Method for preparing [18f]fallypride with low base concentration

Active Publication Date: 2012-07-12
SEOUL NAT UNIV R&DB FOUND
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  • Abstract
  • Description
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Benefits of technology

[0014]In the method for preparing [18F]fallypride according to the present invention, it is possible to improve the radiochemical yield and purity of [18F]fallypride with low base concentration method ex

Problems solved by technology

The SPECT disadvantageously has a poor accuracy in a resolution and quantification of the image as compared to the PET.
Such large amounts of base (>3 mg for K2CO3>30 μL for TBAHCO3) lead to more than the expected amounts of various side products, and hence require more quantity of precursor and diminish radioch

Method used

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  • Method for preparing [18f]fallypride with low base concentration
  • Method for preparing [18f]fallypride with low base concentration
  • Method for preparing [18f]fallypride with low base concentration

Examples

Experimental program
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Effect test

experiment 1

Recovery measurement of Fluorine-18

[0064]The separation of Fluorine-18 from Chromafix PS-HCO3 is performed after radioactive fluorine-18 in H218O water is collected in Chromafix PS-HCO3, and the fluorine-18 is isolated and recovered by means of a phase-transfer catalyst (base) and elution solvent.

[0065]The amount of recovered fluorine-18 is based on a reactive substance in the course of preparing [18F]fallypride according to the present invention while influencing the synthetic yield of [18F]fallypride. So, it is needed to measure the recovery ratio of fluorine-18 as follows in order to known the optimum combination of the phase-transfer catalyst (base) and the elution solvent.

[0066]*In more details, K2.2.2. / K2CO3 or 40% TBAHCO3 were used as the phase-transfer catalyst (base), and CH3CN / H2O or MeOH / H2O was used as elution solvent. The recovery ratio of the fluorine-18 at Chromafix PS-HCO3 was measured while changing the concentration of the phase-transfer catalyst (base), a resul

experiment 2

Radiochemical Yield and Total Preparation Time Measurement

[0068]In the method for preparing [18F]fallypride according to the present invention, the following experiments were performed in order to determine what the phase-transfer catalyst (base) and the elution solvent influence the radiochemical yield and total preparation time of [18F]fallypride.

[0069]The [18F]fallypride was prepared in the same method as the embodiment with the reaction time of being 30 minutes and 10 minutes, respectively, by using a combination of four phase-transfer catalysts (base) and solvents which had the best recovery ratio of fluorine-18 as a result of the experiment 1, and the radiochemical yield and total preparation time of the [18F]fallypride were measured, the results of which are shown in Table 2.

TABLE 2Classifi-Phase-transferSolventReactionRadiochemicalTotal preparationcationcatalyst (base)(1.0 / 0.2 mL)time (minutes)yield (%)time (minutes)1K2.2.2. / K2CO3CH3CN / H2O3026 ± 4.974 ± 1.2(13 / 3.0 mg)2K

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Abstract

A method for preparing [18F]fallypride is disclosed, which comprises a first step for trapping a fluorine-18 to a polymer ion exchange cartridge; a second step for extraction of fluorine-18 by inputting low base concentrations: 5.0˜25 μL of 40% TBAHCO3 or K2.2.2./K2CO3 (5˜25 mg/0.5˜3.0 mg) as a phase-transfer catalyst in a mixture of alcohol/water (1.0/0.2 (v/v)) or alcohol as a solvent into the polymer ion exchange cartridge trapped by the fluorine-18; a third step for preparing a [18F]fallypride product by removing the solvent from the trapped fluorine-18, by inputting tosylate precursor in CH3CN as a solvent into a reactor and by reacting the same for 5˜35 minutes at 50˜120° C.; and a fourth step for preparing a pure [18F]fallypride by purifying the prepared [18F]fallypride product.

Description

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Claims

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Application Information

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Owner SEOUL NAT UNIV R&DB FOUND
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