15075-50-0Relevant articles and documents
Network single ion conductors based on comb-branched polyepoxide ethers and lithium bis(allylmalonato)borate
Sun, Xiao-Guang,Kerr, John B.,Reeder, Craig L.,Liu, Gao,Han, Yongbong
, p. 5133 - 5135 (2004)
The synthesis of network single ion conductors to obtain single ion conductors with high ambient temperature conductivity and mechanical strength is discussed. The single ion conductors were based on comb-branched polyepoxide ethers and lithium (Li) bis(allylmelonato)borate. The single ion conductors possessed good mechanical strength due to the formation of network structure and the Li/Li symmetric cell cycling showed no concentration polymerization. The results show that the backbone structure of the polyepoxides contributes to the total ionic conductivity and it increases with the increasing side chain length.
Selectivity in reactions of allyl diazoacetates as a function of catalyst and ring size from γ-lactones to macrocyclic lactones
Doyle,Hu
, p. 8839 - 8847 (2000)
Catalytic reactions of diazoacetates tethered through zero, one, two, and three ethylene glycol units to an allyl group have been investigated for chemoselectivity, diastereoselectivity, and enantioselectivity. Results from cyclopropanation, carbon-hydrogen insertion, and oxonium ylide generation are compared from reactions of achiral and chiral catalysts of copper(I) and dirhodium(II) carboxylates and carboxamidates. Relative to results from intermolecular reactions of ethyl diazoacetate with allyl ethyl ether, intermolecular reactions show a diversity of selectivities including preference for the opposite configurational arrangement from the one preferred in corresponding intermolecular cyclopropanation reactions. Enantioselectivities for cyclopropanation are dependent on the catalyst ligands in a manner that reflects divergent trajectories of the carbon-carbon double bond to the reacting carbene center. Enantioselectivity increases as a function of ring size with chiral copper catalysts, but the reverse occurs with chiral dirhodium(II) carboxamidates. Mechanistic implications, including those related to the conformation of the reacting metal carbene, offer a new dimension to understanding of enantioselectivity in catalytic asymmetric cyclopropanation reactions.
Iterative Design and Optimization of Initially Inactive Proteolysis Targeting Chimeras (PROTACs) Identify VZ185 as a Potent, Fast, and Selective von Hippel-Lindau (VHL) Based Dual Degrader Probe of BRD9 and BRD7
Zoppi, Vittoria,Hughes, Scott J.,Maniaci, Chiara,Testa, Andrea,Gmaschitz, Teresa,Wieshofer, Corinna,Koegl, Manfred,Riching, Kristin M.,Daniels, Danette L.,Spallarossa, Andrea,Ciulli, Alessio
, p. 699 - 726 (2019/01/11)
Developing PROTACs to redirect the ubiquitination activity of E3 ligases and potently degrade a target protein within cells can be a lengthy and unpredictable process, and it remains unclear whether any combination of E3 and target might be productive for degradation. We describe a probe-quality degrader for a ligase-target pair deemed unsuitable: the von Hippel-Lindau (VHL) and BRD9, a bromodomain-containing subunit of the SWI/SNF chromatin remodeling complex BAF. VHL-based degraders could be optimized from suboptimal compounds in two rounds by systematically varying conjugation patterns and linkers and monitoring cellular degradation activities, kinetic profiles, and ubiquitination, as well as ternary complex formation thermodynamics. The emerged structure-activity relationships guided the discovery of VZ185, a potent, fast, and selective degrader of BRD9 and of its close homolog BRD7. Our findings qualify a new chemical tool for BRD7/9 knockdown and provide a roadmap for PROTAC development against seemingly incompatible target-ligase combinations.
TAU-PROTEIN TARGETING PROTACS AND ASSOCIATED METHODS OF USE
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Paragraph 1505, (2018/05/24)
The present disclosure relates to bifunctional compounds, which find utility as modulators of tau 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 tau protein, such that tau protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tau. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tau protein. Diseases or disorders that result from aggregation or accumulation of tau protein are treated or prevented with compounds and compositions of the present disclosure.
The silane compound surface modification material phosphorylcholine-
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Paragraph 0022, (2018/06/29)
PROBLEM TO BE SOLVED: To provide a novel compound serving as a surface modifying material for a high sensitivity biosensing element, which enables forming of a monomolecular film capable of inhibiting nonspecific adsorption of protein. SOLUTION: The compound is a phosphorylcholine-silane compound represented by chemical formula 1, wherein X1to X3each independently represent halogen, 1-3C alkoxy or 1-3C alkyl, provided that at least one of X1to X3is halogen or 1-3C alkoxy; R1represents -(CH2)m- or -(CH2CH2O)n-(CH2)2-; R2represents -(CH2)s- or -(CH2)3-(OCH2CH2)p-; m is an integer of 2-20, n is an integer of 1-5, s is an integer of 3-20, and p is an integer of 1-5. COPYRIGHT: (C)2013,JPOandINPIT
