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18F-Fallypride automatically synthesizing method

An automated synthesis, sep-pakc-18 technology, applied in the direction of organic chemistry methods, chemical instruments and methods, isotope introduction of organic compounds, etc., can solve the problems of long time-consuming high-efficiency liquid phase purification, unfavorable clinical promotion and use, expensive preparative columns, etc. problems, achieve the effect of high labeling rate, easy operation and high synthesis efficiency

Inactive Publication Date: 2008-04-09
JIANGSU INST OF NUCLEAR MEDICINE
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Problems solved by technology

Currently 18 The purification of F-Fallypride adopts high-performance liquid chromatography preparative column, which is expensive and takes a long time for high-performance liquid chromatography purification, which is not conducive to clinical promotion and use
[0003] Domestic Beijing Paite Biotechnology Co., Ltd. has developed a domestic PET-MF-2V-IT-I multifunctional fluorine labeling module for 18 The preparation of F-Fallypride provides an efficient tool for this module to 18 The method for the automated synthesis of F-Fallypride has not been reported yet

Method used

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  • 18F-Fallypride automatically synthesizing method

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Embodiment 1

[0019] 18 The method of F-Fallypride automatic synthesis is carried out by using the domestic PET-MF-2V-IT-I multifunctional fluorine labeling module 18 Automated synthesis of F-Fallypride, synthesized using Sep-Pak C-18 column pair 18 F-Fallypride was purified:

[0020] Produced by the accelerator 18 The F-solution was absorbed by the QMA column and was absorbed by the 1.5mL K-containing solution in the bottle (1). 222 (50~300mg / mL) and K 2 CO 3 (2~8mg / mL) acetonitrile / water=10 / 1 (V / V) solution is eluted into the reaction tube (7), after heating at 115°C to remove acetonitrile, add 2 mL of acetonitrile in the bottle (2) to the reaction tube Azeotropic removal of water and acetonitrile, then add 4-5mg of 18 F-Fallypride labeled precursor, react at 90°C for 25 minutes, cool down, add 2 mL of 80% acetonitrile in the bottle (4) to mix with it, start the negative pressure to make the liquid in the reaction bottle pass through the tee behind the Sep-Pak C-18 column Into the ...

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Abstract

The invention relates to an automatically synthetic method of <18>F-Fallypride, and belongs to the technical field of the synthesis of the <18>F-Fallypride for dopamine D2 receptor positron(PET) developer. By adopting the PET-MF-2V-IT-I type multifunctional fluorine marking module to carry out the automatic synthesis of the <18>F-Fallypride, as well as adopting the Sep-PakC-18 to purify the <18>F-Fallypride, the invention is capable of producing D2 receptor positron(PET) developer (s)-(-)(1-allyl pyrrolidine-2-amino methyl)-5-(3-[<18>f] fluoropropyl)-2, 3-dimethoxy benzamide(<18>F-Fallypride), and surveying the biological distribution in the mouse. The radiochemical productivity of the (<18>F-Fallypride) is 40.7 percent (verified), and the synthetic period is 25mins without HPLC separation, moreover, the radiochemical purity is higher than 95 percent. After the <18>F-Fallypride in injected, the radioactivity is mainly distributed in the liver. The injection of the striaturn in the brain is the highest, and the cleanness is slow. The automatic synthesis of the <18>F-Fallypride is rapid and efficient. Besides, the <18>F-Fallypride is a fine dopamine D2 receptor positron(PET) developer.

Description

technical field [0001] 18 The method of F-Fallypride automatic synthesis belongs to a kind of novel dopamine D2 receptor positron electron (PET) imaging agent 18 F-Fallypride synthesis technology field. Background technique [0002] (s)-(-)-N-(1-allylpyrrolidine-2-aminomethyl)-5-(3-[ 18 F] fluoropropyl)-2,3-dimethoxybenzamide ( 18 F-Fallypride) is a better dopamine D2 / D3 receptor imaging agent, with high selectivity and strong affinity with D2 receptors (Kd=30pmol / L), and has been widely used in schizophrenia and Parkinson's disease abroad Diagnosis, mechanism research, curative effect monitoring, etc. of various neuropsychiatric diseases [Document 1 Yang Min. 18F-fallypride: a dopamine D2 receptor PET imaging agent. Foreign Medical Radiation Medicine Nuclear Medicine Volume, 2003, 27(6): 259-262]. Currently 18 The synthesis of F-Fallypride is mostly prepared manually, and there is no report on the synthesis module. Manual preparation has great radiation hazards for ...

Claims

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Application Information

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IPC IPC(8): C07D207/14C07B59/00A61K51/04A61K101/02
Inventor 杨敏徐宇平潘栋辉赵富宽王颂佩唐婕刘春仪
Owner JIANGSU INST OF NUCLEAR MEDICINE
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