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    • 3. 发明授权
    • Selective halogenation of 2-fluoroaniline
    • 2-氟苯胺的选择性卤化
    • US4443631A
    • 1984-04-17
    • US340569
    • 1982-01-18
    • Amphlett G. Padilla
    • Amphlett G. Padilla
    • C07C85/24
    • Novel processes for making arylpropionic acids are described. One process comprises carboxylating particular Grignard compounds which are the products of a catalyzed reaction between corresponding arylmagnesium bromides and ethylene. Furthermore, the reaction making the particular Grignard compounds is itself novel. Also, an improved method is disclosed for making coupled aryl compounds useful as intermediates for making compounds having a pharmaceutical use. For example, particular biaryls may be used to make some of the Grignard compounds herein from which the arylpropionic acids are made. Finally, an improved bromination is disclosed giving high yields of 4-bromo-2-fluoroaniline, which is thereafter coupled with benzene, then used to make the arylmagnesium bromide reacted with ethylene to obtain the particular Grignard compound and subsequent desired arylpropionic acid, i.e. 2-(2-fluoro-4-biphenylyl)propionic acid.
    • 描述了制备芳基丙酸的新方法。 一种方法包括羧化特定的格氏化合物,其是相应的芳基溴化镁和乙烯之间的催化反应的产物。 此外,使特定格利雅化合物的反应本身是新颖的。 此外,公开了一种改进的制备偶联芳基化合物的方法,其用作制备具有药物用途的化合物的中间体。 例如,特定的联芳基可以用于制备一些本文的格利雅化合物,其中制备芳基丙酸。 最后,公开了改进的溴化,得到高产量的4-溴-2-氟苯胺,然后与苯偶联,然后用于使芳基溴化镁与乙烯反应,得到特定的格利雅化合物和随后所需的芳基丙酸,即2 - (2-氟-4-联苯基)丙酸。