40359-46-4Relevant academic research and scientific papers
HEMIAMINAL-TAG FOR PROTEIN LABELING AND PURIFICATION
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Page/Page column 15; 16, (2018/06/30)
The invention pertains to the synthesis, isolation, and characterization of hemiaminal for selective labeling of peptides, proteins, antibodies, and organic fragments with -C(=0) CH2NH2 and derivatives with -CH2NH2 group over -C(=0) CHRNH2 group (where R≠H). The invention also pertains to the method of single-site immobilization of proteins through N-terminus Gly on solid phase. The invention includes late-stage tagging of N-terminus Gly with an affinity tag, 19F NMR probe, and a fluorophore and a method for metal-free protein purification and isolation of analytically pure proteins.
5-AMINO-4-CARBAMOYL-PYRAZOLE COMPOUNDS AS SELECTIVE AND IRREVERSIBLE T790M OVER WT-EGFR KINASE INHIBITORS AND USE THEREOF????
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Paragraph 0396, (2016/03/13)
Disclosed are compounds of Formula (I), pharmaceutical compositions comprising the same, processes for the preparation thereof, and the use thereof.
Efficient preparation of medium ring oxygen heterocycles
Nishiguchi, Atsuko,Ikemoto, Tomomi,Ito, Tatsuya,Miura, Shotaro,Tomimatsu, Kiminori
, p. 445 - 452 (2008/02/09)
We achieved efficient preparation of medium ring oxygen heterocycles (1), 1-benzoxepines and 1-benzoxocines, by applying intramolecular Claisen-type condensation in dialkyl carbonate with metal alcoholate. Furthermore, we accomplished the preparation of 2
Discovery and optimisation of potent, selective, ethanolamine inhibitors of bacterial phenylalanyl tRNA synthetase
Jarvest, Richard L.,Erskine, Symon G.,Forrest, Andrew K.,Fosberry, Andrew P.,Hibbs, Martin J.,Jones, Joanna J.,O'Hanlon, Peter J.,Sheppard, Robert J.,Worby, Angela
, p. 2305 - 2309 (2007/10/03)
High throughput screening of Staphylococcus aureus phenylalanyl tRNA synthetase (FRS) identified ethanolamine 1 as a sub-micromolar hit. Optimisation studies led to the enantiospecific lead 64, a single-figure nanomolar inhibitor. The inhibitor series shows selectivity with respect to the mammalian enzyme and the potential for broad spectrum bacterial FRS inhibition.
Efficient combination of task-specific ionic liquid and microwave dielectric heating applied to one-pot three component synthesis of a small library of 4-thiazolidinones
Fraga-Dubreuil, Joan,Bazureau, Jean Pierre
, p. 6121 - 6130 (2007/10/03)
The first report of the use of task-specific ionic liquid as synthetic equivalent of ionic liquid-phase matrice for the preparation of a small library of 4-thiazolidinones is reported in this paper. The starting (ethyleneglycol)ionic liquid-phase is funct
Process for producing cyclic compound
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, (2008/06/13)
A process suitable for safely mass-producing, through a short step, cyclic compounds useful in medicines, agricultural chemicals, foods, cosmetics, and chemical products or as intermediates therefor. The process, which is for producing a compound represen
Grafted ionic liquid-phase-supported synthesis of small organic molecules
Fraga-Dubreuil, Joan,Bazureau, Jean Pierre
, p. 6097 - 6100 (2007/10/03)
The preparation and applications in the Knoevenagel and 1,3-dipolar cycloaddition reactions of new grafted soluble liquid phases derived from imidazolium ionic liquids are described. Good yields and high regioselectivity are the features observed with these unconventional liquid phases.
Catalytic Cyclophanes. Part VIII. Cytochrome P-450 Activity of a Porphyrin-Bridged Cyclophane
Benson, David R.,Valentekovich, Robert,Tam, Suk-Wah,Diederich, Francois
, p. 2034 - 2060 (2007/10/02)
Following a known synthetic procedure, the porphyrin-cyclophane 1 having a porphyrin attached by two straps to an apolar cyclophane binding site was prepared.Upon metallation, the ZnII and FeIII derivatives 2 and 3, respectively, were obtained in good yields.Treatment of 3 with base yielded the μ-oxo dimer 4 in which the two oxo-bridged porphyrins moieties are both capped by cyclophane binding sites.All compounds 1-4 are freely soluble in protic solvents such as MeOH and CF3CH2OH, and the FIII derivatives 3 and 4 are active cytochrome P-450 mimics in these protic environments.Strong inclusion complexation of polycyclic aromatic hydrocarbons by 1 and 3 in alcoholic solvents was observed and quantified by 1H-NMR and UV/VIS titrations.Acenaphthylene binds in an 'equatorial' orientation which locates its reactive 1,2-double bond near the porphyrin center, whereas phenanthrene binds 'axially' with the reactive 9,10-double bond oriented away from the porphyrin.The reduction potential of 3 was not significantly altered by substrate binding.In the unbound form, the FeIII center in porphyrin 3 was found by ESR and 1H-NMR to prefer a high-spin state (S = 5/2).In CF3CH2OH, using iodosylbenzene as O-transfer agent, the FeIII derivative 3 catalyzed the oxidation of acenaphthylene to acenaphthen-1-one (14).Phenanthrene inhibited the reaction, possibly as a result of strong but nonproductive binding.Under similar conditions, isotetralin (18) was aromatized with high turnover to 1,4-dihydronaphthalene.The μ-oxo dimer 4 also showed high catalytic activity in the oxidation of acenaphthylene in MeOH, a result which provides strong evidence for efficient supramolecular catalysis.Due to as yet unknown reaction channels leading to polymeric products, poor mass balances were generally obtained in the oxidations effected in MeOH and CF3CH2OH in the presence of PhIO.
Leukotriene-B4 derivatives, process for their production and their use as pharmaceutical agents
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, (2008/06/13)
The invention relates to leukotriene-B4 derivatives of formula I, STR1 in which n=1-10, R1 means radical CH2 OH, radical COOR4, radical CONHR5 or radical CONR6 R7, A means a cis,
