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Preparation method of eltrombopag with stable performance

A kind of Eltrombopag and stable technology, applied in the field of Eltrombopag preparation, can solve the problems of many reaction steps, high cost, high environmental protection pressure, etc., and achieve the effect of easy availability of raw materials, high product yield and high product purity

Inactive Publication Date: 2021-06-25
HANGZHOU HUANGSEN BIOLOGICAL TECH CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0011] Analyzing the disclosed preparation methods of Eltrombopag and its intermediates, there are generally disadvantages such as many reaction steps, high environmental protection pressure, and high cost. Therefore, a simpler, more convenient, environmentally friendly and cost-controllable process route is sought. The economic and technological development of medicine is very important

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  • Preparation method of eltrombopag with stable performance
  • Preparation method of eltrombopag with stable performance
  • Preparation method of eltrombopag with stable performance

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Embodiment Construction

[0049] A method for preparing Eltrombopag with stable performance, adding 3'-amino-2'-hydroxybiphenyl-3-carboxylic acid (II) (2.29g, 10mmol) and 50mL of 1N hydrochloric acid into a reaction flask, stirring and dissolving . Add 25mL aqueous solution of sodium nitrite (0.76g, 11mmol) dropwise under ice bath, after dropping, add ethyl acetoacetate (1.63g, 12.5mmol) and sodium acetate (8.2g, 0.1mol) ethanol 75mL solution under stirring , raised to room temperature, and reacted for 10 hours, and TLC detected that the reaction was complete. Filtration, the crude product was recrystallized with methanol to obtain a light yellow solid (Z)-2-[3'-(2'-hydroxy-3-carboxylic acid biphenyl)hydrazono]-3-oxobutanoic acid ethyl ester (III ) 2.7g, yield 73.0%;

[0050] At room temperature, add 3,4-dimethylphenylhydrazine (0.75 g, 5.5 mmol) and glacial acetic acid (25 mL) into the reaction flask, and stir to dissolve. Add (Z)-2-[3'-(2'-hydroxyl-3-carboxybiphenyl)hydrazono]-3-oxobutanoic acid e...

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Abstract

The invention discloses a preparation method of eltrombopag with stable performance, which comprises the following steps: adding 3 '-amino-2'-hydroxybiphenyl-3-carboxylic acid (II) and hydrochloric acid into a reaction box, stirring and dissolving; dropwise adding a sodium nitrite aqueous solution under an ice bath, adding an ethanol solution containing ethyl acetoacetate and sodium acetate under stirring after dropwise adding, heating to room temperature, reacting for 10 hours, and completing TLC (Thin Layer Chromatography) detection reaction; and filtering, and recrystallizing the crude product with methanol to obtain an intermediate (Z)-2-[3'- (2'- hydroxy-3-carboxylic acid biphenyl) hydrazono ]-3-oxobutanoate (III), and carrying out condensation cyclization reaction on the intermediate (III) and 3, 4-dimethylphenylhydrazine to obtain Eltrombopag (I).

Description

technical field [0001] The invention belongs to the technical field of organic synthesis route design and preparation of raw materials and intermediates, and in particular relates to a preparation method of Eltrombopag with stable performance. Background technique [0002] Eltrombopag (Eltrombopag) is an oral thrombopoietin drug developed by GlaxoSmithKline. Produces a signaling cascade that induces the proliferation and differentiation of bone marrow megakaryocytes. The drug was approved by the U.S. Food and Drug Administration (FDA) for marketing in the U.S. in November 2008. It is used for the treatment of chronic idiopathic thrombocytopenic purpura ( Thrombocytopenia in patients with ITP). The trade name is Promacta. Eltrombopag is the first oral non-peptide thrombopoietin receptor agonist approved for the treatment of adults with chronic ITP, and its approval for the treatment of ITP patients is an important milestone. Currently, the drug is still undergoing clinica...

Claims

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Application Information

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IPC IPC(8): C07D231/46
CPCC07D231/46
Inventor 姚红罗瑾
Owner HANGZHOU HUANGSEN BIOLOGICAL TECH CO LTD
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