32873-57-7Relevant articles and documents
Synthetic method for drug intermediate 1,3,4-thiadiazole-2-acetamido-5-sulfonyl chloride
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Paragraph 0017-0018; 0021-0022; 0023-0026, (2018/07/30)
The invention discloses a synthetic method for the drug intermediate 1,3,4-thiadiazole-2-acetamido-5-sulfonyl chloride. The synthetic method comprises the following steps: adding 2-acetamido-5-thiomethyl-1,3,4-thiadiazole into a reaction vessel, controlling a temperature, adding a potassium nitrate solution, controlling a stirring speed and carrying out a reaction; and adding lanthanum nitrate inbatches, controlling the temperature, adding a 3-chlorophenol solution in batches within a certain period of time, continuing the reaction, adjusting the pH of value the obtained solution, allowing asolid to be precipitated, washing the solid with a sodium sulfate solution a plurality of times, then washing the solid with a cyclobutane solution a plurality of times, then washing the solid with amethylamine solution a plurality of times, carrying out recrystallization in a t-butanol solution, and then carrying out dehydration with a dehydrating agent so as to obtain the finished 1,3,4-thiadiazole-2-acetamido-5-sulfonyl chloride.
Key intermediate aqiang 2-acetyl-5-chlorosulfonyl -1, 3, 4-thiadiazole method for preparing the non-chlorine (by machine translation)
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Paragraph 0029, (2017/01/02)
The invention discloses a preparation method of non-chlorine gas of acetazolamide key intermediate 2-acetamido-5-chlorosulfonyl-1, 3, 4-thiadiazole. The preparation method comprises the steps of firstly adding hydrochloric acid into a reactor and then dropwise adding hydrogen peroxide to perform reaction so as to obtain a reaction solution; adding 2-acetamido-5-sulfydryl-1, 3, 4-thiadiazole into the obtained reaction solution in batch to perform reaction and obtaining a reactant after reaction is completed; directly conducting suction filtration, washing and drying on the reactant and performing drying to obtain the intermediate 2-acetamido-5-chlorosulfonyl-1, 3, 4-thiadiazole. The preparation method is more moderate in operate and more environment-friendly, and the obtained intermediate 2-acetamido-5-chlorosulfonyl-1, 3, 4-thiadiazole is good in color and luster and high in purity.
Synthesis, antibacterial and?antitubercular activities of?some?7-[4-(5-amino-[1,3,4]thiadiazole-2-sulfonyl)-piperazin -1-yl] fluoroquinolonic derivatives
Talath,Gadad
, p. 918 - 924 (2007/10/03)
In the present study, a series of 7-[4-(5-amino-1,3,4 thiadiazole-2-sulfonyl)]-1-piperazinyl fluoroquinolonic derivatives VIIa-d were synthesized in good yields and characterized by IR, 1H-NMR, 13C-NMR, FAB Mass spectral and elemental analyses. The compounds were evaluated for their preliminary in vitro antibacterial activity against some Gram-positive and Gram-negative bacteria and selected compounds VIIa, b were screened for antitubercular activity against Mycobacterium tuberculosis H37Rv strain by broth dilution assay method. The antibacterial data of the tested N-sulfonylfluoroquinolones VIIa-d indicated that all the synthesized compounds showed better activity against Gram-positive bacteria S.?aureus, E.?faecelis, Bacillus sp. (MIC = 1-5?μg?ml-1, respectively) compared to reference drugs. The MIC values of tested derivatives connotes that the sparfloxacin and gatifloxacin derivatives VIIc, d were most active against the tested Gram-positive bacterial strains (MIC = 1-5?μg?ml-1). All the tested compounds VIIa-d showed poor activity against the Gram-negative bacteria. The in vitro antitubercular activity reports of selected compounds VIIa, b against M.?tuberculosis strain H37Rv showed moderate activity at MIC of 10?μg?ml-1.
