http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2018091043-A1

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publicationDate 2018-05-24-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber WO-2018091043-A1
titleOfInvention Precursors for radiofluorination
abstract The invention relates to a method for producing a radiofluorinated compound which has an aromatic or heteroaromatic ring which carries [ 18 F] fluorine as the first substituent, a bonding unit which can bond to a peptide or a peptide mimetic, and a spacer group which connects the aromatic or heteroaromatic ring to the bonding unit, the bonding unit carrying at least one second substituent selected from the group consisting of -OH, -CONH and -COOH, the bonding unit being connected to the spacer group via a bond A 1 , and the spacer group being connected to the aromatic or heteroaromatic ring via a bond A 2 . According to the invention, the method comprises the following steps: (a) providing a precursor which has the aromatic or heteroaromatic ring which carries a substituent Y, the bonding unit which can bond to the peptide or the peptide mimetic and carries the at least one second substituent, and the spacer group, wherein the substituent Y is selected from the group consisting of -N + (R 1 R 2 R 3 ), -NO 2 , -Cl, -Br, -F or -I, and R 1 , R 2 and R 3 are identical to or different from one another and are each unsubstituted or substituted C 1 -C 6 alkyl; and (b) reacting the precursor with an [ 18 F] fluoride anion in the presence of an activation salt to produce the radiofluorinated compound, wherein the substituent Y is replaced by [ 18 F] fluorine and wherein the activation salt has a cation of the general formula N + (R 4 R 5 R 6 R 7 ), where R 4 , R 5 , R 6 and R 7 are identical to or different from one another and are each unsubstituted or substituted C 1 -C 6 alkyl.
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priorityDate 2016-11-18-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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