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Standard precursor of positron imaging agent and preparation method thereof

A technology for positron imaging agent and standard product, which is applied in the preparation of sugar derivatives, chemical instruments and methods, pharmaceutical formulations, etc., can solve the problems of high cost of raw materials and reagents, low yield, difficulty in synthesizing galactose analogs, etc. , to achieve the effect of simple and fast synthesis process and high yield

Inactive Publication Date: 2019-01-18
NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] At present, there are few studies on galactose analogs specifically targeting ASGPR, and the existing processes generally have the following disadvantages: 1) The synthesis of galactose analogs is difficult and the yield is low; 2) The reaction time is long; 3) High cost of raw materials and reagents

Method used

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  • Standard precursor of positron imaging agent and preparation method thereof
  • Standard precursor of positron imaging agent and preparation method thereof
  • Standard precursor of positron imaging agent and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] A positron imaging agent standard precursor, the preparation method is as follows:

[0055] 1) Put (1eq) dispersed in 20mL of dichloromethane (DCM), then add an appropriate amount of freshly evaporated molecular sieve MS4A, stir for 20min, then add trimethylsilane azide (1.2eq) and tin tetrachloride (1.6eq), Stir at room temperature for 7 hours, dilute with DCM, remove molecular sieve by suction filtration, and separate the filtrate by column chromatography to obtain white solid crystals 80% yield;

[0056] 2) Put (1eq) dispersed in 20mL solvent (10mL tert-butanol + 10mL water), then add 4-pentyn-1-ol (2eq), copper sulfate pentahydrate (1eq) and sodium ascorbate (2eq), stir at room temperature for 12h , The reaction solution was extracted with ethyl acetate, and then the extract was dewatered with anhydrous sodium sulfate, and then separated by column chromatography to obtain a colorless viscous liquid The yield is 95%;

[0057] 3) Put (1eq) dispersed in 12mL of dichloro...

Embodiment 2

[0064] A positron imaging agent standard precursor, the preparation method is as follows:

[0065] 1) Put (1eq) dispersed in 20mL of dichloromethane (DCM), then add an appropriate amount of freshly evaporated molecular sieve MS4A, stir for 20min, then add trimethylsilane azide (1.3eq) and tin tetrachloride (1.8eq), Stir at room temperature for 8h, dilute with DCM, remove molecular sieve by suction filtration, and separate the filtrate by column chromatography to obtain white solid crystals 80% yield;

[0066] 2) Disperse 4-pentyn-1-ol (1eq) in 20mL solvent (10mL tert-butanol + 10mL water), add diethylaminosulfur trifluoride (5eq), and react at -30°C for 12h to obtain 5-fluoro-1-pentyne, yield 60%;

[0067] 3) Put (1eq) dispersed in 15mL of dichloromethane, then add 5-fluoro-1-pentyne (2eq), copper sulfate pentahydrate (1eq) and sodium ascorbate (2eq), react at room temperature for 12h, and use ethyl acetate to react After extraction, the extract was dewatered with anhydrous sodi...

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Abstract

The invention discloses a standard precursor of a positron imaging agent and a preparation method thereof. The structural formula of the standard precursor is shown in the specification. The standardprecursor of the positron imaging agent is simple and rapid in synthesis process and high in yield and can be used for preparing imaging agent standards which specifically target an asialoglycoproteinreceptor (ASGPR).

Description

Technical field [0001] The invention relates to a standard precursor of a positron imaging agent and a preparation method thereof. Background technique [0002] PET Tumor Receptor Imaging (Tumor Receptor Imaging) is based on the principle that the corresponding ligands labeled with positron radionuclide are combined with specific receptors that are highly expressed in tumors and have high affinity with target tissues, showing the spatial distribution and density of tumor receptors. The imaging technology with affinity. PET tumor receptor imaging has high affinity, strong specificity, strong penetrating ability, radiolabeled ligands reach the target and fast blood clearance, and can obtain high-contrast images of tumor and normal tissue in a short time. The human body has the advantages of immune response and other advantages, and it is also non-invasive. The ability to conduct cell-molecular-level research in a living state is one of the important development directions of molec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H19/056C07H1/00A61K51/04A61K101/02
CPCA61K51/0491A61K51/0497C07H1/00C07H19/056
Inventor 孙朋辉胡孔珍黄顺韩彦江王猛王全师吴湖炳谭建儿王丽娟
Owner NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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