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Preparation technology of 18F labelled positive electron radioactivity tracer precusor

A technology of radiotracer and preparation process, which is applied in the field of synthesis of 18F-labeled positron radiotracer labeling process precursors, which can solve the problem of inability to determine the chemical and biological differences of radioactive compounds and the inability to determine the chemistry of positron radionuclides. and spatial location to achieve the effect of shortening synthesis efficiency, shortening synthesis time, and reducing environmental pollution

Inactive Publication Date: 2007-02-14
郭启勇 +1
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Problems solved by technology

If ordinary compounds or chemical molecules are directly radiolabeled with positrons, radionuclides may react with all functional groups, so we cannot determine the exact chemical and spatial positions of positron radionuclides in compounds or molecules. Unable to determine whether the labeled radioactive compound is chemically or biologically different from the original compound or molecule
Therefore, general compounds or molecules cannot be used directly 18 F-labeled positron radiotracer

Method used

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  • Preparation technology of 18F labelled positive electron radioactivity tracer precusor
  • Preparation technology of 18F labelled positive electron radioactivity tracer precusor
  • Preparation technology of 18F labelled positive electron radioactivity tracer precusor

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[0069] Highly selective organic reactions are one of the important topics in the research of organic synthesis methodology. Selecting the appropriate reaction volume and reaction conditions can improve the selectivity of the reaction. The selectivity of organic synthesis includes: chemoselectivity (chemoselectivity), regioselectivity (regioselectivity) and stereoselectivity (stereoselectivity). Chemoselectivity is determined by differences in the reactivity of different functional groups. Regioselectivity is determined by the difference in reactivity of different positions around the active group. Stereoselectivity concerns the relative or absolute stereochemistry of product molecules.

[0070] 1) The use of protective groups in organic chemical synthesis: In the process of organic synthesis, the parts that do not want to react are protected in the form of derivatives, and the original functional groups are restored after the purpose is achieved. This method is called "prote...

Embodiment 1

[0088] 3-N-tert-butylacyl-(5'-O-(4,4'-dimethoxytrityl)-2'-deoxy-3'-O-(4-nitrobenzenesulfonyl)- b-D-5 furan) thymine [3-N-t-Butoxycarbonyl-(5'-O-(4,4'-dimethoxytriphenylmethyl)-2'-deoxy-3'-O-(4-nitrobenzensulfonyl)-b-D-threopento furanosyl) thymine] synthetic steps:

[0089] 3-N-tert-butylacyl-(5'-O-(4,4'-dimethoxytrityl)-2'-deoxy-3'-O-(4-nitrobenzenesulfonyl)- The process of b-D-5furan) thymine is divided into three stages: first, thymine is used to synthesize [5'-O-(4,4'-bismethoxytrityl)-2'-deoxy-β-D -5 furan]thymine, then [5'-O-(4,4'-bismethoxytrityl)-2'-deoxy-3'-O-(4-nitrobenzenesulfonyl)- After β-D-5furan]thymine, the final product, 3-N-tert-Butoxycarbonyl-(5'-O-(4,4'-dimethoxytripphenylmethyl)-2'-deoxy-3, was obtained after protecting the pyrimidine functional group '-o-(4-nitrobenzenesulfonyl)-β-D-threopentofuranosyl)thymine. [5'-O-(4,4'-bismethoxytrityl)-2'-deoxy-3'-O-(4- Nitrobenzenesulfonyl)-β-D-5furan]thymine directly as a precursor (intermediate).

[0090] 1....

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Abstract

The present invention discloses synthesis process of precursor for the 18F labeled positron radioactive tracer. The synthesis process includes the following steps: 1. preparing [5'-O-(4, 4'-dimethoxyl trityl)-2'-deoxy-beta-D-5-furan] thymine through reaction of the material with ionic liquid as catalyst; 2. preparing [5'-O-(4, 4'-dimethoxyl trityl)-2'-deoxy-3'-O-(4-nitrophenylsulfonyl)-beta-D-5-furan] thymine through separating and treating the intermediate product of the forgoing step; 3. synthesizing the target product via introducing sulfonyl group as the leaving group into the product of the step 2 and reaction with ionic liquid; and 4. separating the final product. The present invention has the features of multiple use, great output, high efficiency, stable process, short synthesis period, low cost, etc.

Description

technical field [0001] The invention belongs to the field of chemical synthesis, in particular to a 18 Synthetic method of F-labeled positron radiotracer labeling process precursor (intermediate). Background technique [0002] Positron nuclides produced by medical cyclotrons are currently used clinically 15 O. 13 N. 11 C. 18 F 18 F has a half-life of 110 minutes and has become the most clinically valued positron radionuclide. 18 F-labeled positron radiotracers are the most commonly used positron radiotracers for clinical PET / CT, PET and coincident line systems. for example, 18 F-FDG, 18 F-FLT, 18 F-acetate, 18 F-choline, etc. as positive radiation tracers have been widely used in the early diagnosis, treatment plan formulation and curative effect observation of tumors, cardiovascular and nervous system diseases. However, currently used clinical 18 F-labeled positron radiotracers are 18 F nucleophilic substitution reaction specifically replaces elements, ions, fu...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H19/073C07B59/00A61K51/04A61K101/02
Inventor 郭启勇辛军
Owner 郭启勇
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