1352625-29-6Relevant articles and documents
Synthesis of pyrazol [1,5-alpha] pyridine-3-carboxylic acid derivatives
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Paragraph 0012; 0058; 0059; 0060; 0061; 0062; 0063, (2019/02/04)
The invention relates to synthesis of pyrazol [1,5-alpha] pyridine-3-carboxylic acid derivatives, and belongs to the field of organic synthesis. Trimethylsulfonyl chloride is used as a raw material toreact with tert-butoxycarbonyl hydroxylamine to obtain a compound 3; then the compound 3 reacts with trifluoroacetic acid to obtain a mixed solution of a compound 4; the mixed solution directly reacts with pyrazine to obtain a compound 6 without carrying out separation, washing and drying; an ethyl propiolate reaction is continuously performed; a water phase obtained after the reaction is extracted by ethyl acetate; an organic extract obtained after extraction is dried by anhydrous MgSO4 and evaporated; remaining residues are subjected to recrystallization (ethyl acetate, methylbenzene or petroleum ether), separation, washing and drying to obtain a compound 8; the compound 8 further reacts with NaOH to obtain a compound 9. In the route, the second step and the third step are continuouslycarried out, so that not only is the risk of the process reduced, but also yield is over 70%. No matter whether the raw material is of a symmetrical structure, the target product can be accurately obtained. The synthesis is suitable for industrial production.
Heteroaryl imidazolone derivatives as jak inhibitors
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Page/Page column 107, (2012/01/06)
New heteroaryl imidazolone derivatives having the chemical structure of formula (I) are disclosed; as well as process for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Janus Kinases (JAK).
