Invention Grant
- Patent Title: Precursors for radiofluorination
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Application No.: US16778155Application Date: 2020-01-31
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Publication No.: US11053200B2Publication Date: 2021-07-06
- Inventor: René Martin , René Smits , Ronny Hesse , Alexander Hoepping , Marco Müller , Sandra Hübner
- Applicant: ABX advanced biochemical compounds GmbH
- Applicant Address: DE Radeberg
- Assignee: ABX advanced biochemical compounds GmbH
- Current Assignee: ABX advanced biochemical compounds GmbH
- Current Assignee Address: DE Radeberg
- Agency: Maier & Maier, PLLC
- Priority: DE102016122273.9 20161118
- Main IPC: C07D213/82
- IPC: C07D213/82 ; C07B59/00 ; A61K51/04

Abstract:
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.
Public/Granted literature
- US20200165204A1 PRECURSORS FOR RADIOFLUORINATION Public/Granted day:2020-05-28
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