221218-33-3Relevant articles and documents
Electrochemically Enabled Intramolecular Aminooxygenation of Alkynes via Amidyl Radical Cyclization
Hou, Zhong-Wei,Xu, Hai-Chao
supporting information, p. 394 - 398 (2020/03/04)
An electrochemical synthesis of oxazol-2-ones and imidazol-2-ones has been developed via 5-exo-dig cyclization of propargylic carbamates- and ureas-derived amidyl radicals. The electrosynthesis relies on the dual function of 2,2,6,6-tetramethylpiperidin- 1-yl)oxyl (TEMPO) as a redox mediator for amidyl radical formation and an oxygen atom donor. The reactions are conducted under mild conditions using a simple setup and provide convenient access to functionalized oxazol-2-ones and imidazol-2-ones from readily available materials.
N - (4 - (3 - amino - 1 H - indazole - 4 - yl) phenyl) - N' - (2 - fluoro - 5 - methylphenyl) urea intermediate preparation method
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Paragraph 0152; 0154; 0155, (2018/03/02)
The invention provides a preparation method of N-(4-(3-amino-1H-indazol-4-yl) phenyl)-N'-(2-fluoro-5-methylphenyl) urea and an intermediate thereof. Specifically, the invention provides a preparation method of a borate ester compound as shown in a formula I, and the preparation method comprises the following steps: enabling a compound as shown in a formula III to react with a compound as shown in a formula IV to generate a compound as shown in a formula V, and enabling the compound as shown in the formula V to react with a boron reagent to generate the compound as shown in the formula I. The method has the characteristics of convenience in reaction, easiness in obtainment of the intermediate, high yield, high product purity of above 98.5%, low cost of raw materials and the like, and is suitable for industrial application.