1421312-33-5Relevant academic research and scientific papers
Preparation method of roxadustat intermediate
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, (2021/04/17)
The invention discloses a preparation method of a roxadustat intermediate. The method comprises the following steps: anhydride ring opening, esterification, ring closing, aromatization, deprotection, chlorination and methylation to obtain the roxadustat intermediate. According to the invention, the preparation method provided by the invention makes full use of the atom economy theory, is easy to operate, low in cost and low in pollution, and is suitable for large-scale industrial production; and only one-time refining is carried out, the chromatographic purity can reach 99.5% or above, and the total yield of the six-step reaction is 30% or above.
Method for preparing isoquinolinone compound
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Paragraph 0172-0174, (2021/04/21)
The invention provides a method for preparing an isoquinolinone compound. Specifically, the invention provides a method for preparing a compound as shown in a formula 3, which is characterized by comprising the following steps: 1) reacting a compound as shown in a formula 1 with acyl chloride to obtain a compound as shown in a formula 2; and 2) reacting the compound of the formula 2 with an aminolysis reagent selected from glycine, glycine derivatives, or a combination thereof, and then carrying out a hydrolysis reaction to obtain a compound of a formula 3. The method disclosed by the invention has the excellent technical effects of reasonable route, convenience, feasibility, high preparation yield and purity, suitability for industrial production and the like.
Preparation method of drug for chronic anemia
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, (2018/09/11)
The invention discloses a synthesis method for a drug Roxadustat for chronic anemia. The synthesis method comprises the following steps: hydrolyzing and acidifying a compound shown as a formula 6 under the action of alkali to obtain a key intermediate compound shown as a formula 7; carrying out condensation reaction on the compound shown as the formula 7 and carbonyl diimidazole under suitable conditions to obtain an intermediate compound shown as a formula 8, and separating or not separating the compound shown as the formula 8 from a system to directly take part in subsequent reaction; and finally, reacting the product with glycine to obtain a final product Roxadustat shown as a formula 9. The preparation method has the advantages that the route efficiency is improved, the process cost isreduced, side products are reduced and the purity of a final product is favorably improved (The formula is shown in the description), wherein R2 in the compound shown as the formula 6 represents alkyl, and includes but not limited to methyl, ethyl, isopropyl, tertiary butyl or benzyl.
Isoquinolone compound and application thereof
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Paragraph 0388-0391, (2018/09/08)
The invention relates to an isoquinolone compound and application thereof. The invention in particular relates to an isoquinolone compound used as a HIF prolyl hydroxylase inhibitor (HIF-PHI) and a pharmaceutical composition thereof. Moreover, the present invention provides the application of the isoquinolinone compound or the pharmaceutical composition thereof in the preparation of a medicament for preventing or treating HIF-associated or HIF-mediated diseases as anemia or ischemia, local ischemia or hypoxia.
CRYSTAL TYPES OF COMPOUNDS INHIBITING ACTIVITY OF PROLYL HYDROXYLASE AND USE THEREOF
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Paragraph 0145; 0157; 0158, (2017/10/27)
The invention relates to crystal types of compound shown as structural formula I, methods of preparing the compound, intermediate, pharmaceutical composition, and use of treating disease or pharmaceutical preparations for treating disease.
POLYMORPHIC FORMS OF COMPOUNDS AS PROLYL HYDROXYLASE INHIBITOR, AND USES THEREOF
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Paragraph 0149, (2015/02/19)
The present invention relates to the polymorphic forms of the compound of Formula (I), preparation thereof including the preparation of intermediates and pharmaceutical compositions, and use of a polymorph above in the treatment of a disease, a disorder o
POLYMORPHIC FORMS OF COMPOUNDS AS PROLYL HYDROXYLASE INHIBITOR, AND USES THEREOF
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Page/Page column 17, (2013/03/26)
The present invention relates to the polymorphic forms of the compound of Formula (I), preparation thereof including the preparation of intermediates and pharmaceutical compositions, and use of a polymorph above in the treatment of a disease, a disorder o
