A carbon-11 ( 11 c) Radiopharmaceuticals and their preparation methods and applications

A radiopharmaceutical and radioactive technology, applied in the field of medicine, achieves the effects of simple synthesis, fast and efficient labeling, and good targeting.

Active Publication Date: 2022-03-04
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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  • A carbon-11 ( <sup>11</sup> c) Radiopharmaceuticals and their preparation methods and applications
  • A carbon-11 ( <sup>11</sup> c) Radiopharmaceuticals and their preparation methods and applications
  • A carbon-11 ( <sup>11</sup> c) Radiopharmaceuticals and their preparation methods and applications

Examples

Experimental program
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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) The radiopharmaceutical and its preparation method and application relate to the field of medical technology. use 11 C-labeled positron radiopharmaceuticals, including 11 C‑FAPI‑01 and 11 C-FAPI-02, the chemical names are (S)-N-(2-(2-cyanopyrrolidin-1-yl)-2-oxoethyl)-6-(methoxy- 11 C) quinoline-4-carboxamide and (S)-N-(2-(2-cyano-4,4-difluoropyrrolidin-1-yl)-2-oxoethyl)-6-( Methoxy- 11 C) quinoline-4-carboxamide; its preparation includes synthesis and separation and purification methods; the radiopharmaceutical can be used as an imaging agent for positron emission tomography PET / CT inspection. The radiochemical synthesis reaction condition of the invention is mild, the synthesis time is fast, the radiochemical yield is high, and the fibroblast activation protein can be targeted.

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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Patent Type & Authority Patents(China)
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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