76088-98-7Relevant articles and documents
Targeting sars-cov-2 polymerase with new nucleoside analogues
Apostolou, Panagiotis,Daikopoulou, Vasiliki,Gougousi, Maria,Mourati, Sofia,Papasotiriou, Ioannis,Vlachou, Ioanna
, (2021/06/21)
Despite the fact that COVID-19 vaccines are already available on the market, there have not been any effective FDA-approved drugs to treat this disease. There are several already known drugs that through drug repositioning have shown an inhibitory activity against SARS-CoV-2 RNA-dependent RNA polymerase. These drugs are included in the family of nucleoside analogues. In our efforts, we synthesized a group of new nucleoside analogues, which are modified at the sugar moiety that is replaced by a quinazoline entity. Different nucleobase derivatives are used in order to increase the inhibition. Five new nucleoside analogues were evaluated with in vitro assays for targeting polymerase of SARS-CoV-2.
Facile and efficient synthesis of quinazoline-2,4(1H,3H)-diones through sequential hydrogenation condensation
Wang, Peng-Xu,Wang, Ya-Nan,Lin, Zi-Yun,Li, Gang,Huang, Hai-Hong
supporting information, p. 1183 - 1189 (2018/04/02)
The heterocyclizations from various methyl (2-nitrobenzoyl)carbamates to substituted quinazoline-2,4(1H,3H)-diones under hydrogenation conditions were investigated in this study. In the presence of p-toluenesulfonic acid monohydrate in methanol, various q
Preparation method of quinazoline diketone derivative
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Paragraph 0018, (2017/03/28)
The invention belongs to the technical field of medicine, and especially relates to a preparation method of a quinazoline diketone derivative. The preparation method is friendly to the environment; synthesis requirements are low; and operation method is simple. The preparation method comprises following steps: (1) acetonitrile with excellent dissolvability is taken as a solvent, isocyanic acid is prepared via acidification of potassium isocyanate with 2.0 times equivalent weight, and reaction is carried out for 2h at 50 DEG C; (2) 1.88g PPh3 is dissolved in 15ml of methylbenzene, 0.8ml of ethyl bromoacetate is added, reaction is carried out at room temperature for one night; (3) NaOH is added into an obtained reaction liquid, when alkali adding amount is 4 times equivalent weight, it is shown by LC-MS that cyclization reaction is completed, hydrochloric acid is added so as to adjust pH value to 1, the solvent is recovered via decompression, and the quinazoline diketone derivative is obtained via silica-gel column chromatography separation.