20054-45-9Relevant articles and documents
Axitinib intermediate compound and preparation method thereof
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Paragraph 0040-0057, (2021/01/24)
The invention belongs to the field of pharmaceutical chemicals, and particularly relates to an axitinib intermediate compound and a preparation method thereof. The present invention provides a novel axitinib intermediate compound S-(2-(methylcarbamoyl) phenyl) dimethylthioformate, the invention also provides a preparation method thereof. The method comprises the following steps: dissolving 2-hydroxy-N-methylbenzamide in an organic solvent, and adding dimethylaminothioformyl chloride and a catalyst to obtain the S-(2-(methylcarbamoyl) phenyl) dimethylthioformate. The new intermediate compound can be used for preparing the axitinib important intermediate 2-sulfydryl-N-methylbenzamide, and the synthesis method provided by the invention is short in route, simple to operate and high in yield and purity of the obtained 2-sulfydryl-N-methylbenzamide, and is suitable for industrial production.
Safe, Scalable, Inexpensive, and Mild Nickel-Catalyzed Migita-Like C?S Cross-Couplings in Recyclable Water
Yu, Tzu-Yu,Pang, Haobo,Cao, Yilin,Gallou, Fabrice,Lipshutz, Bruce H.
supporting information, p. 3708 - 3713 (2020/12/17)
A new approach to C?S couplings is reported that relies on nickel catalysis under mild conditions, enabled by micellar catalysis in recyclable water as the reaction medium. The protocol tolerates a wide range of heteroaromatic halides and thiols, including alkyl and heteroaryl thiols, leading to a variety of thioethers in good isolated yields. The method is scalable, results in low residual metal in the products, and is applicable to syntheses of targets in the pharmaceutical area. The procedure also features an associated low E Factor, suggesting a far more attractive entry than is otherwise currently available, especially those based on unsustainable loadings of Pd catalysts.
NOVEL ULK1 INHIBITORS AND METHODS USING SAME
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Page/Page column 145, (2016/03/22)
In certain aspects, the invention provides a method for treating a disease or condition in a subject, the method comprising co-administering to a subject in need thereof a therapeutically effective amount of at least one ULK1-inhibiting pyrimidine, and a therapeutically effective amount of an mTOR inhibitor.