6890-60-4Relevant academic research and scientific papers
ANTIBIOTIC COMPOUNDS
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Page/Page column 175; 176, (2018/03/25)
The present invention relates to antibiotic compounds of formula (I), to compositions containing these compounds and to methods of treating bacterial diseases and infections using the compounds. The compounds find application in the treatment of infection with, and diseases caused by, Gram-positive and/or Gram-negative bacteria, and in particular in the treatment of infection with, and diseases caused by, Neisseria gonorrhoeae.
NOVEL MORPHOLINE DERIVATIVE OR SALT THEREOF
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Paragraph 0970-0972, (2016/07/05)
There is provided a morpholine derivative represented by General Formula [1A] or a salt thereof. (In the formula, a ring A represents a ring represented by General Formula [I]; * represents a bonding position; Z2 represents CH or the like; Z1 represents CR6 or the like; R6 represents a hydrogen atom or the like; X1 represents CHR7 or the like; R7 represents a hydrogen atom or the like; X2 represents CH2 or the like; R1 and R2 are the same as or different from each other, and each of R1 and R2 represents a hydrogen atom or the like; R3, R4, and R5 are the same as or different from each other, and each of R3, R4, and R5 represents a hydrogen atom, NRaRb, or the like; and each of Ra and Rb represents a hydrogen atom, a C1-8 alkyl group which may have a substituent, or the like.)
Pyridine to aniline: An exceptional biologically driven rearrangement
Arnauld, Thomas,Beaumal, Jean-Yves,Lefoulon, Francois,Petit, Alain,Renaud, Tristan
supporting information, p. 2217 - 2219 (2013/04/23)
During the course of our study on the innovative ligand for nicotinic acetylcholinergic receptors, LNAChR, and in order to assess activity and toxicity profiles of the drug's metabolites, synthesis of the main metabolites was undertaken. This synthesis work was done in parallel by organic chemistry and by biotransformation of LNAChR. Filamentous fungus Aspergillus alliaceus (NRRL 315) neatly afforded three of the main metabolites, one of which arose from a very unexpected and very uncommon rearrangement.
Substituent effects on the catalytic activity of bipyrrolidine-based iron complexes
Olivo, Giorgio,Lanzalunga, Osvaldo,Mandolini, Luigi,Di Stefano, Stefano
supporting information, p. 11508 - 11512 (2013/12/04)
The catalytic activity and the selectivity of the new bipyrrolidine-based Fe(II) complexes 2·Fe(OTf)2 and 3·Fe(OTf)2 in the oxidation of a series of alkyl and alkenyl hydrocarbons as well as of an aromatic sulfide with H2O2 were tested and compared with the catalytic efficiency of White's parent complex 1·Fe(OTf)2 in order to evaluate the sensitivity of the reaction to electronic effects.
PYRIMIDINE DERIVATIVES AND THEIR USE AS MODULATORS OF FGFR ACTIVITY
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Page/Page column 54-55, (2009/06/27)
There is provided pyrimidine compounds of formula 1: or pharmaceutical salts thereof. There is al so provided processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy, for exampl e in the treatment of proliferative disease such as cancer and particular ly in disease mediated by a FGFR inhibitory effect.
Chiral amine-imine ligands based on trans-2,5-disubstituted pyrrolidines and their application in the palladium-catalyzed allylic alkylation
Chen, Hongfeng,Sweet, James A.,Lam, Kin-Chung,Rheingold, Arnold L.,McGrath, Dominic V.
scheme or table, p. 1672 - 1682 (2009/12/04)
A series of amine-imine bidentate ligands based on a trans-2,5-disubstituted pyrrolidine and pyridine moieties have been prepared. The use of these ligands in the palladium-catalyzed allylic alkylation reaction of rac-(E)-1,3-diphenylprop-2-enyl acetate is reported. The results suggest that these ligands are good catalyst precursors for the reaction. Electronic modification on the pyridine ring of the ligands does not have a significant effect on the enantioselectivity of the reaction but does on the reaction rate, while structural modification on either the pyridine or the pyrrolidine moiety affords dramatic changes on the outcome of the stereochemistry. Evidence from various studies suggested that during the palladium-catalyzed allylic alkylation reaction, nucleophilic attack onto the 1,3-diphenylallyl moiety in the transition state occurs mainly trans to the pyridine ring of the less stable conformation of the palladium complexes.
