259248-35-6

Upstream product

• 326-62-5 2-fluorophenyl acetonitrile 
• 67-56-1 methanol 
• 259248-36-7 methyl 2-cyano-2-(2-fluorophenyl) acetate 
• 57486-67-6 methyl o-fluorophenylacetate 
• 616-38-6 carbonic acid dimethyl ester 

Downstream Products

• 144616-11-5 2-(2-fluorophenyl)propanedioic acid 
• 1263089-47-9 1,3-bis(4-nitrophenyl) 2-(2-fluorophenyl)propanedioate 
• 1263089-46-8 1,3-bis(2,4,6-trichlorophenyl) 2-(2-fluorophenyl)propanedioate 
• 1263486-06-1 1-[(2-chloro-5-thiazolyl)methyl]-3-(2-fluorophenyl)-2-oxido-9-methyl-4-oxo-4H-pyrido[1,2-a]pyrimidinium 

Relevant academic research and scientific papers

Ring closure strategy leads to potent RIPK3 inhibitors

Necroptosis is a form of regulated necrotic cell death that is independent of caspases. Receptor-interacting protein kinase 3 (RIPK3) has been identified as a key regulator for necroptosis, and has been proposed as a potential therapeutic target for the treatment of diseases associated with necroptosis. In this report, we describe the design, synthesis, and evaluation of a series of novel RIPK3 inhibitors. The lead compound 38 exhibited potent activity (EC50 = 0.42 μM) in blocking TNFα, Smac mimetic and z-VAD (TSZ) induced cell death in HT-29 cells. Mechanistic studies showed that compound 38 bound to RIPK3 with high affinity (Kd = 7.1 nM), and inhibited RIPK3 kinase activity in a ADP-Glo functional assay. In addition, compound 38 displayed good selectivity over another necroptosis regulator RIPK1 (Kd = 6000 nM). Furthermore, compound 38 demonstrated excellent in vitro safety profiles with minimal inhibition of CYP isozymes and hERG potassium channel. Lastly, compound 38 efficiently blocked hypothermia and death in mice in the TNFα-induced systemic inflammatory response syndrome model.

HETEROARYL COMPOUNDS AS INHIBITORS OF PROGRAMMED NECROSIS PATHWAY, COMPOSITION AND METHOD USING THE SAME

The present disclosure provides heteroaryl compounds of Formula (I), processes for their preparation, pharmaceutical compositions containing them, and their use in the treatment of diseases and disorders, arising from or related to the programmed necrosis pathway.

Gold(I)-Catalyzed Enantioselective Desymmetrization of 1,3-Diols through Intramolecular Hydroalkoxylation of Allenes

A gold(I)-catalyzed enantioselective desymmetrization of 1,3-diols was achieved by intramolecular hydroalkoxylation of allenes. The catalyst system 3-F-dppe(AuCl)2 /(R)-C8-TRIPAg proved to be specifically efficient to promote the desymmetrizing cyclization of 2-aryl-1,3-diols, which have proven challenging substrates in previous reports. Multisubstituted tetrahydrofurans were prepared in good yield with good enantioselectivity and diastereoselectivity by this method.

MESOIONIC PESTICIDES

Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein (Formula 1) X is O or S; Y is O or S; A is O, S, NR3e or C(R3c)=C(R3d); Z is a direct bond, O, S(O)n,191, NR6, C(R7/sup

Microbial asymmetric decarboxylation of fluorine-containing arylmalonic acid derivatives

α-Methyl-α-(trifluoromethylphenyl)malonic acids have been incubated with Alcaligenes bronchisepticus to afford optically active α-arylpropionic acids.Generally, the chemical and optical yields of the reaction products were higher when the substituents on the aromatic ring were strongly electron-withdrawing.Decarboxylation of α-fluoro-α-phenylmalonic acid with the aid of the same bacterium afforded optically active α-fluoro-α-phenylacetic acid.