41270-66-0Relevant articles and documents
Method for preparing selexipag intermediate
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Paragraph 0014, (2020/07/24)
The invention discloses a preparation method of a selexipag intermediate 5-chloro-2,3-diphenyl piperazine. The preparation method comprises the following steps: carrying out a reaction on 5,6-diphenyl-2-hydroxypyrazine with phosphorus oxychloride for 10-12 hours under heating, wherein an acid-binding agent is added into an organic solvent environment; adding the reaction product into ice water forcrystallization, and performing filtration and washing to obtain the 5-chloro-2,3-diphenyl piperazine. By means of the method, the defects of an existing method are overcome, wherein the use amount of phosphorus oxychloride is reduced, phosphorus-containing sewage discharge is reduced, and the obtained intermediate is high in purity, good in yield, simple to operate and suitable for industrial production.
PROCESS FOR THE PREPARATION OF DIPHENYLPYRAZINE DERIVATIVES
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, (2017/10/31)
The present invention relates to a process for the preparation of amorphous Selexipag from Selexipag crystalline salts using a solvent.
3-(Piperidin-4-ylmethoxy)pyridine Containing Compounds Are Potent Inhibitors of Lysine Specific Demethylase 1
Wu, Fangrui,Zhou, Chao,Yao, Yuan,Wei, Liping,Feng, Zizhen,Deng, Lisheng,Song, Yongcheng
, p. 253 - 263 (2016/01/29)
Methylation of histone lysine residues plays important roles in gene expression regulation as well as cancer initiation. Lysine specific demethylase 1 (LSD1) is responsible for maintaining balanced methylation levels at histone H3 lysine 4 (H3K4). LSD1 is a drug target for certain cancers, due to important functions of methylated H3K4 or LSD1 overexpression. We report the design, synthesis, and structure-activity relationships of 3-(piperidin-4-ylmethoxy)pyridine containing compounds as potent LSD1 inhibitors with Ki values as low as 29 nM. These compounds exhibited high selectivity (>160×) against related monoamine oxidase A and B. Enzyme kinetics and docking studies suggested they are competitive inhibitors against a dimethylated H3K4 substrate and provided a possible binding mode. The potent LSD1 inhibitors can increase cellular H3K4 methylation and strongly inhibit proliferation of several leukemia and solid tumor cells with EC50 values as low as 280 nM, while they had negligible effects on normal cells.