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    • 1. 发明申请
    • PREPARATION PROCESS OF AN AGONIST OF THE THROMBOPOIETIN RECEPTOR
    • 血小板生成素受体激动剂的制备方法
    • WO2014177517A1
    • 2014-11-06
    • PCT/EP2014/058610
    • 2014-04-28
    • ESTEVE QUÍMICA, S.A.GALCHIMIA, S.A.
    • BARTRA SANMARTÍ, MartíSOLSONA ROCABERT, Joan GabrielCRUCES COLADO, JacoboENJO BABIO, JuanPAMPÍN CASAL, María Begoña
    • C07C205/59C07C201/12C07D231/22C07C227/04C07C249/16
    • C07C201/12C07C205/59C07C227/04C07C249/16C07D231/22C07C229/70C07C251/76
    • It relates to a preparation process of 2'-(benzyloxy)-3'-nitro-1,1'-biphenyl-3- carboxylic acid or a salt thereof comprising reacting 2-(benzyloxy)-1-bromo- 3-nitrobenzene with a either 3-carboxyphenylboronic acid or a salt thereof or a (C 1 -C 4 )-alkyl ester thereof in the presence of Pd(OAc) 2 , tricydohexylphosphine, a base, an appropriate solvent, and at an appropriate temperature; if appropriate, submitting the compound thus obtained to a hydrolysis reaction; and isolating the compound thus obtained in form of a salt of compound of formula (VI) or in form of the free acid by adding an acid. It also comprises the further preparation to eltrombopag or its salts from the new intermediate thus obtained by subsequent reduction of the nitro group and deprotection of the phenol, conversion of the amine intermediate obtained in a diazonium derivative, and either (1) subsequent reaction with ethyl acetoacetate and with (3,4-dimethylphenyl)hydrazine or a salt thereof, occurring the pyrazole ring formation by intermolecular cyclization, or (2) introduction of the pyrazole ring by reaction with 1-(3,4-dimethylphenyl)-3-methyl-3-pyrazolin-5-one.
    • 本发明涉及2' - (苄氧基)-3'-硝基-1,1'-联苯-3-甲酸或其盐的制备方法,其包括使2-(苄氧基)-1-溴-3-硝基苯与 在Pd(OAc)2,三羟基己基膦,碱,适当的溶剂和适当的温度存在下,3-羧基苯基硼酸或其盐或其(C 1 -C 4) - 烷基酯; 如果合适,将由此获得的化合物提交至水解反应; 并通过添加酸分离由式(VI)化合物的盐形成的化合物或游离酸形式的化合物。 它还包括通过随后还原硝基和脱保护苯酚得到的新中间体进一步制备埃曲波帕或其盐,以及在重氮衍生物中获得的胺中间体的转化,以及(1)随后的反应与乙基 乙酰乙酸酯和(3,4-二甲基苯基)肼或其盐,通过分子间环化形成吡唑环,或(2)通过与1-(3,4-二甲基苯基)-3-甲基 -3-吡唑啉-5-酮。