Vadadustat

Base Information

• Chemical Name: Vadadustat
• CAS No.: 1000025-07-9
• Molecular Formula: C14H11ClN2O4
• Molecular Weight: 306.705
• Mol file: 1000025-07-9.mol

Synonyms:Vadadustat

Chemical Property of Vadadustat

Chemical Property:

• Boiling Point: 674.6±55.0 °C(Predicted)
• PKA: 4.09±0.40(Predicted)
• PSA: 99.52000
• Density: 1.461±0.06 g/cm3(Predicted)
• LogP: 2.31290
• Storage Temp.: Hygroscopic, -20°C Freezer, Under inert atmosphere
• Solubility.: DMSO (Slightly), Methanol (Slightly)

Purity/Quality:

99% ^*data from raw suppliers

Vadadustat ^*data from reagent suppliers

Safty Information:

• Pictogram(s):  
• Hazard Codes: 

MSDS Files:

SDS file from LookChem

Useful:

• Description: Vadadustat is an inhibitor of hypoxia-inducible factor prolyl hydroxylase 2 (HIF-PH2) and HIF-PH3 (IC50s = 1.1 and 0.39 micromolar, respectively). It stabilizes HIF-1α in mouse hepatocyte nuclear extracts. Vadadustat (50 and 100 mg/kg) increases erythropoietin levels in mouse serum.
• Uses: Vadadustat is a novel HIF (Hypoxia-inducible factor) stabilizer. It provides an effective anemia treatment in nondialysis-dependent chronic kidney disease.

Technology Process of Vadadustat

There total 31 articles about Vadadustat which guide to synthetic route it. The literature collected by LookChem mainly comes from the sharing of users and the free literature resources found by Internet computing technology. We keep the original model of the professional version of literature to make it easier and faster for users to retrieve and use. At the same time, we analyze and calculate the most feasible synthesis route with the highest yield for your reference as below:

synthetic route:

Reference yield: 100.0%

methyl [5-(3-chlorophenyl)-3-hydroxy-2-pyridinecarboxamido]acetate → {[5-(3-chloro-phenyl)-3-hydroxy-pyridine-2-carbonyl]-amino}-acetic acid (1000025-07-9)

Guidance literature:

With water; potassium hydroxide; In 2-methyltetrahydrofuran; at 20 - 30 ℃; for 3h; Inert atmosphere;

Reference yield: 98.9%

N-[5-(3-chlorophenyl)-3-methoxypyridine-2-carbonyl]glycine → {[5-(3-chloro-phenyl)-3-hydroxy-pyridine-2-carbonyl]-amino}-acetic acid (1000025-07-9)

Guidance literature:

With hydrogen bromide; at 95 ℃; for 28h; Green chemistry;

Reference yield: 90.2%

5-(3-chlorophenyl)-3-hydroxy-picolinic acid methyl ester + glycine (56-40-6,18875-39-3,25718-94-9) → {[5-(3-chloro-phenyl)-3-hydroxy-pyridine-2-carbonyl]-amino}-acetic acid (1000025-07-9)

Guidance literature:

With sodium ethanolate; In methanol; at 75 ℃; Reagent/catalyst; Inert atmosphere;

upstream raw materials:

3-chlorophenylboronic acid

2-Cyano-3,5-dichloropyridine

5-(3-chlorophenyl)-3-chloro-2-cyanopyridine

5-(3-chlorophenyl)-3-methoxy-2-cyanopyridine

Refernces

• 1、 -. "NOVEL CRYSTALLINE COMPOUND OF VADADUSTAT". Page/Page column 11. . Retrieved 2021/12/31.
• 2、 -. "Preparation method of valduxostat and intermediate thereof". . . Retrieved 2021/09/15.