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

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

Uses

Used in Chronic Liver Disease:
AKR-501 is used as a treatment for thrombocytopenia associated with chronic liver disease in adults who are to undergo a planned medical or dental procedure. It helps increase platelet count, reducing the need for blood transfusions and improving patient outcomes.
Used in Immune Thrombocytopenia:
AKR-501 is also used for the treatment of immune thrombocytopenia, a condition where the immune system mistakenly attacks and destroys platelets. As a thrombopoietin receptor agonist, it stimulates the production of platelets, helping to alleviate symptoms and improve platelet count in affected patients.

Upstream product

• 128094-80-4 4-bromo-2-(2-bromoethyl)butanoic acid 
• 128094-81-5 methyl 4-bromo-2-(2-bromoethyl)butanoate 
• 41668-11-5 6-amino-5-chloro-pyridine-3-carboxylic acid 
• 1126-09-6 4-carbethoxypiperidine 
• 41667-95-2 5,6-dichloronicotinic acid 
• 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 
• 17766-28-8 cyclohexylpiperazine 
• 570407-10-2 4-(4-chlorothiophen-2-yl)-1,3-thiazol-2-amine 
• 2161380-87-4 5-bromo-4-(4-chlorothiophen-2-yl)-2-aminothiazole 
• 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 

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.

Preparation method of Avatrombopag

The invention discloses a preparation method of Avatrombopag. The preparation method comprises the following steps: sequentially carrying out cyclization, amidation, hydrolysis and other reactions byusing 6-amino-5-chloro-3-pyridylbenzoic acid as an initial raw material to obtain the target product Avatrombopag. The preparation process has the advantages of easily available raw materials, rapidness, convenience, economy and 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.

Preparation method of thrombocyte increasing agent

The invention relates to a preparation method of a thrombocyte increasing agent. The preparation method comprises the following steps: enabling a midbody 1 and a midbody 2 to perform amidation in the presence of a catalyst in an aprotic solvent; and adding alkali into a solvent of a midbody A to perform the alkaline hydrolysis reaction to obtain a target compound. The midbody 2 is firstly synthesized and then reacts with the midbody 1; and a synthetic route of the method is a converging reaction, so that the yield is increased, and convenience in quality control is achieved. In addition, by studying the reaction amplification feasibility, the operation such as column chromatography is avoided, the method is more suitable for an industrialized production process, and the emission of waste liquid is reduced. A product obtained by the route is high in purity, the yield is high, the pollution is small, and the preparation method is suitable for the industrialized production.

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.

2-ACYLAMINOTHIAZOLE DERIVATIVE OR SALT THEREOF

A 2-acylaminothiazole derivative or a pharmaceutically acceptable salt thereof having an excellent effect of proliferating human c-mpl-Ba/F3 cells and an activity of increasing platelets based on the effect of promoting the formation of megakaryocytic colonies. A compound or a pharmaceutically acceptable salt thereof useful in treating thrombocytopenia.