Abx Advanced Biochemical Compounds Gmbh

Marco Müller

Nikolas Bugdahn

René Smits

Alexander Hoepping

René Martin

Ronny Hesse

Sandra Hübner

Antje Fasel

Diana Baumgart

Andreas Clausnitzer

A method for producing a radiofluorinated compound having an aromatic or heteroaromatic ring carrying [F] fluorine as first substituent, a bonding unit, which can bind to a peptide or peptide mimetic, and a spacer group connected via bond Ato the bonding unit and via bond Ato the ring, wherein the bonding unit has second substituent(s) &#x2014;OH, &#x2014;CONH, and/or &#x2014;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 &#x2014;N(RRR), &#x2014;NO, &#x2014;Cl, &#x2014;Br, &#x2014;F, or &#x2014;I, and R, R, and Rare independently C-Calkyl; and (b) reacting the precursor with a [F] fluoride anion in the presence of an activation salt to the radiofluorinated compound, which has a cation N(RRRR) with R, R, R, and Rbeing independently C-Calkyl, wherein the substituent Y is replaced by [F] fluoride.

Precursors for radiofluorination

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Dresden, Germany

Marco Müller