55899-12-2

Upstream product

• 626-60-8 3-Chloropyridine 
• 773-64-8 2-mesitylenesulphonyl chloride 
• 36016-40-7 mesitylenesulfonylhydroxylamine 
• 36016-39-4 N-(tert-butoxycarbonyl)-O-(mesitylsulfonyl)hydroxylamine 

Downstream Products

• 1167056-15-6 C₉H₇ClN₂O₂ 
• 1167055-86-8 C₉H₇ClN₂O₂ 
• 1449307-43-0 (3-chloropyridin-1-ium-1-yl)(tosyl)amide 

Relevant academic research and scientific papers

Regioselective Synthesis of Pyrazolo[1,5- a]pyridine via TEMPO-Mediated [3 + 2] Annulation-Aromatization of N-Aminopyridines and α,β-Unsaturated Compounds

A TEMPO-mediated [3 + 2] annulation-aromatization protocol for the preparation of pyrazolo[1,5-a]pyridines from N-aminopyridines and α,β-unsaturated compounds was developed. The procedure offered multisubstituted pyrazolo[1,5-a]pyridines in good to excellent yield with high and predictable regioselectivity. The modification of marketed drugs including Loratadine, Abiraterone, and Metochalcone, and a one-pot three-step gram scale synthesis of key intermediate for the preparation of Selpercatinib were demonstrated. Mechanism studies show that TEMPO serves both as a Lewis acid and as an oxidant.

SUBSTITUTED 1,5-NAPHTHYRIDINES OR QUINOLINES AS ALK5 INHIBITORS

The present disclosure provides inhibitors of activin receptor-like kinase 5 (ALK5). Also disclosed are methods to modulate the activity of ALK5 and methods of treatment of disorders mediated by ALK5.

Structure-kinetics relations holding in the amination of six-membered nitrogen-containing heterocyclic compounds

Relative rates of the amination of 3-X- and 4-X-substituted pyridines (X = H, 3-Me, 4-Me, 3-F3C, 3-CN, 4-CN, 3-Cl, 3-Br, 4-MeO, 4-Me 2N), pyrazine, quinoline, isoquinoline, 2,2′- and 4,4′-bipyridines, and 1,10-phenanthroline with O-

Structure-activity relationship study of EphB3 receptor tyrosine kinase inhibitors

A structure-activity relationship study for a 2-chloroanilide derivative of pyrazolo[1,5-a]pyridine revealed that increased EphB3 kinase inhibitory activity could be accomplished by retaining the 2-chloroanilide and introducing a phenyl or small electron donating substituents to the 5-position of the pyrazolo[1,5-a]pyridine. In addition, replacement of the pyrazolo[1,5-a]pyridine with imidazo[1,2-a]pyridine was well tolerated and resulted in enhanced mouse liver microsome stability. The structure-activity relationship for EphB3 inhibition of both heterocyclic series was similar. Kinase inhibitory activity was also demonstrated for representative analogs in cell culture. An analog (32, LDN-211904) was also profiled for inhibitory activity against a panel of 288 kinases and found to be quite selective for tyrosine kinases. Overall, these studies provide useful molecular probes for examining the in vitro, cellular and potentially in vivo kinase-dependent function of EphB3 receptor.

Pyrazolopyridine-4-Yl Pyridazinone Derivatives and Addition Salts Thereof, and Pde Inhibitors Comprising the Same Derivatives or Salts as Active Ingredient

Novel pyrazolopyridine-4-yl pyridazinone derivatives serve as phosphodiesterase inhibitors and are useful compounds for use in pharmaceutical products. Specifically, the compounds of the present invention are pyrazolopyridine-4-yl pyridazinone derivatives represented by the following general formula (1): (Example: 6-(2-ethyl-7-methoxy-pyrazolo[1,5-a]pyridine-4-yl)-5-methyl-4, 5-dihydro-3(2H)-pyridazinone).