6974-32-9Relevant articles and documents
Method for preparing 1-O-acetyl-2, 3, 5-tri-O-benzoyl-1-beta-D-ribofuranose
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Paragraph 0028; 0031-0032, (2020/08/18)
The invention relates to the field of organic synthesis, in particular to a method for preparing 1-O-acetyl-2, 3, 5-tri-O-benzoyl-1-beta-D-ribofuranose, which comprises the following steps: mixing D-ribose with methanol and a catalyst, heating to react, neutralizing, and concentrating to obtain a methyl esterification intermediate III; mixing the methyl esterification intermediate III with an organic solvent, 4-dimethylaminopyridine and an acid-binding agent, cooling, dropwise adding benzoyl chloride for reaction, washing with water for layering, and drying to obtain a benzoylated intermediateII; finally, mixing the benzoylated intermediate II with an organic solvent and acetic anhydride, then adding a catalyst, stirring, carrying out heat preservation reaction for 10-20 hours at the temperature of 0-70 DEG C, and after the reaction is qualified, cooling, crystallizing and centrifuging to obtain a crude product; finally, performing recrystallization and centrifugal drying to obtain the 1-O-acetyl-2, 3, 5-tri-O-benzoyl-1-beta-D-ribofuranose, and obtaining the 1-O-acetyl-2, 3, 5-tri-O-benzoyl-1-beta-D-ribofuranose. The method has the advantages of short reaction steps, high chemicaland optical purity, simple operation, easily available raw materials, low cost, small amount of three wastes, environmental friendliness and the like, and is suitable for industrial production.
3-Trifluoromethylpyrazolones derived nucleosides: Synthesis and antiviral evaluation
Ahmed, Ayman M. S.,Abou-Elkhair, Reham A. I.,El-Torky, Alaa M.,Hassan, Abdalla E. A.
, p. 590 - 603 (2019/04/03)
Dengue (DENV) viral infection is a global public health problem that infrequently develops life threatening diseases such as dengue hemorrhagic fever (DFS) and dengue shock syndrome (DSS). Middle East respiratory syndrome coronavirus (MERS-CoV) is a highly pathogenic human corona virus with 38% fatality rate of infected patients. A series of 4-arylhydrazono-5-trifluoromethyl-pyrazolones, their ribofuranosyl, and 5′-deoxyribofuranosyl nucleosides were synthesized, geometry optimized using Density functional theory (DFT), and evaluated for their antiviral activity. 2-Nitrophenylhydrazonopyra-zolone derivative 5 showed significant activity against MERS-CoV (EC50 = 4.6 μM). The nucleoside analog 8 showed moderate activity against DENV-2 (EC50 = 10 μM), while the activity was abolished with the corresponding 5′-deoxyribonucleoside analogs. The identified hits in this study set this category of compounds for further future optimizations.
A process for preparing 1 - O - acetyl - 2, 3, 5 - three - O - benzoyl - β - D - ribofuranosyl method (by machine translation)
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Paragraph 0012; 0013; 0016; 0018; 0020, (2018/10/11)
A process for preparing 1 - O - acetyl - 2, 3, 5 - three - O - benzoyl - β - D - ribofuranosyl method, including: S1, benzoylated reaction: the adenosine with organic solvent and mixed acid, dropping benzoyl chloride reaction, filtering, the filter cake washed with organic solvent, the filtrate, concentrating and recovering organic solvent to dry, adding methanol stirring beating, filtering, to obtain the [...]; S2, acylation reaction: [...] with the cosolvent and acetic anhydride mixing, stirring solution cleaning, dropping of a catalytic amount of paratoluenesulfonic acid, thermal insulation reaction, filtering, spend solvent washing the filter cake, the filtrate, washing filtrate, dried anhydrous magnesium sulfate, filtered, concentrated under reduced pressure for recovering the solvent, to obtain crude, recrystallization, get. The invention not only avoids the use of pyridine malodorous materials, but also has the step is short, the operation is simple, low cost, environment-friendly, "three wastes" less amount and the like, suitable for industrial production. (by machine translation)