chlorophenyl)thiazole (7e), 2-((8-methyl-8-azabicyclo[3.2.1]octan-3-yl)thio)-4-phenylthiazole (10a) and 2-((8-methyl-8-azabicyclo [3.2.1]octan-3-yl)thio)-4-(4-chlorophenyl)thiazole (10e) exhibited more than 90% mortality against Bursaphelenchus xylophilus.
- Li, Hui,Lu, Aoyun,Zhang, Yanqiu,Peng, Yanqing,Song, Gonghua
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p. 371 - 375
(2020/01/02)
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- 2-mercapto-4-pyridyl thiazole synthesis method (by machine translation)
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The invention discloses a synthesis method of 2-sulfydryl-4-pyridyl thiazole. According to the technical scheme, 4-acetylpyridine serving as a raw material has a bromination reaction, and then ammonium dithiocarbamate is directly added to for reaction to obtain the 2-sulfydryl-4-pyridyl thiazole. The method is simple, efficient and mild in conditions, the intermediate is a bromide, the target product can be obtained by a one-pot process without purification, and the harm of the intermediate to a human body can be greatly reduced; and moreover, the obtained product is high in purity and yield and very suitable for industrial production.
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Paragraph 0023; 0024
(2017/04/08)
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- Synthesis method of ceftaroline fosamil intermediate 4-(4'-pyridyl)-1,3-thiazolyl-2-thiol
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The invention discloses a synthesis method of an important antibiotic ceftaroline fosamil intermediate 4-(4'-pyridyl)-1,3-thiazolyl-2-thiol. The method comprises the following steps: carrying out Claisen condensation reaction on ethyl isonicotinate and ethyl acetate under alkaline conditions, carrying out acidic hydrolysis for decarboxylation, carrying out bromination reaction on the hydrolysis product and bromine, carrying out cyclization on the bromination product and ammonium dithiocarbamate, and finally, refluxing the cyclization product in glacial acetic acid to obtain the corresponding 4-(4'-pyridyl)-1,3-thiazolyl-2-thiol. The method has the advantages of fewer synthesis steps, low cost, cheap and accessible materials and low pollution, and is beneficial to industrial production.
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- MORPHOLINE COMPOUND
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A compound represented by the formula (1) wherein ring A is aryl optionally having substituent(s) and the like; ring B is arylene optionally having substituent(s) and the like; m=0-2; n=1-5; X is a bond and the like; Y is a bond and the like; and Z is hydrogen atom and the like or a pharmaceutically acceptable salt thereof, and a hydrate or solvate thereof have affinity for CCR3, and can be pharmaceutical products for the treatment and/or prophylaxis of immune or inflammatory diseases.
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Page/Page column 31
(2010/11/27)
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- PHOSPHONOCEPHEM COMPOUND
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A cephem compound (particularly its crystal) represented by the formula [I], wherein X is CH3COOH, CH3CH2COOH or CH3CN, and n is 0 to 5, is useful as an antibacterial agent (particularly anti-MRSA agent) and shows superior quality such as high solid stability, possible long-term stable preservation and the like.
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- Carbapenem compounds and process for producing the same
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A novel β-lactam compound of the formula ?1!: STR1 or a pharmaceutically acceptable salt thereof, which shows an excellent antibacterial activity against Gram-positive bacteria, especially against methicillin-resistant staphylococci and methicillin-resistant coagulase-negative staphylococci, and a process for producing the same. R1, R2, X, Y, Z are as defined in the specifacation.
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