376592-93-7

Basic information

• Product Name: 3''-AMINO-2''-HYDROXY-BIPHENYL-3-CARBOXYLIC ACID
• Synonyms: 3''-AMINO-2''-HYDROXY-BIPHENYL-3-CARBOXYLIC ACID;3'-Amino-2'-hydroxy-[1,1'-biphenyl]-3-carboxylic acid;Eltrombopag Intermediate 2;EltroMbopag I;3-(3-aMino-2-hydroxyphenyl)benzoic acid;[1,1'-Biphenyl]-3-carboxylic acid, 3'-aMino-2'-hydroxy-;3''-AMINO-2''-HYDROXY-BIPHENYL-3-CARBOXYLIC;Eltrombopag olamine Intermediate 1
• CAS NO: 376592-93-7
• Molecular Formula: C₁₃H₁₁NO₃
• Molecular Weight: 229.234
• EINECS: 1592732-453-0
• Mol File: 376592-93-7.mol
• Article Data: 17

Chemical Properties

• Melting Point: 222 °C(dec.)
• Boiling Point: 474.8±45.0 °C(Predicted)
• Appearance: /
• Density: 1.364
• Storage Temp.: Keep in dark place,Inert atmosphere,Room temperature
• Solubility: DMSO (Slightly), Methanol (Slightly, Heated)
• PKA: 3.99±0.10(Predicted)
• CAS DataBase Reference: 3''-AMINO-2''-HYDROXY-BIPHENYL-3-CARBOXYLIC ACID(CAS DataBase Reference)
• NIST Chemistry Reference: 3''-AMINO-2''-HYDROXY-BIPHENYL-3-CARBOXYLIC ACID(376592-93-7)
• EPA Substance Registry System: 3''-AMINO-2''-HYDROXY-BIPHENYL-3-CARBOXYLIC ACID(376592-93-7)

Safety Data

• Hazardous Substances Data: 376592-93-7(Hazardous Substances Data)

Usage

Uses

3’-Amino-2’-Hydroxy-[1,1’]Biphenyl-3-carboxylic Acid is used in the synthesis of monoethanolamine salts. A hydrazine cleavage product from Eltrombopag (E508000), an agonist of the Thrombopoietin (Tpo) receptor, used as treatment for thrombocytopenia

Upstream product

• 58349-02-3 4-bromo-2-iodo-6-nitrophenol 
• 7693-52-9 4-bromo-2-nitrophenol 
• 106-41-2 4-bromo-phenol 
• 106-48-9 4-chloro-phenol 
• 376591-94-5 2'-methoxy-3'-nitrobiphenyl-3-carboxylic acid 
• 95-85-2 2-hydroxy-5-chloro-aniline 
• 585-76-2 m-bromobenzoic acid 
• 64682-89-9 benzyl N-(2-hydroxyphenyl)carbamate 
• 56836-51-2 ethyl (2-hydroxyphenyl)carbamate 
• 88-75-5 2-hydroxynitrobenzene 
• 618-51-9 3-Iodobenzoic acid 
• 186663-74-1 tert-butyl (2-hydroxyphenyl)carbamate 

Downstream Products

• 376591-99-0 3’-{N’-[1-(3,4-dimethylphenyl)-3-methyl-5-oxo-1,5-di-hydropyrazol-4-ylidene]hydrazino}-2’-hydroxybiphenyl-3-carboxylic acid 
• 893736-72-6 2′-hydroxy[1,1-biphenyl]-3-carboxylic acid 

Relevant articles and documents

Preparation method of drug intermediate for treating idiopathic blood diseases

The invention provides a preparation method of a drug intermediate for treating idiopathic blood diseases, which comprises the following steps: by using 2'-hydroxy-3'-nitrobiphenyl-3-carboxylic acid as a starting material and adopting a hydrazine hydrate-iron-carrier reduction method, avoiding the conventional Pd/C hydrogenation reduction reaction conditions, and carrying out aftertreatment by regulating the pH value and filtering, and the operability of amplify production is strong. Compared with Pd/C, the price advantage of hydrazine hydrate is obvious, the material cost can be greatly reduced, and the method is very suitable for industrial production.

PROCESS FOR THE PREPARATION OF KEY INTERMEDIATES FOR THE SYNTHESIS OF ELTROMBOPAG OR SALT THEREOF

Object of the present invention is an improved process for the preparation of key intermediates for the synthesis of Eltrombopag, passing through/using intermediate 5'-Chloro-2'-hydroxy[1,1'-biphenyl]-3-carboxylic acid alkaline metal salt of formula: wherein A is an alkaline metal.

Synthetic method of eltrombopag intermediate and synthetic method of eltrombopag

The invention relates to the field of medicine synthesis, in particular to a synthesis method of an eltrombopag intermediate and a synthesis method of eltrombopag. The synthesis method of the eltrombopag intermediate comprises the following steps: mixing 2'-hydroxyl-3'-nitrobiphenyl-3-carboxylic acid or 5'-chloro-2'-hydroxyl-3'-nitrobiphenyl-3-carboxylic acid with an alkali, a catalyst and water,introducing hydrogen, and carrying out a hydrogenation reaction to form the eltrombopag intermediate. The synthesis steps are simplified, the generation of impurities is reduced, and the yield and purity are improved.