42753-71-9Relevant articles and documents
Directing Group Enables Electrochemical Selectively Meta-Bromination of Pyridines under Mild Conditions
Wu, Yanwei,Xu, Shanghui,Wang, Hong,Shao, Dongxu,Qi, Qiqi,Lu, Yi,Ma, Li,Zhou, Jianhua,Hu, Wei,Gao, Wei,Chen, Jianbin
, p. 16144 - 16150 (2021/07/19)
Without the use of catalysts and oxidants, a facile and sustainable electrochemical bromination protocol was developed. By introducing the directing groups, the regioselectivity of pyridine derivatives could be controlled at themeta-position utilizing the inexpensive and safe bromine salts at room temperature. A variety of brominated pyridine derivatives were obtained in 28-95% yields, and the reaction could be readily performed at a gram scale. By combining the installation and removing the directing group, the concept ofmeta-bromination of pyridines could be verified.
multi-links class PI3K inhibitors (by machine translation)
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Paragraph 0271; 0272; 0273, (2016/10/09)
The invention belongs to the field of medical technology, in particular of formula (I) shown in multi-links class of PI3K inhibitors, its stereoisomers or its pharmaceutically acceptable salt thereof, wherein the R 1, R 2, R 3, R 4 or R 5 as defined in the specification; the invention also relates to methods of preparing such compounds, pharmaceutical compositions of these compounds in the preparation and treatment and/or prevention of proliferative diseases of the use of the medicament. (by machine translation)
Preparation method of 2-amino-5-methyl-6-bromopyridine
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Paragraph 0023; 0024; 0025, (2016/10/07)
For overcoming defects in the prior art, the invention provides a preparation method of 2-amino-5-methyl-6-bromopyridine, which belongs to the technical field of synthesis of pharmaceutical intermediates. The method comprises the following steps: adding an organic solvent subjected to water removal into sodamide under the protection of nitrogen, then heating a solution, and after 2-bromo-3-methylpyridine is added, carrying out reflux reaction on the obtained mixture under the condition that the temperature is kept; and after the reaction is completed, cooling the solution, adding ice water, separating out an upper organic solvent, and sequentially carrying out concentration and crystallization on the organic solvent, so that a product is obtained. According to the invention, a product is directly obtained through one-step amination, therefore, the method is safe and simple in process, and suitable for industrial production.