951888-61-2

Upstream product

• 63082-45-1 4-fluoro-2-methylbenzaldehyde 
• 452-63-1 2-Bromo-5-fluorotoluene 
• 95-92-1 oxalic acid diethyl ester 

Downstream Products

• 1011463-77-6 ethyl 2-(4-fluoro-2-methyl-5-nitrophenyl)-2-oxoacetate 
• 1208864-74-7 C₂₆H₂₆F₇N₃O₃ 

Relevant academic research and scientific papers

Divergent Photocatalytic Reactions of α-Ketoesters under Triplet Sensitization and Photoredox Conditions

The long-lived triplet excited states of transition metal photocatalysts can activate organic substrates via either energy- or electron-transfer pathways, and the rates of these processes can be influenced by rational tuning of the reaction conditions. The characteristic reactive intermediates generated, however, are distinct and can exhibit very different reactivity patterns. This mechanistic diversity available to photocatalytic reactions might thus offer an opportunity to engineer divergent reactions that give markedly different chemical outcomes under superficially similar conditions. Herein, we show that the photocatalytic reactions of benzoylformate esters with alkenes can be directed toward either Paternò-Büchi cycloadditions or allylic functionalization reactions under conditions favoring energy transfer or electron transfer, respectively. These studies provide a framework for designing other divergent photocatalytic methods that produce different sets of reaction outcomes under photoredox and triplet sensitization conditions.

Discovery of novel 2-(3-phenylpiperazin-1-yl)-pyrimidin-4-ones as glycogen synthase kinase-3β inhibitors

We herein describe the results of further evolution of glycogen synthase kinase (GSK)-3β inhibitors from our promising compounds containing a 2-phenylmorpholine moiety. Transformation of the morpholine moiety into a piperazine moiety resulted in potent GSK-3β inhibitors. SAR studies focused on the phenyl moiety revealed that a 4-fluoro-2-methoxy group afforded potent inhibitory activity toward GSK-3β. Based on docking studies, new hydrogen bonding between the nitrogen atom of the piperazine moiety and the oxygen atom of the main chain of Gln185 has been indicated, which may contribute to increased activity compared with that of the corresponding phenylmorpholine analogues. Effect of the stereochemistry of the phenylpiperazine moiety is also discussed.

KINASE INHIBITORS USEFUL FOR THE TREATMENT OF PROLIFERATIVE DISEASES

The present invention relates to novel kinase inhibitors and modulator compounds useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferrably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.