19490-91-6Relevant academic research and scientific papers
Optimized S-trityl-l-cysteine-based inhibitors of kinesin spindle protein with potent in vivo antitumor activity in lung cancer xenograft models
Good, James A. D.,Wang, Fang,Rath, Oliver,Kaan, Hung Yi Kristal,Talapatra, Sandeep K.,Podgórski, Dawid,MacKay, Simon P.,Kozielski, Frank
supporting information, p. 1878 - 1893 (2013/05/08)
The mitotic kinesin Eg5 is critical for the assembly of the mitotic spindle and is a promising chemotherapy target. Previously, we identified S-trityl-l-cysteine as a selective inhibitor of Eg5 and developed triphenylbutanamine analogues with improved pot
DUTPASE INHIBITORS
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Page/Page column 52-53, (2008/06/13)
Deoxyuridine derivatives of the formula (I) where R1 is H or various substituents; D is -NHCO-, -CONH-, -0-, -C(=O)-, -CH=CH, -CΞC-, -NR5-; R4 is hydrogen or various substituents; R5 is H, C1-C4 alkyl, C1-C4 alkanoyl; E is Si or C; R6, R7 and R8 are independently selected from C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl or a stable monocyclic, bicyclic or tricyclic ring system; G is -O-, -S-, -CHR10-, -C(=O)-; J is -CH2-, or when G is CHR10 may also be -O- or -NH-; R10 is H, F, -CH3, -CH2NH2, -CH2OH; -OH R11 is H, F, -CH3, -CH2 NH2, -CH2OH, CH(OH)CH3, CH(NH3)CH3; or R10 and R11 together define an olefinic bond, or together form a -CH2-group, thereby defining a cis or trans cyclopropyl group; have utility in the prophylaxis or treatment of protozoal diseases such as malaria.
Effective lithiation of 3-bromopyridine: Synthesis of 3-pyridine boronic acid and variously 3-substituted pyridines
Cai, Dongwei,Larsen, Robert D,Reider, Paul J
, p. 4285 - 4287 (2007/10/03)
By using toluene as a solvent, 3-lithiopyridine can be generated cleanly at -50°C. The addition of various electrophiles affords useful building blocks, such as the 3-pyridine boronic acid in 87% isolated yield.
New syntheses of substituted pyridines via bromine-magnesium exchange
Trécourt, Fran?ois,Breton, Gilles,Bonnet, Véronique,Mongin, Florence,Marsais, Francis,Quéguiner, Guy
, p. 1349 - 1360 (2007/10/03)
Bromine-magnesium exchange using iPrMgCl in THF at room temperature on 2-, 3- and 4-bromopyridines allowed the synthesis of various functionalized pyridines. The methodology was successfully used for the synthesis of 4- azaxanthone. Moreover, single exchange reactions observed on 2,6-, 3,5-, 2,3- and 2,5-dibromopyridines, with complete regioselectivity in the case of 2,3- and 2,5-dibromopyridines, afforded substituted bromopyridines, which were then involved in a second exchange step to provide difunctionalized pyridines. (C) 2000 Elsevier Science Ltd.
Diphenylpyridylmethyl radicals. Part 1. Synthesis, dimerization and ENDOR spectroscopy of diphenyl(2-, 3- or 4-pyridyl)methyl radicals; bond dissociation enthalpies of their dimers
Tzerpos, Nikolaos I.,Zarkadis, Antonios K.,Kreher, Richard P.,Repas, Liesel,Lehnig, Manfred
, p. 755 - 762 (2007/10/02)
ortho-ortho hydrogen van der Waals repulsions are the origin of the propeller shape of the triphenylmethyl radical and the main reason for the low bond dissociation enthalpy (BDH) of its dimer 1 (44.8 J mol-1).In order to reduce these steric repulsions (eliminating some aromatic hydrogens), diphenyl(2-, 3- or 4-pyridyl)methyl radicals 2-4 were prepared through reductive dehalogenation of the corresponding triarylchloromethanes 2-4a with silver in benzene.They form α,p-dimers 2-4e exclusively through the pyridine ring.ENDOR spectroscopy shows that the structure of the radicals, does not deviate substantially from that of the parent radical, PH3C-radical.In contrast, the BDH values of the dimers (measured using EPR spectroscopy) show strengthening of the central C-C bond in 2e (88.7 kJ mol-1) and 3e (90.0 kJ mol-2) and a silimar value for 4e (46.4 kJ mol-1) with respect to the trityl dimer 1.This is a consequence of the ground state stabilization of the dimers 2-4e due to relief of strain (elimination of ring hydrogens), whereas in the case of 4e, this stabilization is probably compensated by the formation of a weaker C-N bond with respect to the C-C bond.The above dimers undergo easy 1,5-H-rearrangement, autocatalysed by the basic pyridyl groups themselves.
