1223404-88-3

Usage

Uses

Used in Pharmaceutical Industry:
(R)-5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-amine is used as a potential pharmaceutical candidate for the development of new therapeutic agents. Its unique structure and functional groups may contribute to its efficacy in treating various diseases or conditions, although further research is required to characterize its specific biological and pharmacological properties.
Used in Medicinal Chemistry Research:
In the field of medicinal chemistry, (R)-5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-amine serves as a valuable molecule for research into the discovery and optimization of new drugs. Its distinct chemical features may provide insights into the design of novel compounds with improved pharmacological profiles, potentially leading to the development of more effective and safer medications.

Upstream product

• 29274-24-6 5-chloropyrazolo[1,5-a]pyrimidine 
• 899819-34-2 (2,5-difluorophenyl)magnesium bromide 
• 2646-90-4 2,5-difluorobenzaldehyde 
• 1218935-60-4 (2R)-2-(2,5-difluorophenyl)pyrrolidine hydrochloride 
• 29274-22-4 4H,5H-pyrazolo[1,5-a]pyrimidine-5-one 
• 1919868-77-1 (R)-2-(2,5-difluorophenyl)-pyrrolidine (R)-2-hydroxy-succinate 
• 1919868-75-9 3-nitropyrazolo[1,5-a]pyrimidin-5(4H)-one 
• 1224944-43-7 sodium pyrazolo[1,5-a] pyrimidin-5-olate 
• 1218935-59-1 (R)-(+)-2-(2,5-difluorophenyl)pyrrolidine 
• 1443623-92-4 5-(2,5-difluorophenyl)-3,4-dihydro-2H-pyrrole 
• 399-94-0 2-bromo-1,4-difluorobenzene 
• 1363380-51-1 5-chloro-3-nitropyrazolo[1,5-a]pyrimidine 
• 1223404-90-7 (R)-5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)-3-nitropyrazolo[1,5-a]pyrimidine 

Downstream Products

• 1223403-62-0 (R)-1-(5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-(4-fluorophenyl)urea 
• 1223403-61-9 (R)-N-(5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxy-3-methylazetidine-1-carboxamide 
• 1223404-67-8 (1S,4S)-N-(5-((R)-2-(2.5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-2-oxa-5-azabicyclo[2.2.1]heptane-5-carboxamide 
• 1223403-58-4 (3S)-N-[5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidi n-3-yl]-3-hydroxypyrrolidine-1-carboxamide 
• 1223403-59-5 (3R,4R)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3,4-dihydroxypyrrolidine-1-carboxamide 
• 1223403-74-4 (R)-N-(5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-4-isopropylpiperazine-1-carboxamide 
• 1223403-60-8 (R)-N-(5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-methoxyazetidine-1-carboxamide 
• 1223403-43-7 (R)-1-tert-butyl-3-(5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)urea 
• 1223403-45-9 (R)-N-(5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)isobutyramide 
• 1223404-01-0 (R)-N-(5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)pivalamide 
• 1223404-82-7 (R)-methyl 2-(5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-ylamino)-2-oxoacetate 
• 1223403-85-7 (R)-methyl 1-(5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-ylcarbamoyl)cyclopropanecarboxylate 
• 1223404-13-4 (R)-N-(5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-1-(trifluoromethyl)cyclopropanecarboxamide 
• 1223404-33-8 (R)-N-(5-(2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)pyrimidine-2-carboxamide 

Relevant academic research and scientific papers

Assignment of NMR data and Conformational analysis of larotrectinib and its precursors

NMR experiments were used to identify the two main conformations of Larotrectinib and its synthetic precursor, the nitro compound 4. Conformational analysis by dynamic NMR was performed in different temperature and solvents, combining 2D EXSY and NOE expe

Preparation and application of protein receptor kinase inhibitor

The invention provides a preparation method of a protein receptor kinase inhibitor. Specifically, the invention discloses a compound as shown in a formula I or a stereoisomer or racemate or pharmaceutically acceptable salt thereof, and the definition of each group is as shown in the specification. The invention also discloses application of the compound as a TRK kinase inhibitor.

Carbamate compound, pharmaceutical composition and application of carbamate compound

The invention discloses a carbamate compound, a pharmaceutical composition and application of the carbamate compound and belongs to the technical field of pharmaceutical compound synthesis. The carbamate compound is a compound of a general formula I or ge

Pharmaceutical compound, composition and application thereof

The invention provides a novel compound, which shows biological activity and can be used as a TRK kinase inhibitor, such as drugs for treatment of TRK-mediated diseases or symptoms and for treatment and prevention of cancers, dermatitis or asthma and the like.

Synthesis method of Larotrectinib intermediate and Larotrectinib

The invention discloses a synthesis method of Larotrectinib and a Larotrectinib intermediate. N-Boc pyrrolidone and 2,5-difluorophenyl magnesium bromide serve as raw materials, an intermediate A-1 isprepared, the intermediate A-1 is subjected to chiral catalysis hydrogenation, cyclization or first cyclization and afterwards chiral catalysis hydrogenation to obtain a chiral pyrrodlidine intermediate A-4, the intermediate A-4 and an intermediate B-3 are condensed to obtain an intermediate AB-1, the intermediate AB-1 is reduced to obtain an intermediate AB-2, the AB-2 is acylated to obtain an intermediate AB-3, and the AB-3 is subjected to a substitution reaction to obtain the target product Larotrectinib (AB-4). The intermediate A-4 with a high yield and high chiral purity is obtained through a chiral catalysis method, the B-3 with a high yield is obtained through a solvent-free one-pot method, and the Larotrectinib (AB-4) with a high yield and high purity is obtained. According to themethod, the reaction condition can also be applied to large-scale preparation, the method is suitable for industrial production, and therefore, the method has high practical values and social and economic benefits.

SUBSTITUTED PYRAZOLOPYRIMIDINES USEFUL AS KINASES INHIBITORS

Disclosed are novel pyrzaolopyrimidines of Formula (I), their derivatives, pharmaceutically acceptable salts, solvates and hydrates thereof. The compounds have protein kinases inhibitory activities and are expected to be useful for the treatment of protei

METHODS OF TREATING PEDIATRIC CANCERS

A method of treating a pediatric cancer in a subject in need thereof. The method includes administering to the subject a therapeutically effective amount of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrro

SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS TRK KINASE INHIBITORS

Compounds of Formula (I) in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor.