1224944-43-7

Upstream product

• 874-14-6 1,3-dimethyluracil 
• 1225387-53-0 3⁽⁵⁾-aminopyrazole 
• 1820-80-0 3-aminopyrazole 

Downstream Products

• 29274-22-4 4H,5H-pyrazolo[1,5-a]pyrimidine-5-one 
• 1224943-35-4 5-amino-pyrazolo[1,5-a]pyrimidine-3-carboxylic acid [3-(3-chloro-phenyl)-1H-pyrazol-4-yl]-amide 
• 1224942-21-5 5-amino-pyrazolo[1,5-a]pyrimidine-3-carboxylic acid [5-(3-chloro-phenyl)-isoxazol-4-yl]-amide 
• 1224942-28-2 5-aminopyrazolo[1,5-a]pyrimidine-3-carboxylic acid [3-(3-chlorophenyl)isoxazol-4-yl]amide 
• 1224942-33-9 5-amino-pyrazolo[1,5-a]pyrimidine-3-carboxylic acid [4-(3-chloro-phenyl)-2-methylthiazol-5-yl]-amide 
• 1919868-75-9 3-nitropyrazolo[1,5-a]pyrimidin-5(4H)-one 
• 1363380-51-1 5-chloro-3-nitropyrazolo[1,5-a]pyrimidine 
• 2135871-21-3 phenyl (5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-3,3a-dihydropyrazolo[1,5-a]pyrimidin-3-yl)carbamate 
• 1223405-08-0 (S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate 
• 1223404-88-3 5-[(2R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidin-3-amine 
• 1224939-87-0 5-(3-chlorobenzylamino)-N-cyclohexylpyrazolo[1,5-a]pyrimidine-3-carboxamide 
• 1224942-12-4 5-amino-pyrazolo[1,5-a]pyrimidine-3-carboxylic acid [2-(3-trifluoromethyl-phenyl)-2H-pyrazol-3-yl]-amide 
• 1224944-88-0 5-chloro-N-(1-(3-(trifluoromethyl)phenyl)-1H-pyrazol-5-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide 
• 1224942-11-3 5-amino-pyrazolo[1,5-a]pyrimidine-3-carboxylic acid (3-o-tolyl-isoxazol-4-yl)-amide 

Relevant academic research and scientific papers

Clean process for preparing larotinib intermediate

The invention discloses a clean process for preparing a larotinib intermediate, belonging to the field of organic synthesis. Key technical points of the invention are as follows: the clean process comprises the following steps: step 1, preparing a Vilsmeier reagent from a non-phosphorus reagent and N,N-dimethylformamide in an aprotic organic solvent; step 2, adding 5-hydroxy-6-nitropyrrole[1,5-a]pyrimidine into the Vilsmeier reagent prepared in the step 1, and carrying out a chlorination reaction; step 3, after the chlorination reaction is finished, adding water into a reaction system, separating a product from the reaction system, and carrying out filtering, washing and drying; and step 4, layering a filtrate, and recovering an organic layer for reuse. According to the invention, the yield of the obtained larotinib intermediate is high; discharging of a phosphorus waste liquid can be completely eradicated for an original process; and the environment is protected.

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

CRYSTALLINE FORM OF (S)-N-(5-((R)-2-(2,5-DIFLUOROPHENYL)-PYRROLIDIN-1-YL)-PYRAZOLO[1,5-A]PYRIMIDIN-3-YL)-3-HYDROXYPYRROLIDINE-1-CARBOXAMIDE HYDROGEN SULFATE

A novel crystalline form of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide, pharmaceutical compositions containing said crystalline form and the use of said crystalline form in the treatment of pain, cancer, inflammation, neurodegenerative disease or Trypanosoma cruzi infection are disclosed. In some embodiments, the novel crystalline form comprises a stable polymorph of (S)—N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)-pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide hydrogen sulfate. The present invention is further directed to a process for the preparation of the novel crystalline form.

PYRAZOLOPYRIMIDINE JAK INHIBITOR COMPOUNDS AND METHODS

The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R7 and Z are defined herein, a pharmaceutical composition that includes a compound of Formula Ia and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a JAK kinase activity in a patient.

Discovery of potent and selective pyrazolopyrimidine Janus kinase 2 inhibitors

The discovery of somatic Jak2 mutations in patients with chronic myeloproliferative neoplasms has led to significant interest in discovering selective Jak2 inhibitors for use in treating these disorders. A high-throughput screening effort identified the p

PYRAZOLOPYRIMIDINE JAK INHIBITOR COMPOUNDS AND METHODS

The invention provides JAK kinase inhibitors of Formula Ia, enantiomers, diasteriomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R7 and Z are defined herein, a pharmaceutical composition that includes a compound of Formula Ia and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a JAK kinase activity in a patient. Ia