20054-45-9Relevant articles and documents
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.
Preparation method of axitinib intermediate
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Paragraph 0056-0072, (2021/01/24)
The present invention belongs to the field of medicine synthesis, and particularly relates to a preparation methodof an axitinib intermediate 2-sulfydryl-N-methylbenzamide, the method comprises the following steps: the intermediate compound S-(2-(methylcarbamoyl) phenyl) dimethylthioformate is synthesized by taking 2-hydroxy-N-methylbenzamide as a raw material under the action of a catalyst, and the new intermediate is further synthesized into the 2-sulfydryl-N-methylbenzamide under the action of alkali. The synthesis method provided by the invention is short in route and simple to operate, and the obtained 2-sulfydryl-N-methylbenzamide is high in yield, high in purity and more suitable for industrial production.
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.