1421312-32-4Relevant articles and documents
Preparation method of roxadustat intermediate
-
Paragraph 0056; 0062; 0067; 0073; 0078; 0084, (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.
Preparation method of drug for chronic anemia
-
Paragraph 0055-0058, (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.
CRYSTAL TYPES OF COMPOUNDS INHIBITING ACTIVITY OF PROLYL HYDROXYLASE AND USE THEREOF
-
Paragraph 0145; 0155; 0156, (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
-
Paragraph 0148, (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
-
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