877399-31-0

Basic information

• Product Name: tert-butyl 3-{[4-(tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl]methyl}azetidine-1-carboxylate
• Synonyms: tert-butyl 3-{[4-(tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl]methyl}azetidine-1-carboxylate;tert-Butyl 3-((4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)methyl)azetidine-1-carboxylate;(1-((1-(TERT-BUTOXYCARBONYL)AZETIDIN-3-YL)METHYL)-1H-PYRAZOL-4-YL)BORONIC ACID PINACOL ESTER
• CAS NO: 877399-31-0
• Molecular Formula: C₁₈H₃₀BN₃O₄
• Molecular Weight: 363.2595
• Mol File: 877399-31-0.mol

Chemical Properties

• Appearance: /
• Storage Temp.: under inert gas (nitrogen or Argon) at 2-8°C
• CAS DataBase Reference: tert-butyl 3-{[4-(tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl]methyl}azetidine-1-carboxylate(CAS DataBase Reference)
• NIST Chemistry Reference: tert-butyl 3-{[4-(tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl]methyl}azetidine-1-carboxylate(877399-31-0)
• EPA Substance Registry System: tert-butyl 3-{[4-(tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl]methyl}azetidine-1-carboxylate(877399-31-0)

Safety Data

• Hazardous Substances Data: 877399-31-0(Hazardous Substances Data)

Usage

Uses

Used in Pharmaceutical Industry:
tert-butyl 3-[4-(tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl]methylazetidine-1-carboxylate is used as a reactant for the preparation of pyrazole-substituted aminoheteroaryl compounds. These compounds are specifically designed to act as c-Metathesis protein kinase inhibitors, which are essential for combating cancer and other abnormal cell growth disorders. The development of such inhibitors is crucial in the pharmaceutical industry, as they can potentially lead to the creation of novel therapeutic agents that can effectively target and mitigate the growth of cancerous cells and other abnormal cellular processes.

Upstream product

• 877399-37-6 tert-butyl 3-((4-bromo-1H-pyrazol-1-yl)methyl)azetidine-1-carboxylate 
• 73183-34-3 bis(pinacol)diborane 
• 142253-57-4 3-methanesulfonyloxymethyl-azetidine-1-carboxylic acid tert-butyl ester 
• 142253-56-3 3-hydroxymethyl-azetidine-1-carboxylic acid tert-butyl ester 
• 269410-08-4 pyrazole-4-boronic acid pinacol ester 

Relevant articles and documents

Compounds used as JAK inhibitor, and use of compounds

The invention provides compounds used as a JAK inhibitor, and a use of the compounds, and concretely provides compounds (represented by formula (I)) with JAK inhibition activity or a stereoisomer, a geometric isomer, a tautomer, a racemate, a nitrogen oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and a medicinal composition including the compounds. The invention also discloses a use of the compounds or the medicinal composition thereof in the preparation of medicines used for treating autoimmune diseases or proliferative diseases.

Structure based drug design of crizotinib (PF-02341066), a potent and selective dual inhibitor of mesenchymal-epithelial transition factor (c-MET) kinase and anaplastic lymphoma kinase (ALK)

Because of the critical roles of aberrant signaling in cancer, both c-MET and ALK receptor tyrosine kinases are attractive oncology targets for therapeutic intervention. The cocrystal structure of 3 (PHA-665752), bound to c-MET kinase domain, revealed a novel ATP site environment, which served as the target to guide parallel, multiattribute drug design. A novel 2-amino-5-aryl-3-benzyloxypyridine series was created to more effectively make the key interactions achieved with 3. In the novel series, the 2-aminopyridine core allowed a 3-benzyloxy group to reach into the same pocket as the 2,6-dichlorophenyl group of 3 via a more direct vector and thus with a better ligand efficiency (LE). Further optimization of the lead series generated the clinical candidate crizotinib (PF-02341066), which demonstrated potent in vitro and in vivo c-MET kinase and ALK inhibition, effective tumor growth inhibition, and good pharmaceutical properties.

PYRAZOLE-SUBSTITUTED AMINOHETEROARYL COMPOUNDS AS PROTEIN KINASE INHIBITORS

Compounds of formula (1) are provided, as well as methods for their synthesis and use. Preferred compounds are potent inhibitors of the c-Met protein kinase, and are useful in the treatment of abnormal cell growth disorders, such as cancers.