Abx Advanced Biochemical Compounds Gmbh

Helmholtz-Zentrum Dresden-Rossendorf E.v.

Universitaet Leipzig

Alexander Hoepping

Nikolas Bugdahn

René Smits

Ronny Hesse

Marco Müller

Sandra Hübner

René Martin

Marianne Patt

Peter Brust

Osama Sabri

Jörg Thomas Patt

Jörg Steinbach

Winnie Deuther-Conrad

Achim Hiller

Steffen Fischer

Sandra Hubner

Rene Martin

Marco Muller

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

The invention relates to a compound of formula Ia or Ib wherein Rrepresents &#x2014;COR, &#x2014;CORor &#x2014;R, wherein Rrepresents unsubstituted or substituted C-Calkyl, Rrepresents hydrogen, unsubstituted or substituted C-Calkyl, and Rrepresents hydrogen, unsubstituted or substituted C-Calkyl, Rrepresents &#x2014;N(R)(R)(R)Xor a nitro group, wherein R, R, Rindependently of each other represent unsubstituted or substituted C-Calkyl or unsubstituted or substituted &#x2014;(CH)n- with n=1 to 12 provided that at least two of the substituents RRRare C-Calkyl, and Xrepresents a halide, sulphonate, unsubstituted or substituted acetate, sulphate, hydrogen sulphate, nitrate, perchlorate, or oxalate.

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Dresden, Germany

Alexander Hoepping