1000025-07-9Relevant articles and documents
MANUFACTURING PROCESS FOR 3,5-DICHLOROPICOLINONITRILE FOR SYNTHESIS OF VADADUSTAT
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, (2022/01/12)
Disclosed herein are methods and processes of preparing vadadustat or a pharmaceutically acceptable salts thereof, and intermediates (e.g., a compound of Formula (I), (I-F), (II), or (IV), or a pharmaceutically acceptable salts thereof) useful for the syn
Development of a Robust and Scalable Process for the Large-Scale Preparation of Vadadustat
Lin, Biyue,Kou, Jingping,Wu, Shuming,Cai, Xuerong,Xiao, Qingbo,Li, Yinglong,Hu, Jian,Li, Jianbing,Wang, Zhongqing
, p. 960 - 968 (2021/04/05)
A novel and scalable process is developed for the industrial synthesis of vadadustat. The four-step process is one step shorter compared to the reported routes with an increase in total yield to 49.1%. Detailed optimizations furnish vadadustat with a purity of >99.5% through cross-coupling, aromatic substitution and nitrile hydrolysis, amidation, and ester-ether deprotection. The process is also robust and was demonstrated in a kilogram laboratory. Meanwhile, the corresponding impurity profile was thus studied in detail and well documented.
Preparation method of valduxostat and intermediate thereof
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Paragraph 0067-0076, (2021/09/15)
The invention relates to a preparation method of valduxostat and an intermediate thereof, and belongs to the field of medicinal chemistry. The preparation method comprises the following steps: taking 3-chloro-5-(3-chlorphenyl)-2-cyanopyridine as a starting material, carrying out hydrolysis reaction, and then carrying out condensation reaction to obtain a compound, namely the intermediate; and further reacting the intermediate compound to obtain vadadustat. The method has the advantages of short route, simple and easily available raw materials, low cost and mild reaction conditions, and is suitable for industrial large-scale production.
NOVEL CRYSTALLINE COMPOUND OF VADADUSTAT
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Page/Page column 11, (2021/12/31)
The present invention relates to a novel crystalline compound of Vadadustat, to processes for its preparation, to pharmaceutical compositions containing it and to its use in therapy.
Preparation method of pyridine cyclic compound
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Paragraph 0041; 0054-0057; 0064-0065, (2020/06/16)
The invention provides a preparation method of a pyridine cyclic compound, and belongs to the field of pharmaceutical chemicals. The method comprises the steps: mixing 3,5-dihydroxypicolinic acid, concentrated sulfuric acid and an alcohol solvent, and performing esterification reaction to obtain 3,5-dihydroxypicolinic acid methyl ester; then sequentially carrying out protection group feeding and ammoniation to obtain {[5-(3-chlorphenyl)-3-hydroxypyridin-2-yl]amino}acetic acid. The product produced by the method has the characteristics of high purity, high yield, low cost, simple operation andstable process.
Preparation method and application of phenylpyridine compound
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Paragraph 0039; 0059-0066, (2020/07/28)
The invention relates to a preparation method and application of a phenylpyridine compound, and belongs to the field of pharmaceutical chemicals. The method disclosed by the invention comprises the following steps: mixing 5-(3-chlorphenyl)-2-cyano-3-chloropyridine, alkali and an organic solvent to obtain 5-(3-chlorphenyl)-3-hydroxyl-pyridine formamide; and then sequentially carrying out a reactionwith sulfuric acid and glycine so as to obtain {[5-(3-chlorphenyl)-3-hydroxypyridine-2-yl] amino} acetic acid. The product produced by the method is high in purity, high in yield, low in process cost, simple to operate and stable in process.
Preparation method and application of picolinamide
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, (2020/07/12)
The invention provides a preparation method of a picolinamide compound, and belongs to the field of pharmaceutical and chemical industry. According to the preparation method, 3,5-dihydroxypicolinic acid methyl ester, hydroxylamine hydrochloride, an alkali
Preparation method of vadadustat
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Paragraph 0047; 0060-0065, (2020/04/02)
The invention provides a preparation method of vadadustat, and belongs to the field of pharmaceutical chemical industry. The method comprises the following steps: mixing 3,5-dichloro-2-picolinic acid,methanol and sulfuric acid at a certain temperature, and carrying out a reaction to obtain 3,5-dichloro-2-picolinic acid methyl ester; adding 3-chlorophenylboronic acid, and carrying out a catalyticreaction to obtain 5-(3-chlorphenyl)-3-chloropyridine-methyl formate; and adding glycine into the 5-(3-chlorphenyl)-3-chloropyridine-methyl formate, and carrying out a reaction to obtain the 5-(3-chlorphenyl)-3-chloropyridine-methyl formate. The method has the characteristics of high product purity, high yield, low cost, simple operation and stable process.
Preparation method of vardoxostat intermediate
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Paragraph 0057-0059, (2020/11/12)
The invention relates to a preparation method of a vardoxostat intermediate, and belongs to the field of medicinal chemistry. The preparation method comprises the following steps: taking 3-methoxy-5-(3-chlorphenyl)-2-cyanopyridine as a starting material, carrying out hydrolysis reaction and condensation reaction to obtain an intermediate of a compound; the intermediate compound can be subjected toa further reaction to obtain vadustat (vardoxostat); the method has the advantages of short route, simple and accessible raw materials, lower cost and mild reaction conditions, and is suitable for industrial large-scale production.
PROCESS FOR PREPARING 2-[[5-(3-CHLOROPHENYL)-3-HYDROXYPYRIDINE-2-CARBONYL]AMINO]ACETIC ACID
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Paragraph 0071, (2019/11/28)
Disclosed herein are methods and processes of preparing vadadustat and pharmaceutically acceptable salts thereof, and intermediates of formula (I) and their salts useful for the synthesis of vadadustat.