- Preparation method of Eltrombopag key intermediate 3'-amino-2'-hydroxybiphenyl-3-carboxylic acid
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The invention discloses a preparation method of an Eltrombopag key intermediate 3'-amino-2'-hydroxybiphenyl-3-carboxylic acid. The preparation method comprises the following steps: (1) nitrating o-bromophenol with a nitrating reagent by using water as a s
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Paragraph 0019; 0020
(2019/11/20)
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- Preparation method of 3'-nitro-2'-hydroxybiphenyl-3-formic acid
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The invention provides a preparation method of 3'-nitro-2'-hydroxybiphenyl-3-formic acid. The method uses 2-halogenated acrolein and nitromethane as starting raw materials, obtains 2-halo-4-nitro-n-butyraldehyde through an addition reaction, obtains 2-(3-
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Paragraph 0064-0065
(2019/11/29)
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- Synthetic method of eltrombopag intermediate
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The application discloses a synthetic method of an eltrombopag intermediate, comprising: subjecting 2-aminophenol derivative shown as formula (II) as a raw material to react with an aromatic reagent shown as formula (III) to obtain an intermediate product shown as formula (IV); using the intermediate product shown as formula (IV) as a raw material to prepare the eltrombopag intermediate shown as formula (I), wherein R1 is selected from amino derivatives, and R2 is selected from halogen and sulfonyloxy group. The synthetic method has few reaction steps; the starting material is simple; the synthetic method is simpler, more economical and greener.
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Paragraph 0063-0064
(2019/04/06)
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- Preparation method of eltrombopag
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The invention relates to the technical field of medicine manufacturing, and discloses a preparation method of eltrombopag. The preparation method comprises the following steps: 1, sequentially carrying out a continuous reaction on a starting material I, glacial acetic acid and hydrobromic acid until the reaction is completed to obtain an intermediate I; 2, reducing the intermediate I by hydrazinehydrate under catalytic action of palladium to obtain an intermediate II; and 3, carrying out diazotization addition on the intermediate II to obtain the eltrombopag. According to the method, nitryl is prevented from being directly reduced by hydrogen on the premise that the medicine quality is guaranteed, so that production can be safely amplified, and market competitiveness of the variety is improved.
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Paragraph 0020; 0024; 0025; 0029
(2019/12/25)
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- THROMBOPOIETIN ACTIVITY MODULATING COMPOUNDS AND METHODS
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Disclosed herein are substituted arylhydrazino compounds, pharmaceutical compositions comprising the same, methods of modulating the activity a thrombopoietin receptor using the same, methods of identifying compounds as thrombopoietin receptor modulators, and methods of treating disease by administering a compound of the invention to a patient in need thereof.
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Page/Page column 45; 155
(2010/11/08)
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- Regulated activation of cell-membrane receptors by metal-chelating agonists
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Invented is a regulated activation of cell-membrane receptors by small molecule agents. Also invented is a method to render a cell-membrane receptor responsive to the activation by small molecule compounds by specific single point mutations in the transmembrane region.
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- Thrombopoietin mimetics
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Invented are non-peptide TPO mimetics. Also invented are novel processes and intermediates used in the preparation of the presently invented compounds. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected hydroxy-1-azobenzene derivative.
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