2-aminoethanol;3-[(5E)-5-[[2-(3,4-dimethylphenyl)-5-methyl-3-oxo-1H-pyrazol-4-yl]hydrazinylidene]-6-oxocyclohexa-1,3-dien-1-yl]benzoic acid

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 2-aminoethanol;3-[(5E)-5-[[2-(3,4-dimethylphenyl)-5-methyl-3-oxo-1H-pyrazol-4-yl]hydrazinylidene]-6-oxocyclohexa-1,3-dien-1-yl]benzoic acid
• 化学式: C29H36N6O6
• 分子量: 564.6
• InChiKey: TYYXAUPVEKKAFG-HTQZHWFGSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.65
• 重原子数：
  41
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.24
• 拓扑面积：
  204
• 氢给体数：
  7
• 氢受体数：
  11

文献信息

• Preparation process of an agonist of the thrombopoietin receptor
  申请人：Esteve Química, S.A.

  公开号：EP2799425A1

  公开（公告）日：2014-11-05

  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 (C1-C4)-alkyl ester thereof in the presence of Pd(OAc)2, tricyclohexylphosphine, 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.

  它涉及到2'-(苄氧基)-3'-硝基-1,1'-联苯-3-羧酸或其盐的制备过程，包括在Pd(OAc)2、三环己基膦、碱、适当溶剂和适当温度下，将2-(苄氧基)-1-溴-3-硝基苯与3-羧基苯硼酸或其盐或其(C1-C4)烷基酯之一反应；如适当，将得到的化合物提交给水解反应；通过加入酸，将得到的化合物以化合物式(VI)的盐形式或自由酸形式分离出来。它还包括从所得的新中间体中进一步制备厄洛替尼或其盐，方法是通过连续还原硝基团和去保护酚基，将获得的胺中间体转化为重氮衍生物，然后（1）与乙酰乙酸乙酯和（3,4-二甲基苯基）肼或其盐反应，通过分子间环化形成吡唑环，或者（2）通过与1-(3,4-二甲基苯基)-3-甲基-3-吡唑啉-5-酮反应引入吡唑环。
• [EN] PREPARATION PROCESS OF AN AGONIST OF THE THROMBOPOIETIN RECEPTOR<br/>[FR] PROCÉDÉ DE PRÉPARATION D'UN AGONISTE DU RÉCEPTEUR DE LA THROMBOPOÏÉTINE
  申请人：ESTEVE QUÍMICA S A

  公开号：WO2014177517A1

  公开（公告）日：2014-11-06

  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 (C1-C4)-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.

  这段文字描述了2'-(苄氧基)-3'-硝基-1,1'-联苯-3-羧酸或其盐的制备过程，包括在Pd(OAc)2、三环己基膦、一种碱、适当的溶剂和适当的温度下，将2-(苄氧基)-1-溴-3-硝基苯与3-羧基苯硼酸或其盐或其(C1-C4)烷基酯之一反应；如适当，将得到的化合物提交给水解反应；通过加入酸，以化合物的盐的形式或自由酸的形式分离得到的化合物，其为化合物的公式(VI)的盐或自由酸形式。它还包括从所得的新中间体中进一步制备厄洛替尼或其盐，方法为随后还原硝基团并去保护酚基，将获得的胺中间体转化为重氮衍生物，然后(1)与乙酰乙酸乙酯和(3,4-二甲基苯基)肼或其盐反应，通过分子间环化发生吡唑环形成，或者(2)通过与1-(3,4-二甲基苯基)-3-甲基-3-吡唑啉-5-酮反应引入吡唑环。
• PHARMACEUTICAL COMPOSITION COMPRISING ELTROMBOPAG OLAMINE, REDUCING SUGAR, AND POLYMERIC BINDER
  申请人：Alfred E. Tiefenbacher (GmbH & Co. KG)

  公开号：EP3409272A9

  公开（公告）日：2019-01-16

  The present invention relates to a pharmaceutical tablet composition comprising eltrombopag olamine, one or more reducing sugars, and one or more polymeric binder agents, a production process therefore, a pharmaceutical tablet composition comprising eltrombopag olamine, one or more reducing sugars, and one or more polymeric binder agents obtainable by the production process, a use / method of use of the pharmaceutical tablet compositions in the treatment or prophylaxis of immune (idiopathic) thrombocytopenic purpura (ITP), thrombocytopenia and/or acquired severe aplastic anaemia (SAA).

  本发明涉及一种药物片剂组合物，该组合物包含艾曲波帕乙醇胺、一种或多种还原糖和一种或多种高分子粘合剂；一种生产工艺；一种药物片剂组合物，该组合物包含艾曲波帕乙醇胺、一种或多种还原糖、一种药用片剂组合物在治疗或预防免疫性（特发性）血小板减少性紫癜（ITP）、血小板减少症和/或获得性严重再生障碍性贫血（SAA）中的用途/使用方法。
• PHARMACEUTICAL TABLET COMPOSITION COMPRISING ELTROMBOPAG OLAMINE
  申请人：Alfred E. Tiefenbacher (GmbH & Co. KG)

  公开号：EP3395331A1

  公开（公告）日：2018-10-31

  The present invention relates to a pharmaceutical tablet composition comprising eltrombopag olamine and one or more reducing sugars, a production process therefore, a pharmaceutical tablet composition comprising eltrombopag olamine and one or more reducing sugars obtainable by the production process, a use / method of use of the pharmaceutical tablet compositions in the treatment or prophylaxis of immune (idiopathic) thrombocytopenic purpura (ITP), thrombocytopenia and/or acquired severe aplastic anaemia (SAA).

  本发明涉及一种包含艾曲波帕乙醇胺和一种或多种还原糖的药用片剂组合物、一种生产工艺、一种包含艾曲波帕乙醇胺和一种或多种还原糖的药用片剂组合物、药用片剂组合物在治疗或预防免疫性（特发性）血小板减少性紫癜（ITP）、血小板减少症和/或获得性重型再生障碍性贫血（SAA）中的用途/使用方法。
• [EN] NOVEL CRYSTALLINE FORM OF ACETYLATED ELTROMBOPAG AND PREPARATION METHOD THEREOF<br/>[FR] NOUVELLE FORME CRISTALLINE D'ELTROMBOPAG ACÉTYLÉ ET SON PROCÉDÉ DE PRÉPARATION<br/>[ZH] 乙酰化艾曲波帕的新晶型及其制备方法
  申请人：SUNSHINE LAKE PHARMA CO LTD

  公开号：WO2021078076A1

  公开（公告）日：2021-04-29

  乙酰化艾曲波帕的新晶型及其制备方法，属于药物化学领域。所述晶型具有较好的稳定性有利于储存、转移、生产工艺中操作，其能够在动物体内能良好释放，可以用于制备成制剂。