5444-02-0Relevant articles and documents
Continuous flow synthesis of some 6- And 1,6-substituted 3-cyano-4-methyl-2-pyridones
Tadi?, Julijana,Mihajlovi?, Marina,Jovanovi?, Mi?a,Mijin, Du?an
, p. 531 - 538 (2019/08/30)
In this study, six 6- and 1,6-substituted-3-cyano-4-methyl-2-pyri-dones were synthesized in a continuous flow microreactor system. The syntheses were realized at room temperature and the obtained results were compared to those achieved within classical syntheses. In order to optimize the continuous flow syntheses and increase the yield of the products, the retention time in the microreactor was varied by changing the flow rates of the reactant solutions. Furthermore, the reaction was optimized for 3-cyano-4,6-dimethyl-2-pyridone and 3-cyano-6-hydroxy-4-methyl-2-pyridone, which are comercially important in the pharmaceutical and dye industries. Both 2-pyridones were obtained in satisfactory yield of circa 60 % in less than 10 min. The resulting compounds were characterized by their melting points, FT-IR, 1H-NMR and UV–Vis spectra. The efficiency of the presented method for the synthesis of 2-pyridone-based molecules has promising potential for industrial production.
NEK6 KINASE INHIBITORS USEFUL FOR THE TREATMENT OF SOLID TUMORS
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Page/Page column 14, (2019/10/29)
The mitotic kinases regulating the dynamics of centrosomes and the functions of the mitotic spindle are potential targets for the antitumour therapy. In the present invention some molecules with inhibitory activity on NEK6 have been identified. The present invention relates to such molecules and to the compositions including them for use as inhibitors of NEK6 in a method of treatment of tumours both in monotherapy and in combinations with other drugs.
Preparation method for nevirapine intermediate
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Paragraph 0009; 0031; 0041; 0051; 0059-0061, (2019/01/14)
The invention provides a preparation method for a nevirapine intermediate. The preparation method comprises: performing a cyclization reaction of ammonia water, methyl cyanoacetate and methyl acetoacetate to form a compound hydroxyl: 2,6-dihydroxy-3-cyano-4-methylpyridine; adding triethylamine dropwise, introducing chlorine gas at the temperature until the reaction is complete, and obtaining 2,6-dichloro-3-cyano-4-methylpyridine; adding concentrated sulfuric acid, heating to 120 DEG C to react for 3-5 h, and then cooling to 60 DEG C; adding water to perform hydrolysis reaction, and obtaining 2,6-dichloro-3-amido-4-methylpyridine; adding a degradation reagent sodium hypochlorite, and obtaining a nevirapine intermediate 2,6-dichloro-3-amino-4- methylpyridine by Hofmann reaction. According tothe preparation method, commonly used phosphorus oxychloride is replaced with the directly introduced chlorine gas, which solves the problems that the wastewater content is too high, it is difficultto perform treatment and the odor of phosphorus oxychloride is bad, and the one-time yield of the product is 90.1%.