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C-acetate preparation method

A technology of acetate and acetyl bromide, which is applied in the field of 11C-acetate preparation, can solve the problems of easy blockage, synthesis and failure of pipelines, and achieve the effect of low production cost

Inactive Publication Date: 2009-12-09
THE FIRST AFFILIATED HOSPITAL OF SUN YAT SEN UNIV
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  • Abstract
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  • Application Information

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Problems solved by technology

However, the biggest disadvantage of this method is that the pipeline is easily blocked and the synthesis fails.

Method used

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Embodiment 1

[0029] 1.1 11 Synthesis of C-CA

[0030] Synthesized using a slightly modified carbon-11 choline / methionine synthesis module 11 In addition to the change of the purification column and reagents, C-AC only needs a slight change in the structure. Only 5# bottles and a vacuum pump are added to the original module to achieve 11 C-AC is fully automatically synthesized, and its synthesis process is shown in figure 1 .

[0031] Before synthesis, take 0.1 mL of anhydrous tetrahydrofuran solution of methylmagnesium bromide with a concentration of 0.87-1.5 mol / L and put it in Loop2. by PETtrace Cyclotron via 14 N(p,α) 11 C nuclear reaction production 11 CO 2 , 11 CO 2Trapped in Loop1 ring under liquid nitrogen cooling. At room temperature, with 10mL / min nitrogen as the carrier gas, 11 CO 2 In the LOOP2 ring, it reacts with methylmagnesium bromide to generate the intermediate acetylmagnesium bromide adduct, and the solvent tetrahydrofuran is passed to the waste gas bottle und...

Embodiment 2

[0038] Adopt 0.2mL 1.0mol / L methylmagnesium chloride to replace the 0.1mL 1.5mol / L methylmagnesium bromide in embodiment 1, radioactive decline in waste liquid, in crude product 11 CO 2 As the content increased, the labeling rate decreased slightly.

[0039] The present invention uses an integrated small column to complete the hydrolysis and purification work in the column. Compared with the small column purification method reported in the existing literature (references 1, 3-7), this method is very simple and easy to implement 11 The automatic synthesis of C-AC avoids production failure caused by the use of Ag+ column to generate silver halide precipitation to block the pipeline, and the production cost is significantly reduced. intermediate 11 C-acetyl bromide (or chloride) magnesium adduct can be hydrolyzed in the SEP-PAK TSCX column; the impurities contained in the product are mainly 11 CO 2 , 11 C-acetone and 11 C-carbonate, 11 C-tert-butanol, tetrahydrofuran, Mg ...

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Abstract

An C-acetate preparation method comprises the following steps: adopting methyl magnesium bromide or methyl magnesium chloride as precursor, reacting the precursor with CO2 in a Loop to prepare an intermediate C-acetyl bromine or magnesium chloride adduct; without adopting purification process, injecting N2 and removing tetrahydrofuran (THF), adding water in the mixture, injecting the mixture through integral small columns (C18 small column, SEP-PAK TSCX small column and SEP-PAK TIX small column) in turn for isolation and purification where the intermediate C-acetyl bromine or magnesium chloride hydrolyzes, filtrating by aseptic filter membrane, neutralizing by alkaline solution and obtaining C-AC parenteral solution. The preparation method of the invention has the advantages of the realization of column hydrolysis and purification, fully automatic synthesis, short synthesis time, high radiochemical yield, high radiochemical purity and low production cost.

Description

【Technical field】 [0001] The present invention relates to the application field of PET (Positron Emission Tomography positron emission tomography imaging), specifically relates to 11 Preparation method of C-acetate. 【Background technique】 [0002] PET uses the principle of photon collimation and coincidence detection technology to detect the photons of annihilation radiation produced by the tracer in vitro, and the collected information is processed by a computer to display the tomographic image of the target organ and give quantitative physiological parameters. At present, PET has become a very important diagnostic tool in clinical work, especially in the early diagnosis of cancer and brain functional imaging, for early diagnosis of malignant tumors, cardiovascular diseases, nervous system diseases, etc. has an irreplaceable role. [0003] 11 C-acetate ( 11 C-AC, 11 C-Aceate) is a positron emission tomography (PET) imaging agent used to measure the oxidative metabolism...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C53/10C07C51/41C07C51/04A61K51/04A61K51/12
Inventor 唐刚华唐小兰张祥松
Owner THE FIRST AFFILIATED HOSPITAL OF SUN YAT SEN UNIV
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