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Device and process capable of simultaneously preparing three different <18>F radiopharmaceuticals

A 18F and drug synthesis technology, applied in the field of imaging agent devices, can solve the problems of waste, high construction costs, and increased investment in PET centers, so as to achieve full and reasonable utilization and reduce investment costs.

Inactive Publication Date: 2008-12-31
BEIJING NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The construction cost of the hot chamber itself is quite high, which will inevitably increase the investment of the PET center, and there are still 18 F's waste problem

Method used

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  • Device and process capable of simultaneously preparing three different &lt;18&gt;F radiopharmaceuticals
  • Device and process capable of simultaneously preparing three different &lt;18&gt;F radiopharmaceuticals
  • Device and process capable of simultaneously preparing three different &lt;18&gt;F radiopharmaceuticals

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0056] Embodiment 1, synthesized with the BNUF-A3 device shown in Figure 1 18 F-FET, 18 F-AV133 and 18 F-FDG

[0057] 1-(2-(2-fluoro[ 18 F] on behalf of ethoxy) ethyl-2-nitro-1-H-imidazole ( 18 F-FET) is a hypoxic imaging agent. Through 2-(2-(2-nitro-1 H-imidazole) ethoxy) ethyl p-toluenesulfonate and K 18 The acetonitrile solution of F-K2.2.2 was reacted at 100°C for 10 minutes to 18 F is substituted for p-toluenesulfonate to give 18 F-FETs. 18 The reaction formula of F-FET:

[0058]

[0059] 2-(2-(2-nitro-1H-imidazole)ethoxy)ethyl 1-(2-(2-fluoro[ 18 F] on behalf of ethoxy) ethyl -

[0060] p-Toluenesulfonate 2-nitro-1-H-imidazole

[0061] 18 F-AV133 is a molecular probe for early diagnosis of Parkinson's disease (PD). Similarly, 18 F-AV133 interacts with K through its precursor 18 The acetonitrile solution of F-K2.2.2 was reacted at 100°C for 10 minutes to make 18 Made by substituting p-toluenesulfonate at the end of the propoxy group.

[0062] 18 The re...

Embodiment 2

[0088] Embodiment 2, synthesize with BNUF-A3 two-step method shown in Fig. 1 18 F-FECNT

[0089] 18 The preparation of F-FECNT is through ethylene glycol 1,2-p-toluenesulfonate and K18 The acetonitrile solution of F-K2.2.2 was reacted at 100°C for 10 minutes to obtain the intermediate p-toluenesulfonic acid-2-fluoro[ 18 F] ethyl ester; then, p-toluenesulfonic acid-2-fluoro[ 18 F] Ethyl ester reacts with (2S,3S)-3-(p-chlorophenyl)-8-N-bicyclo[3,2,1]octane-2-acid methyl ester in DMF at 135°C 45 minutes to get it.

[0090] 18 F-FECNT synthetic route:

[0091]

[0092] 1,2-Ethylene p-toluenesulfonate p-toluenesulfonate-2-fluoro[ 18 F] ethyl ester

[0093]

[0094] (2S,3S)-3-(p-chlorophenyl)-8-N-bicyclic 18 F-FECNT

[0095] [3.2.1] Octyl-2-acid methyl ester

[0096] 1) Preparation:

[0097] Referring to Figure 1, connect thermal ports r-r" and t-t'; install a silica gel column at chromatographic column 37; inject 0.5 mL of acetonitrile solution of 1,2-di-p-toluenes...

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Abstract

The invention discloses an 18F drug synthesis device which comprises a nitrogen source, a cold trap foracetonitrile condensation, a liquid waste bottle for collecting waste liquid, an 18F purification system, at least a reaction system, as well as a standby reaction system which is connected with one or more of the reaction systems. The 18F drug synthesis device of the invention can greatly reduce the cost of PET center investment, fully and rationally make use of 18F and meet a variety of clinical demands for 18F drugs.

Description

technical field [0001] The invention relates to a device for preparing imaging agents used in positron tomography (PET), more particularly to a device capable of simultaneously preparing multiple imaging agents for PET 18 F Synthesis device and process of radiopharmaceuticals. Background technique [0002] C, N, O, and H are the basic elements that make up the living matter of the human body, and most PET drugs are human endogenous metabolites or analogues labeled with their positron nuclides. Different from morphological imaging examinations such as computed tomography (CT), PET images reflect the physiological and biochemical distribution changes of drugs in the body, and are biochemical imaging in vivo. The examination of biochemical abnormalities can diagnose diseases earlier and more accurately, and evaluate treatment effects more sensitively and objectively. F is a H-like element, and the H in the compound molecule is replaced by F. As long as the substitution site i...

Claims

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Application Information

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IPC IPC(8): C07B59/00A61K51/00A61K101/02
Inventor 李崧朱霖浮吉生刘亚静刘正浩孙继壮
Owner BEIJING NORMAL UNIVERSITY
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