892664-11-8Relevant articles and documents
Mild and selective synthesis of an aryl boronic ester by equilibration of mixtures of boronic and borinic acid derivatives
Hawkins, Vanessa F.,Wilkinson, Mark C.,Whiting, Matthew
, p. 1265 - 1268 (2008)
Quenching of aryl Grignard reagents with 2-isopropoxy-4,4,5,5-tetramethyl- 1,3,2-dioxaborolane (isopropyl pinacol borate) under noncryogenic conditions can lead to mixtures of the corresponding boronic ester along with, generally undesired, borinic acid derivatives. We have found that in certain cases gentle heating of the crude reaction mixtures leads to complete equilibration to give the borinic esters as the sole product which can then be isolated in high yield. This novel equilibration can reduce the need for use of cryogenic conditions or large excesses of reagents to obtain selectivity during boronic ester syntheses.
Discovery of sodium 6-[(5-chloro-2-{[(4-chloro-2-fluorophenyl)methyl]oxy}phenyl)methyl]-2-pyridinecarboxylate (GSK269984A) an EP1 receptor antagonist for the treatment of inflammatory pain
Hall, Adrian,Billinton, Andy,Brown, Susan H.,Chowdhury, Anita,Clayton, Nicholas M.,Giblin, Gerard M.P.,Gibson, Mairi,Goldsmith, Paul A.,Hurst, David N.,Naylor, Alan,Peet, Caroline F.,Scoccitti, Tiziana,Wilson, Alexander W.,Winchester, Wendy
scheme or table, p. 2599 - 2603 (2010/05/19)
We describe the medicinal chemistry programme that led to the identification of the EP1 receptor antagonist GSK269984A (8h). GSK269984A was designed to overcome development issues encountered with previous EP1 antagonists such as GW8
PYRIDINE COMPOUNDS FOR THE TREATMENT OF PROSTAGLANDIN MEDIATED DISEASES
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Page/Page column 38; 41-42, (2008/06/13)
Compounds of formula (I) or a pharmaceutiically acceptable derivative thereof: wherein X, Y, Z, R2a, R2b, R3a, R3b, R8, R9, and Rx are as defined in the specification, a process
