445264-61-9Relevant articles and documents
Transformations of Aryl Ketones via Ligand-Promoted C?C Bond Activation
Dai, Hui-Xiong,Li, Hanyuan,Li, Ling-Jun,Liu, Qi-Sheng,Ma, Biao,Wang, Mei-Ling,Wang, Xing,Wang, Zhen-Yu,Xu, Hui
, p. 14388 - 14393 (2020/07/06)
The coupling of aromatic electrophiles (aryl halides, aryl ethers, aryl acids, aryl nitriles etc.) with nucleophiles is a core methodology for the synthesis of aryl compounds. Transformations of aryl ketones in an analogous manner via carbon–carbon bond activation could greatly expand the toolbox for the synthesis of aryl compounds due to the abundance of aryl ketones. An exploratory study of this approach is typically based on carbon–carbon cleavage triggered by ring-strain release and chelation assistance, and the products are also limited to a specific structural motif. Here we report a ligand-promoted β-carbon elimination strategy to activate the carbon–carbon bonds, which results in a range of transformations of aryl ketones, leading to useful aryl borates, and also to biaryls, aryl nitriles, and aryl alkenes. The use of a pyridine-oxazoline ligand is crucial for this catalytic transformation. A gram-scale borylation reaction of an aryl ketone via a simple one-pot operation is reported. The potential utility of this strategy is also demonstrated by the late-stage diversification of drug molecules probenecid, adapalene, and desoxyestrone, the fragrance tonalid as well as the natural product apocynin.
COMBINATION THERAPY WITH A PHOSPHOINOSITIDE 3-KINASE INHIBITOR WITH A ZINC BINDING MOIETY
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Page/Page column 26; 28, (2018/05/24)
The invention provides a method of treating cancer in a subject in need thereof, comprising administering to the subject: (a) a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein R is hydrogen or an acyl group; and (b) a BCL-2 inhibitor; wherein the compound of Formula I or pharmaceutically acceptable salt thereof and a BCL-2 inhibitor are administered in amounts which in combination are therapeutically effective. The invention further provides a pharmaceutical composition comprising a compound of Formula I or a pharmaceutically acceptable salt thereof, a BCL-2 inhibitor and a pharmaceutically acceptable carrier or excipient.
2-methoxy-5-(pyridine-2-yl)pyridine synthesis method
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Paragraph 0005; 0014, (2017/03/17)
The invention belongs to the field of medicinal chemistry and relates to a preparation technology of 2-methoxy-5-(pyridine-2-yl)pyridine as a perampanel intermediate. The preparation technology comprises that 5-bromo-2-methoxypyridine and bis(pinacolato)diboron undergo a reaction to produce 2-methoxypyridine-5-boronic acid pinacol ester and the 2-methoxypyridine-5-boronic acid pinacol ester and 2-halogenated pyridine undergo a reaction to produce 2-methoxy-5-(pyridine-2-yl)pyridine as a perampanel intermediate. The synthesis method solves the problem of a high catalyst cost, has the advantages of simple processes and low cost and is convenient for large scale production.
