- Selection and development of the manufacturing route for EP1 antagonist GSK269984B
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A potential manufacturing route for the EP1 antagonist GSK269984B was developed. Four synthetic approaches were examined, and a successful realisation of each is presented. The rationale supporting selection of the preferred route is discussed.
- Whiting, Matthew,Harwood, Kathy,Hossner, Frank,Turner, Peter G.,Wilkinson, Mark C.
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p. 820 - 831
(2011/03/19)
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- Mild and selective synthesis of an aryl boronic ester by equilibration of mixtures of boronic and borinic acid derivatives
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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.
- Hawkins, Vanessa F.,Wilkinson, Mark C.,Whiting, Matthew
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p. 1265 - 1268
(2013/01/03)
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- PYRIDYL COMPOUNDS
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Compounds of formula (I) or a pharmaceutically acceptable derivative thereof: wherein R1, R2, and R3 are as defined in the specification, a process for the preparation of such compounds, pharmaceutical compositions compris
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Page/Page column 22-23
(2008/06/13)
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- PYRIDINE COMPOUNDS FOR THE TREATMENT OF PROSTAGLANDIN MEDIATED DISEASES
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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
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Page/Page column 43
(2008/06/13)
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