28749-88-4Relevant articles and documents
TAU-PROTEIN TARGETING COMPOUNDS AND ASSOCIATED METHODS OF USE
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Paragraph 0704; 0705, (2021/02/12)
The present disclosure relates to bifunctional compounds, which find utility as modulators of tan protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tan protein, such that tan protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tan. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tan protein. Diseases or disorders that result from aggregation or accumulation of tan protein are treated or prevented with compounds and compositions of the present disclosure.
A polymer-supported chiral fluorinated dirhodium(II) complex for asymmetric amination of silyl enol ethers
Oohara, Tadashi,Nambu, Hisanori,Anada, Masahiro,Takeda, Koji,Hashimoto, Shunichi
supporting information, p. 2331 - 2338 (2012/11/13)
The immobilization of dirhodium(II) tetrakis[N-tetrafluorophthaloyl-(S)- tert-leucinate], [Rh2(S-TFPTTL)4], has been accomplished by copolymerization of a dirhodium(II) complex-containing monomer with styrene and 1,6-bis(4-vinylbenzyloxy)hexane as a flexible cross-linker. The polymer-supported chiral fluorinated dirhodium(II) complex catalyzed the amination of silyl enol ethers with [N-(2-nitrophenylsulfonyl)imino] phenyliodinane (NsN=IPh) to provide α-amino ketones in high yields with high levels of enantioselectivity and could be used up to 20 times as the catalyst readily withstood stirring in the presence of the solid reactant. Copyright
Process improvements in the synthesis of 2,4,5-trifluorobenzoic acid. selective hydrodefluorination of tetrafluorophthalimides
Fertel, Lawrence B.
, p. 111 - 115 (2013/09/08)
An improved preparation of the fluoroquinolone antibacterial intermediate 2,4,5-trifluorobenzoic acid is described. A combination of a selective hydrodefluorination and hydrolysis reaction of 3,4,5,6-tetrafluoro-N-methylphthalimide leading to 3,5,6-trifluorophthalic acid was key to the success of the process. In addition the development of a two-step, one-pot imidization/ halogen exchange from tetrachlorophthalic anhydride to 3,4,5,6-tetrafluoro-N-methylphthalimide in sulfolane solvent is detailed.