36404-90-7Relevant academic research and scientific papers
Synthesis of some fluorine-containing pyridinealdoximes of potential use for the treatment of organophosphorus nerve-agent poisoning
Timperley, Christopher M.,Banks, R. Eric,Young, Ian M.,Haszeldine, Robert N.
, p. 541 - 547 (2011/09/15)
Fluoroheterocyclic aldoximes were screened as therapeutic agents for the treatment of anticholinesterase poisoning. 2-Fluoropyridine-3- and -6-aldoxime, and 3-fluoropyridine-2- and -4-aldoxime, were synthesised. Attempts to obtain 3,5,6-trifluoropyridine-2,4-bis(aldoxime) and -2-aldoxime, however, proved unsuccessful. Pentafluorobenzaldoxime was prepared by oximation of pentafluorobenzaldehyde. Acid dissociation constants (pKa) and second-order rate constants (kox-) of the fluorinated pyridinealdoximes towards sarin were measured. 2,3,5,6-Tetrafluoropyridine-4- aldoxime had the best profile: its kox- approached that of the therapeutic oxime P2S (310 vs. 120 l mol-1 min-1), but its higher pKa (9.1 vs. 7.8) fell short of the target figure of 8 required for reactivation of inhibited acetylcholinesterase in vivo. N-alkylation of the fluorinated pyridine-aldoximes may reduce their pK a nearer to 8 and enhance their therapeutic potential. Crown Copyright
TETRACYCLIC INHIBITORS OF JANUS KINASES
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Page/Page column 91-92, (2008/06/13)
The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.
USING ALKYLMETAL REAGENTS FOR DIRECTED METALATION OF AZAAROMATICS
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Page 7-8, (2010/02/09)
Substituted alkylmetal reagents such as (trimethylsilylmethyl)lithium are reacted with azaaromatic compounds and/or nitrogen heterocycle compounds to produce functionalized azaaromatic compounds and functionalized nitrogen heterocycle compounds.
UROKINASE INHIBITORS
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, (2008/06/13)
Disclosed are benzothiophene and thienothiophene derivatives useful for inhibiting urokinase activity.
Le phenyl-lithium: nouvel agent de metallation du cycle pyridinique
Mallet, Marc
, p. 49 - 56 (2007/10/02)
Nucleophilic addition was the sole reaction of phenyl-lithium with a pyridinic ring; now the novel catalysed metallation, with phenyl-lithium, of many substituted pyridine compounds giving various derivatives in high yields with many different reagents, has been achieved.
Migration du lithium en serie pyridinique: double catalyse et reformage. Acces aux derives de la bromo-2 lithio-3 pyridine et des bromo-4 halogeno-2 lithio-3 pyridines
Mallet, Marc,Branger, Gilles,Marsais, Francis,Queguiner, Guy
, p. 319 - 332 (2007/10/02)
The lithium of an organolithium-pyridinic derivative can be moved from one position to an another by an intermolecular reaction.Two new reactions are possible for pyridinic organic synthesis: the isomerisation of any lithio derivative to a more stable one, and a reaction that transforms a mixture of various bromo-lithio derivatives into a single one.The processes involved and the experimental tools used are described in terms of the 2-bromo-3-lithio- and 4-bromo-2-halogeno-3-lithiopyridines derivatives synthesis.
