16849-88-0Relevant articles and documents
Synthesis and Antiviral Bioactivity of Novel 2-Substituted Methlthio-5-(4-Amino-2-Methylpyrimidin-5-yl)-1,3,4-Thiadiazole Derivatives
Wu, Wen-Neng,Tai, An-Qi,Chen, Qin,Ouyang, Gui-Ping
, p. 626 - 632 (2016)
A series of novel 2-substituted methlthio-5-(4-amino-2-methylpyrimidin-5-yl-)-1,3,4-thiadiazole derivatives were synthesized, characterized and evaluated for antiviral activities against tobacco mosaic virus (TMV). The preliminary biological results indicated that most compounds exhibit excellent antiviral activity against TMV in vivo. Among these compounds, compounds 9c, 9i, and 9p displayed the similar curative effect against TMV (EC50 = 287.05-322.47 μg/mL) to that of the commercial agent Ningnanmycin (EC50 = 301.83 μg/mL). In particular, compound 9d demonstrated the best curative effect against TMV (EC50 = 266.21 μg/mL), which was better than that of commercial Ningnanmycin.
Fully Continuous Flow Synthesis of 5-(Aminomethyl)-2-methylpyrimidin-4-amine: A Key Intermediate of Vitamin B1
Chen, Fener,Huang, Huashan,Jiang, Meifen,Liu, Minjie
supporting information, p. 2331 - 2337 (2021/10/25)
Herein, we demonstrate an expeditiously fully continuous flow synthesis of 5-(aminomethyl)-2-methylpyrimidin-4-amine, a key intermediate for vitamin B1. The process is accomplished via three chemical transformations in six sequential continuous flow devices from an economical starting material, 2-cyanoacetamide. First, single step continuous flow synthesis is demonstrated in a certain type of flow reactor for each reaction step, with a yield of 94, 90, and 99%, respectively. Then, fully continuous flow synthesis of 5-(aminomethyl)-2-methylpyrimidin-4-amine is demonstrated in 84% total yield with a total residence time of 74 min and 0.92 g/h throughput.
Method for continuously preparing (dimethylamine methylene)malononitrile by using micro-reaction system
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Paragraph 0048-0134, (2020/12/15)
The invention discloses a method for continuously preparing (dimethylamine methylene)malononitrile by using a micro-reaction system. The method comprises the steps of respectively and simultaneously pumping a solution obtained by mixing cyanoacetamide, N,N-dimethylformamide and a catalyst and phosphorus oxychloride into a micro-reaction system comprising a first micro-mixer and a micro-channel reactor which are communicated with each other, and carrying out continuous catalytic dehydration condensation reaction; after the pH value of the crude product mixed solution is adjusted, carrying out continuous liquid-liquid extraction separation on the crude product mixed solution in a centrifugal extraction unit composed of a plurality of annular space type centrifugal extractors connected in series by using an organic solvent, collecting an extraction phase to obtain the target product (dimethylamine methylene)malononitrile. Compared with the prior art, the method has the advantages that thereaction can be safely carried out at normal temperature, the reaction time is short, the product yield is greater than 95%, the efficiency of the technological process is high, the energy consumption is low, and the method has a good industrial application prospect.