Equilibrium of acyl transfer between pyridine N-oxides and their acylonium salts
Rubachenko,Schroeder,Chotii,Kovalenko,Red'ko,Lenska
, p. 1241 - 1246 (2008/12/22)
Transfer of acyl groups from N-acyloxypyridinium salts to pyridine N-oxides in acetonitrile was studied. The equilibrium constants of acyl exchange were determined. These quantities vary in the range covering eight orders of magnitude, depending on the st
Synthesis and antiviral activity evaluation of some novel acyclic C-nucleosides
Lougiakis, Nikolaos,Marakos, Panagiotis,Poul, Nicole,Balzarini, Jan
scheme or table, p. 775 - 780 (2009/06/25)
The preparation of novel 5-amino or 7-hydroxy substituted pyrazolo[4,3-b]pyridine and pyrazolo[3,4-c]pyridine acyclic C-nucleosides is described. Their synthesis was carried out by condensation of suitably substituted lithiated picolines with 2-benzyloxyethoxymethylchloride followed by pyrazole ring annulation. The compounds were evaluated for their antiviral activity against a wide panel of viruses, but were found inactive at subtoxic concentrations.
The synthesis of the new C-nucleoside 6-deazaformycin B
Korouli, Stella,Lougiakis, Nikolaos,Marakos, Panagiotis,Pouli, Nicole
, p. 181 - 184 (2008/09/21)
The synthesis of the 6-deaza analogue of formycin B is described, through the condensation of lithiated 4-methoxy-2-methyl-3-trifluoroacetamidopyridine with a suitably protected ribonolactone, dehydration of the resulting hemiacetal, reduction and subsequent ring closure followed by protecting group manipulation. Georg Thieme Verlag Stuttgart.
Resonance Raman investigation of equatorial ligand donor effects on the CU2O22+ core in end-on and side-on μ-peroxo-dicopper(II) and bis-μ-oxo-dicopper(III) complexes
Henson, Mark J.,Vance, Michael A.,Zhang, Christiana Xin,Hong-Chang, Liang,Karlin, Kenneth D.,Solomon, Edward I.
, p. 5186 - 5192 (2007/10/03)
The effect of endogenous donor strength on CU2O2 bonds was studied by electronically perturbing [{(R-TMPA)CuII}2(O2)]2+ and [{(R-MePY2)Cu}2(O2)]2+ (R = H, MeO, Me2N), which form the end-on μ-1,2 bound peroxide and an equilibrium mixture of side-on peroxo- dicopper(II) and bis-μ-oxo-dicopper(III) isomers, respectively. For [{(R-TMPA)CUII}2(O2)]2+, vo-o shifts from 827 to 822 to 812 cm-1 and VCu-O(sym) shifts from 561 to 557 to 551 cm-1, respectively, as R- varies from H to MeO to Me2N. Thus, increasing the N-donor strength to the copper decreases peroxide π*σ donation to the copper, weakening the Cu-O and O-O bonds. A decrease in vCu-O of the bis-μ-oxo- dicopper(III) complex was also observed with increasing N-donor strength for the R-MePY2 ligand system. However, no change was observed for vO-O of the side-on peroxo. This is attributed to a reduced charge donation from the peroxide π*σ orbital with increased N-donor strength, which increases the negative charge on the peroxide and adversely affects the back-bonding from the Cu to the peroxide σ*orbital. However, an increase in the bis-μ-oxo-dicopper(III) isomer relative to side-on peroxo-dicopper(II) species is observed for R-MePY2 with R = H 2N. This effect is attributed to the thermodynamic stabilization of the bis-μ-oxo-dicopper(III) isomer relative to the side-on peroxo-dicopper(II) isomer by strong donor ligands. Thus, the side-on peroxo-dicopper(II)/bis-μ-oxo-dicopper(III) equilibrium can be controlled by electronic as well as steric effects.
