398489-26-4Relevant articles and documents
PROCESSES OF PREPARING A JAK1 INHIBITOR
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, (2021/12/17)
The present application provides processes for preparing 4-[3-(cyanomethyl)-3-(3′,5′-dimethyl-1H, 1′H-4,4′-bipyrazol-1-yl)azetidin-1-yl]-2,5-difluoro-N-[(1S)-2,2,2-trifluoro-1-methylethyl]benzamide, and phosphoric acid salt thereof, which is useful as a selective (Janus kinase 1) JAK1 inhibitor, as well as salt forms and intermediates related thereto.
Synthesis of trisubstituted alkenes by Ni-catalyzed hydroalkylation of internal alkynes with cycloketone oxime esters
Lu, Xiao-Yu,Liu, Chuang-Chuang,Jiang, Run-Chuang,Yan, Lu-Yu,Liu, Qi-Le,Wang, Qing-Qing,Li, Jia-Mei
supporting information, p. 14191 - 14194 (2020/11/24)
A method for Ni-catalyzed hydroalkylation of internal alkynes with cycloketone oxime esters was developed. The reaction has a broad substrate scope. This hydroalkylation shows excellent regio-and stereo-selectivity. This method enables readily available starting materials to be used to access a range of cyano-substituted single-configuration trisubstituted alkenes. These are valuable feedstock chemicals and are widely used in synthetic and medicinal chemistry.
Preparation method of 3-oxazetidine-1-carboxylic acid tert-butyl ester
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Paragraph 0029; 0033-0035, (2020/07/15)
The invention discloses a preparation method of 3-oxaazetidine-1-carboxylic acid tert-butyl ester. The preparation method comprises the following steps: firstly, synthesizing 2,2-bis(bromomethyl)-1,3-dioxolane from 1,3-dibromoacetone and ethylene glycol under the action of an acid, and cyclizing the 2,2-bis(bromomethyl)-1,3-dioxolane and tert-butyl carbamate under the action of an alkali to generate the 3-oxazetidine-1-carboxylic acid tert-butyl ester. The raw materials adopted in the method are cheap and easy to obtain, and the method is simple to operate, mild in reaction conditions, low inequipment requirements and suitable for industrial large-scale production.