45534-08-5Relevant articles and documents
Preparation method of 3-amino-5-methylmercapto-1,2,4-triazole
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Paragraph 0031-0033, (2017/07/07)
The invention discloses a preparation method of 3-amino-5-methylmercapto-1,2,4-triazole. The preparation method comprises the following steps of carrying out nitrogen replacement on a reactor, and then using dimethyl cyanimino dithiocarbonate and a hydrazine hydrate as raw materials, wherein a solvent is an alcohol organic solvent; adding the dimethyl cyanimino dithiocarbonate into the solvent, agitating an obtained first mixture to dissolve the dimethyl cyanimino dithiocarbonate, and then slowly dropwise adding the hydrazine hydrate into the first mixture in a condition of 25 to 28 DEG C, wherein the mole ratio of the dimethyl cyanimino dithiocarbonate to the hydrazine hydrate is (1 to 1.1) to (1 to 15); dropwise adding the hydrazine hydrate for 1.5 to 2 hours, subsequently raising a temperature to 65 to 70 DEG C, in a refluxing condition, carrying out a reaction for 2 to 3 hours, preparing and synthesizing a similarly white solid through a one-step reaction, and confirming the similarly white solid to be the target product 3-amino-5-methylmercapto-1,2,4-triazole through nuclear magnetic resonance. The target product is prepared and synthesized through the one-step reaction; the costs of the raw materials are low; iodine-containing wastewater which pollutes an environment is not generated; operation steps are simple; further, the purity of the product can reach 98 percent or above; the preparation method has a quite good commercial application prospect, and is worthy to popularized in a large range.
ANTI-VIRAL DRUG
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Page/Page column 24-25, (2017/09/21)
An antiviral compound for use in the treatment of negative-sense, single-stranded RNA [herein after ssRNA] virus infections different from the Influenza A and Influenza B virus infections wherein said antiviral compound is of general formula (I) ) [compound (A), herein after] or a pharmaceutically acceptable salt thereof wherein - R1 is selected from an alkyl group having 1 to 12 carbon atoms which is optionally substituted by a halogen atom or hydroxyl group, a cycloalkyl group having 3 to 12 carbon atoms which is optionally substituted by a halogen atom or hydroxyl group, an aryl group, an alkylaryl group, or a cycloheteroalkyl group having 3 to 12 carbon atoms, preferably an alkyl group having 1 to 8 carbon atoms optionally substituted by a halogen atom or hydroxyl group, a cycloalkyl group having 3 to 6 carbon atoms which is optionally substituted by a halogen atom or hydroxyl group, a phenyl, a benzyl, a morpholine, or an imidazolyl, more preferably an alkyl group having 1 to 4 carbon atoms, a cyclohexyl, a phenyl or a benzyl.
Synthesis and evaluation of 1,2,4-triazolo[1,5- a ]pyrimidines as antibacterial agents against Enterococcus faecium
Wang, Huan,Lee, Mijoon,Peng, Zhihong,Blázquez, Blas,Lastochkin, Elena,Kumarasiri, Malika,Bouley, Renee,Chang, Mayland,Mobashery, Shahriar
, p. 4194 - 4203 (2015/06/08)
Rapid emergence of antibiotic resistance is one of the most challenging global public health concerns. In particular, vancomycin-resistant Enterococcus faecium infections have been increasing in frequency, representing 25% of enterococci infections in intensive care units. A novel class of 1,2,4-triazolo[1,5-a]pyrimidines active against E. faecium is reported herein. We used a three-component Biginelli-like heterocyclization reaction for the synthesis of a series of these derivatives based on reactions of aldehydes, β-dicarbonyl compounds, and 3-alkylthio-5-amino-1,2,4-triazoles. The resulting compounds were assayed for antimicrobial activity against the ESKAPE panel of bacteria, followed by investigation of their in vitro activities. These analyses identified a subset of 1,2,4-triazolo[1,5-a]pyrimidines that had good narrow-spectrum antibacterial activity against E. faecium and exhibited metabolic stability with low intrinsic clearance. Macromolecular synthesis assays revealed cell-wall biosynthesis as the target of these antibiotics.
