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Method for synthesizing radionuclide-labeled compounds using exchange resins

A radionuclide and resin synthesis technology, applied in the field of computer programs, can solve problems such as unstable yields

Inactive Publication Date: 2011-12-21
BAYER SCHERING PHARMA OY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, automated synthetic methods currently known in the art have proven to produce products in inconsistent yields

Method used

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  • Method for synthesizing radionuclide-labeled compounds using exchange resins
  • Method for synthesizing radionuclide-labeled compounds using exchange resins
  • Method for synthesizing radionuclide-labeled compounds using exchange resins

Examples

Experimental program
Comparison scheme
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Embodiment Construction

[0103] As radionuclide-labeled compounds [ 18 Synthesis of F]-FEDAA

[0104] use image 3 Synthesis of the setup for automated radiolabeling (here radiofluorination) shown in [ 18 F] - FEDAA.

[0105] will 5GBq[ 18 F] Trapped on the first solid-phase extraction resin in the form of a QMA-column with 0.5 mol / l K 2 CO 3 The solution was pretreated and washed with water. Subsequently, with K 222 / K 2 CO 3 solution (dissolved in 0.2ml H 2 1.0 mg K in O and 0.8 ml acetonitrile (ACN) 2 CO 3 , 5.0 mg K 222 )Will[ 18 F] Elution into a reactor preheated to 60°C. Elution was performed in pulsed mode by repeatedly closing and reopening the input tubing with the valve (ACG-SV1) at a 5 second cycle.

[0106] The solvent was evaporated by heating to 110 °C under weak vacuum for 10 min with the aid of a gentle stream of dry nitrogen. dry[ 18 F] KF / K 2.2.2., then 2 mg of the precursor dissolved in DMF (600 μl) were added and heated at a reaction temperature of 120°C. After 5 ...

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Abstract

The present invention relates to methods of eluting radionuclide-labeled or radionuclide-labeled compounds using solid phase extraction resins, devices for carrying out such methods and computer programs for controlling such devices. In particular, the method of the invention enables the automated synthesis of radionuclide-labeled compounds using anion-exchange resins or reversed-phase resins, and involves removing or eluting the anion-exchange resin-bound The step of radionuclide labeling (fluorine-18, etc.) or a radionuclide-labeled compound bound to a reversed-phase resin.

Description

[0001] The present invention relates to methods of eluting radionuclide-labeled or radionuclide-labeled compounds using solid phase extraction resins, devices for carrying out such methods and computer programs for controlling such devices. Background of the invention [0002] Methods for the automated synthesis of radionuclide-labeled compounds using solid phase extraction resins, such as anion exchange resins or reverse resins, have long been known in the art. Such methods have been used inter alia to generate radiolabeled compounds that can be used as tracer molecules for a variety of biological applications. Such applications include positron emission tomography (PET), micro-PET, or single-photon emission computed tomography (SPECT), which are nuclear medicine techniques that utilize radioactive positron-emitting isotopes attached to molecules of biological relevance. diagnostic techniques in. [0003] as a radioactive tracer 18 F-radiolabeled molecules are radionuclide-...

Claims

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Application Information

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IPC IPC(8): C22B3/42A61K51/00B01D15/16B01J20/26B01J41/00C07B59/00B01J20/281C22B3/24G01N30/32
CPCB01D15/325A61K51/04C22B3/24B01J20/285B01J20/287G01N2030/009G01N30/32B01D15/424B01D15/363B01D15/362B01D15/16C22B3/42Y02P10/20A61K51/00B01J20/26
Inventor K·格雷厄姆A·罗特尔D·弗兰克
Owner BAYER SCHERING PHARMA OY
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