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Lookup NU author(s): Dr Richard Scott, Kristin Downey, Dr Keith Healy, Dr Alistair Henderson, Claire Robinson, Professor William Clegg, Dr Ross Harrington, Emeritus Professor Bernard Golding
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Metabolism of 6,7-dichloro-1,5-dihydroimidazo[2,1-b]quinazolin-2-one (anagrelide), a drug for treating essential thrombocythemia, gives 6,7-dichloro-3-hydroxy-1,5-dihydroimidazo[2,1-b]quinazolin-2-one (3-hydroxyanagrelide) and 2-amino-5,6-dichloro-3,4-dihydroquinazoline. To enable the properties of 3-hydroxyanagrelide to be fully evaluated, the racemic compound has been synthesized. In pH 7.4 aqueous buffer 3-hydroxyanagrelide readily equilibrates with an isomer, 6,7-dichloro-1-hydroxy-3,5-dihydroimidazo[1,2-alpha]-quinazolin-2-one,and is also hydrolyzed to 2-amino-5,6-dichloro-3,4-dihydroquinazoline. 3-Hydroxyanagrelide (half-life 40 hours) was the dominant species at equilibrium and it was concluded that the equilibration and decomposition are sufficiently slow that published assays of 3-hydroxyanagrelide are reliable.
Author(s): Scott RB, Downey KM, Healy KP, Henderson AP, Robinson CL, Clegg W, Harrington RW, Franklin R, Golding BT
Publication type: Article
Publication status: Published
Journal: Heterocycles
Year: 2012
Volume: 86
Issue: 2
Pages: 1637-1646
Print publication date: 30/10/2012
ISSN (print): 0385-5414
ISSN (electronic): 1881-0942
Publisher: Japan Institute of Heterocyclic Chemistry
URL: http://dx.doi.org/10.3987/COM-12-S(N)115
DOI: 10.3987/COM-12-S(N)115
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