863605-35-0

Upstream product

• 154258-82-9 3-(4-fluorophenyl)-1H-pyrazole 
• 74-88-4 methyl iodide 
• 454662-11-4 C₈H₉FN₂ 
• 107-06-2 1,2-dichloro-ethane 
• 75175-77-8 3-(dimethylamino)-1-(4-fluorophenyl)prop-2-en-1-one 
• 403-42-9 1-(4-fluorophenyl)ethanone 
• 57056-43-6 3-bromo-1-(4-fluorophenyl)propan-1-one 
• 462-06-6 fluorobenzene 

Downstream Products

• 1383377-50-1 3-fluoro-4-(3-(4-fluorophenyl)-1-methyl-1H-pyrazol-4-yl)-picolinonitrile 
• 1286230-78-1 3-(4-fluorophenyl)-1-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole 
• 863605-34-9 4-bromo-3-(4-fluorophenyl)-1-methyl-1H-pyrazole 

Relevant academic research and scientific papers

Cascade reaction to 1H-pyrazoles from hydrazones via sodium Ni-trite promoted dual C–C/C–N formation, annulation and aromatization with 1,2-dichloroethane

A novel route for tandem C–C/C–N formation, annulation and aromatization of hydrazones with 1,2-dichloroethane to synthesize 1H-pyrazoles has been developed. Furthermore, the 1,2-dichloroethane serves as alkylation reagent in good to excellent yields. This methodology features mild reaction conditions and good functional group tolerance, providing a direct approach for the preparation of 1H-pyrazoles.

Synthesis of novel fluorophenylpyrazole-picolinamide derivatives and determination of their anticancer activity

A series of fluorophenylpyrazole-picolinamide derivatives were synthesized in high yields using a cross-coupling reaction catalyzed by in situ formed palladium-N-heterocyclic carbenes (Pd-NHCs). The synthesized novel derivatives were evaluated for in vitro anticancer activity against a panel of four human tumor cell lines, HeLa (cervical), A-549 (lung), MCF-7 (breast), and IMR-32 (neuroblastoma). Four compounds, 11c, 11e, 11j, and 11k, showed growth inhibition (low μM) comparable with the standard drug cisplatin, providing a preliminary structure–activity relationship for the series. The present procedure is operationally simple and works with a wide range of substrates and may thus be useful in further compound optimization.

Transformation of arenes into 3-arylpyrazoles and 3-arylisoxazolines with β-bromopropionyl chloride, hydrazine, and hydroxylamine

Successive treatment of arenes with β-bromopropionyl chloride and AlCl3, followed by the reactions with hydrazines and Na2CO3, and then with MnO2 gave the corresponding 3-arylpyrazoles in one pot in good to moderate yields. The same successive treatment of arenes with β-bromopropionyl chloride and AlCl3, followed by the reactions with hydroxylamine and KF gave the corresponding 3-arylisoxazolines in one pot in good to moderate yields.

KINASE INHIBITORS

ABSTRACT The present invention provides kinase inhibitors of Formula I: .