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Carbon-11 (<11>C) radiopharmaceutical, preparation method and application thereof

A radiopharmaceutical technology, 11C-FAPI-02, is applied in the field of medicine to achieve high specific activity, mild labeling conditions, and good targeting effects

Active Publication Date: 2021-07-13
RENJI HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, subsequent researchers used 18 F nuclide substitution 68 Ga nuclide labels FAPI molecules, but it has not been reported at home and abroad 11 C-labeled FAPI molecular probe

Method used

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  • Carbon-11 (&lt;11&gt;C) radiopharmaceutical, preparation method and application thereof
  • Carbon-11 (&lt;11&gt;C) radiopharmaceutical, preparation method and application thereof
  • Carbon-11 (&lt;11&gt;C) radiopharmaceutical, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] targeting fibroblast activation protein (FAP) 11 C-labeled positron radiopharmaceuticals 11 The preparation method of C-FAPI-01 comprises the following steps:

[0053] Step 1. Synthesis reaction: use the accelerator of Sumitomo 10MV in Japan to pass the nuclear reaction 14 N(p,α) 11 C production 11 CO 2 , target beam current is 50μA, bombardment 30min generates 30GBq 11 CO 2 ; 11 CO 2 Use high-purity nitrogen as a carrier gas to transfer it to a temperature of -10°C, 300 μL, a concentration of 0.3M lithium aluminum hydride in tetrahydrofuran solution for 3 minutes, and then heat to 150°C to evaporate tetrahydrofuran to dryness (about 1.5 minutes), and then Add 0.3 milliliters of concentration and be 57% hydroiodic acid, heat to 180 ℃ and react for 3 minutes, the 11 CH 3 I gas is obtained directly by passing through a glass tube loaded with silver trifluoromethanesulfonate at a temperature of 200°C 11 C methyl trifluoromethanesulfonate ( 11 CH 3 OTf), direct...

Embodiment 2

[0057] targeting fibroblast activation protein (FAP) 11 C-labeled positron radiopharmaceuticals 11 The preparation method of C-FAPI-02 comprises the following steps:

[0058] Step 1. Synthesis reaction: use the accelerator of Sumitomo 10MV in Japan to pass the nuclear reaction 14 N(p,α) 11 C production 11 CO 2 , target beam current is 50μA, bombardment 20min generates 25GBq 11 CO 2 ; 11 CO 2 Use high-purity nitrogen as a carrier gas to transfer it to a temperature of -12°C, 500 μL, a concentration of 1M lithium aluminum hydride tetrahydrofuran solution for 2 minutes, then heat to 150°C to evaporate tetrahydrofuran to dryness (about 2 minutes), and then add 0.5 milliliters of concentration is 57% hydroiodic acid, is heated to 180 ℃ and reacts for 4 minutes, generates during the reaction 11 CH 3 I gas is obtained directly by passing through a glass tube loaded with silver trifluoromethanesulfonate at a temperature of 200°C 11 C Methyl trifluoromethanesulfonate ( 11 C...

Embodiment 3

[0061] The target fibroblast activation protein (FAP) obtained in embodiment 1 11 C-labeled positron radiopharmaceuticals 11 C-FAPI-01 was used as a PET imaging agent in the imaging of tumor model mice. will be 7.4MBq 11 C-FAPI-01 was injected into mice through the tail vein, and small animal PET imaging was performed after 30 minutes of drug metabolism, as shown in image 3 Shown, visible radiopharmaceuticals 11 C-FAPI-01 is highly uptaked in tumor sites in high-expression FAP model mice.

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Abstract

The invention discloses a carbon-11 (<11>C) radiopharmaceutical, a preparation method and application thereof, and relates to the technical field of medicines. The <11>C-labeled positron radiopharmaceutical comprises <11>C-FAPI-01 and <11>C-FAPI-02, wherein the <11>C-FAPI-01 and the <11>C-FAPI-02 are chemically named as (S)-N-(2-(2-cyanopyrrolidine-1-yl)-2-oxoethyl)-6-(methoxy-<11>C)quinoline-4-carboxamide and (S)-N-(2-(2-cyan-4,4-difluoropyrrolidine-1-yl)-2-oxoethyl)-6-(methoxy-<11>C) quinoline-4-carboxamide respectively. The preparation method comprises synthesis and separation purification. The radiopharmaceutical can be used as an imaging agent in positron emission computed tomography (PET / CT) examination. According to the invention, the radiochemical synthesis reaction conditions are mild, the synthesis time is short, the radiochemical yield is high, and the fibroblast activating protein can be detected in a targeted manner.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a carbon-11 ( 11 C) Radiopharmaceuticals and their preparation methods and applications. Background technique [0002] Positron emission tomography (PET) is a relatively advanced medical imaging technology in the field of nuclear medicine. Based on radionuclide tracer technology, it has the characteristics of high sensitivity, high spatial resolution, and three-dimensional images of the whole body. , is a diagnostic tool of great clinical value. Currently in PET technology, tracers play an important role. In PET technology, the tracer distribution is usually detected by PET imaging according to the metabolic process of the tracer in the human body, so as to provide a basis for cancer diagnosis and treatment. However, the currently widely used PET tracer 18F-FDG is not targeted to tumor cells, which to some extent limits the application of PET technology in tumor diagnosis and...

Claims

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Application Information

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IPC IPC(8): C07D401/12A61K31/4709A61P35/00A61K51/04A61K101/00
CPCC07D401/12A61P35/00A61K51/0455
Inventor 王成胡周密刘建军黄钢
Owner RENJI HOSPITAL AFFILIATED TO SHANGHAI JIAO TONG UNIV SCHOOL OF MEDICINE
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