1201186-54-0Relevant articles and documents
Preparation method of 2-bromo-5-p-toluenesulfonyl-5H-pyrrolo [2, 3-b] pyrazine
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Paragraph 0029-0040, (2021/11/06)
The method comprises the following steps of: 1, dissolving 3-[(trimethylsilyl) ethynyl]-5-pyrazine-2-amine in a solvent N, N-dimethylacetamide, adding a mild alkali reagent, heating, and reacting for 0.5-2 hours; 2, cooling the reaction system to room temperature, adding paratoluensulfonyl chloride, cooling the reaction system to room temperature, and mkaing the reaction system react at room temperature for 0.5-2 hours; and 3, adding a product into a 0.5-10% wt sodium bicarbonate aqueous solution, and then filtering, recrystallizing, filtering and drying to obtain a finished product of the 2-bromo-5-p-toluenesulfonyl-5H-pyrrolo [2, 3-b] pyrazine. Compared with the prior art in which sodium hydride is adopted as an alkali reagent, the preparation method of the 2-bromo-5-p-toluenesulfonyl-5H-pyrrolo [2, 3-b] pyrazine provided by the invention has the following advantages that: the mild alkali reagent such as sodium tert-butoxide is used in the preparation process, and the purification mode is improved; reaction conditions are mild and controllable, and by-products in the reaction process are few; and the operation and post-treatment are simple, the product yield and quality are obviously improved, the production time and cost can be saved, and the method is suitable for industrial production.
IRAK4 kinase inhibitor and preparation method thereof
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Paragraph 0115-0120; 0152-0157; 0187-0192; 0221-0226; 0252, (2021/02/05)
The present invention provides a compound represented by a general formula I, and a pharmaceutically acceptable salt, a stereoisomer, an ester, a prodrug, a solvate and a deuterated compound thereof,and the compound is an IRAK4 kinase inhibitor, and can be used for prevention and/or treatment of IRAK4 related diseases, such as autoimmune diseases, inflammatory diseases, cancers, heteroimmune diseases, thromboembolism, atherosclerosis, myocardial infarction and metabolic syndrome.
JAK kinase inhibitor, preparation method thereof, and application in the field of medicines
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Paragraph 0268; 0271; 0274; 0275, (2019/04/10)
The application relates to a JAK kinase inhibitor, a preparation method thereof, and an application in the field of medicines and belongs to the field of medical chemistry. In the application, a series of novel small-molecular JAK inhibitors are provided and are represented as the general formula (II). The compounds have better effects and higher safety in prevention or treatment on JAK-related adaptation diseases.