René Martin,René Smits,Ronny Hesse,Alexander Hoepping,Marco Müller,Sandra Hübner
申请号：
US16348997
公开号：
US10759760B2
申请日:
2017.11.17
申请国别(地区):
US
年份:
2020
代理人:
摘要：
A method for producing a radiofluorinated compound having an aromatic or heteroaromatic ring carrying [18F] fluorine as first substituent, a bonding unit, which can bind to a peptide or peptide mimetic, and a spacer group connected via bond A1 to the bonding unit and via bond A2 to the ring, wherein the bonding unit has second substituent(s) —；OH, —；CONH, and/or —；COOH. The steps include (a) providing a precursor having the ring carrying a substituent Y, bonding unit with the second substituent(s), and spacer group, wherein substituent Y is —；N+(R1R2R3), —；NO2, —；Cl, —；Br, —；F, or —；I, and R1, R2, and R3 are independently C1-C6 alkyl； and (b) reacting the precursor with a [18F] fluoride anion in the presence of an activation salt to the radiofluorinated compound, which has a cation N+(R4R5R6R7) with R4, R5, R6, and R7 being independently C1-C6 alkyl, wherein the substituent Y is replaced by [18F] fluoride.
