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Title:
PREPARATION OF FLUORINE-LABELLED COMPOUNDS
Document Type and Number:
WIPO Patent Application WO/2010/007363
Kind Code:
A3
Abstract:
The invention relates to a process for producing a fluorine-labelled compound, the process comprising: (a) treating a compound of formula (I) wherein R1, R2 and the C(H) group to which R1 and R2 are bonded together form a moiety to be labelled with fluorine; and the fluorous tag is a group of formula (II) wherein Rf is a straight-chained or branched C4-I2 perfluoroalkyl group; and L is a single bond, -alk-, -arylene-, -alk-arylene-, alk-X-, -arylene-X-, -alk-arylene-X, -alk- X-arylene-, -alk-X-arylene-X-, -arylene-alk-, -arylene-X-alk-, -arylene-alk-X- or - arylene-X-alk-X-, wherein X is N(R"), O, S, C(O) or C(O)N(R") and wherein alk is unsubstituted or substituted C1-10 alkylene which is optionally interrupted by N(R"), O, S, C(O), C(O)N(R") or arylene, wherein R" is C1-6 alkyl or aryl; with [nF], wherein nF is 18F or 19F, thereby fluorinating and detagging the compound of formula (I) to produce a fluorine-labelled compound of formula (III) The invention further relates to compounds of formula (I), a process for producing such compounds, and a combination product which comprises the two reactants used in that process.

Inventors:
GOUVERNEUR, Veronique (Chemistry Research Laboratory, 12 Mansfield Road, Oxford OX1 3TA, GB)
BEJOT, Romain (Chemistry Research Laboratory, 12 Mansfield Road, Oxford OX1 3TA, GB)
Application Number:
GB2009/001742
Publication Date:
July 01, 2010
Filing Date:
July 14, 2009
Export Citation:
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Assignee:
ISIS INNOVATION LIMITED (Ewert Place, Ewert HouseSummertown, Oxford 0X2 7SG, GB)
GOUVERNEUR, Veronique (Chemistry Research Laboratory, 12 Mansfield Road, Oxford OX1 3TA, GB)
BEJOT, Romain (Chemistry Research Laboratory, 12 Mansfield Road, Oxford OX1 3TA, GB)
International Classes:
C07B59/00; C07B39/00; C07C303/28; C07C309/65
Domestic Patent References:
WO2002090298A22002-11-14
WO2006065038A12006-06-22
Foreign References:
EP2017258A12009-01-21
Other References:
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Attorney, Agent or Firm:
SILCOCK, Peter, James et al. (J.A. KEMP & CO, 14 South SquareGray's Inn, London WC1R 5JJ, GB)
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