570406-98-3

Basic information

• Product Name: AKR-501
• Synonyms: AKR-501;1-[3-Chloro-5-[[[4-(4-chloro-2-thienyl)-5-(4-cyclohexyl-1-piperazinyl)-2-thiazolyl]amino]carbonyl]-2-pyridinyl]-4-piperidinecarboxylic acid;1-[3-Chloro-5-[[4-(4-chlorothiophen-2-yl)-5-(4-cyclohexylpiperazin-1-yl)thiazol-2-yl]carbamoyl]-2-pyridyl]piperidine-4-carboxylic acid;AS 1670542;E 5501;4-Piperidinecarboxylic acid, 1-[3-chloro-5-[[[4-(4-chloro-2-thienyl)-5-(4-cyclohexyl-1-piperazinyl)-2-thiazolyl]amino]carbonyl]-2-pyridinyl]-;Avatrombopag(AS1670542);Crenolanib Besylate
• CAS NO: 570406-98-3
• Molecular Formula: C29H34Cl2N6O3S2
• Molecular Weight: 649.67
• EINECS: 1312995-182-4
• Product Categories: Intermediate
• Mol File: 570406-98-3.mol
• Article Data: 6

Chemical Properties

• Appearance: /
• Density: 1.440
• PKA: 3.04±0.70(Predicted)
• CAS DataBase Reference: AKR-501(CAS DataBase Reference)
• NIST Chemistry Reference: AKR-501(570406-98-3)
• EPA Substance Registry System: AKR-501(570406-98-3)

Safety Data

• Hazardous Substances Data: 570406-98-3(Hazardous Substances Data)

Usage

Description

Avatrombopag is a medication that used for certain conditions that lead to thrombocytopenia (low platelets) such as thrombocytopenia associated with chronic liver disease in adults who are to undergo a planned medical or dental procedure.It was the third thrombopoietin receptor agonist approved for the treatment of immune thrombocytopenia and the first approved to treat periprocedural thrombocytopenia in patients with chronic liver disease (thereby providing an alternative to blood transfusions for these patients). Avatrombopag was approved for medical use in the United States in 2018, and in the European Union in 2019.

Upstream product

• 570403-14-4 ethyl 1-(3-chloro-5-{[4-(4-chlorothiophen-2-yl)-5-(4-cyclohexylpiperazin-1-yl)thiazol-2-yl]carbamoyl}pyridin-2-yl)piperidine-4-carboxylate 
• 2161380-87-4 5-bromo-4-(4-chlorothiophen-2-yl)-2-aminothiazole 
• 570407-10-2 4-(4-chlorothiophen-2-yl)-1,3-thiazol-2-amine 
• 128094-80-4 4-bromo-2-(2-bromoethyl)butanoic acid 
• 17766-28-8 cyclohexylpiperazine 
• 570407-42-0 4-(4-chloro-2-thienyl)-5-(4-cyclohexyl-1-piperazinyl)-2-thiazolamine 
• 931395-73-2 6-(4-(ethoxycarbonyl)piperidin-1-yl)-5-chloropyridine-3-carboxylic acid 
• 41667-95-2 5,6-dichloronicotinic acid 
• 1126-09-6 4-carbethoxypiperidine 
• 41668-11-5 6-amino-5-chloro-pyridine-3-carboxylic acid 
• 128094-81-5 methyl 4-bromo-2-(2-bromoethyl)butanoate 

Relevant articles and documents

Preparation method of avatrombopag

The invention discloses a preparation method of avatrombopag (avatrombopag), which comprises the following steps: by using 6-amino-5-chloro-3-picolinic acid as an initial raw material, sequentially carrying out amidation and cyclization reactions to obtain the target product avatrombopag. The preparation process has the advantages of easily available raw materials, rapidness, convenience, economyand environmental protection, especially overcomes the problems of poor dichloro selectivity and the like in the existing process raw materials, and is suitable for large-scale industrial production.

POLYMORPHIC FORMS OF AVATROMBOPAG MALEATE

The present invention relates generally to pharmaceutically active compounds and more specifically to crystalline Form M1 of Avatrombopag, crystalline Form M2 of Avatrombopag, crystalline Form M3 of Avatrombopag, crystalline Form M4 of Avatrombopag, crystalline Form M5 of Avatrombopag, crystalline Form M1 of Avatrombopag maleate, crystalline Form M2 of Avatrombopag maleate, crystalline Form M3 of Avatrombopag maleate, amorphous Avatrombopag, amorphous Avatrombopag maleate, amorphous solid dispersions of Avatrombopag maleate and processes for the preparation thereof.

2-ACYLAMINOTHIAZOLE COMPOUND CRYSTALS

The purpose of the present invention is to provide crystals of 1-(3-chloro-5-{[4-(4-chlorothiophen-2-yl)-5-(4-cyclohexyl piperazin-1-yl) thiazol-2-yl] carbamoyl} pyridin-2-yl) piperidine-4-carboxylic acid maleic acid salt that can ensure constant quality and constant effects as a drug substance for medicines, and that can be stably supplied in mass production such as industrial production. The present invention relates to crystals of 1-(3-chloro-5-{[4-(4-chlorothiophen-2-yl)-5-(4-cyclohexyl piperazin-1-yl) thiazol-2-yl] carbamoyl} pyridin-2-yl) piperidine-4-carboxylic acid maleic acid salt with endothermic peak top temperatures in differential scanning calorimeter analysis of between approximately 229 and 232 degree C, and between approximately 300 and 303 degree C. The crystals of the present invention are with excellent oral absorption, can be stably supplied in mass production such as industrial production or the like, and can be used as an active ingredient in a pharmaceutical composition for preventing and/or treating various types of thrombocytopenia.