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Preparation method of radioisotope carbon-14 labeled phenol alkali metal salt

A technology of phenol alkali metal salt and radioactive isotope, which is applied in the field of organic radiation chemical synthesis, and can solve problems such as optimization and high-efficiency conversion of synthesis process

Active Publication Date: 2021-05-18
浙江爱索拓标记医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Most of these methods are suitable for small-scale laboratory synthesis or industrial-scale phenol synthesis, but it is difficult to achieve the efficient conversion of trace carbon-14-labeled benzene to carbon-14-labeled phenol alkali metal salts under mild conditions through optimization of the synthesis process

Method used

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  • Preparation method of radioisotope carbon-14 labeled phenol alkali metal salt
  • Preparation method of radioisotope carbon-14 labeled phenol alkali metal salt
  • Preparation method of radioisotope carbon-14 labeled phenol alkali metal salt

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Under the argon atmosphere of the glove box, the pre-cooled (-10°C, the same below) carbon-14 homolabeled benzene (10 μCi) in ethanol (0.1 mL) was transferred to a pre-cooled ampoule (1.5 mL), Then add pre-cooled aqueous sodium hydroxide solution (0.01M, 2.00mL) into the ampoule, and then heat the top opening of the ampoule with a heat gun to melt and seal it tightly to obtain a sealed reaction system. Gently shake the sealed ampoule to mix the contents of the bottle evenly.

[0025] The sealed ampoules obtained above are fixed on a support, and sent into a 10 MeV electron accelerator together with a conveyor belt for electron beam irradiation. The control irradiation dose is 30kGr. After the irradiation, the carbon-14 labeled phenol sodium salt solution sealed in the ampoule was obtained. The radiochemical yield of the reaction was 18% as analyzed by HPLC-FSA (online radioactive high performance liquid chromatography) and LSC (liquid scintillation measurement).

Embodiment 2

[0027] Under the argon atmosphere of the glove box, the pre-cooled (-10°C, the same below) carbon-14 homolabeled benzene (10 μCi) in ethanol (0.1 mL) was transferred to a pre-cooled ampoule (1.5 mL), Then add pre-cooled aqueous sodium hydroxide solution (0.01M, 2.00mL) into the ampoule, and then heat the top opening of the ampoule with a heat gun to melt and seal it tightly to obtain a sealed reaction system.

[0028] The sealed ampoules obtained above are fixed on a support, and sent into a 10 MeV electron accelerator together with a conveyor belt for electron beam irradiation. The control irradiation dose is 100kGr. After the irradiation, the carbon-14 labeled phenol sodium salt solution sealed in the ampoule was obtained. According to HPLC-FSA and LSC analysis, the radiochemical yield of the reaction was 49%.

Embodiment 3

[0030] Under the argon atmosphere of the glove box, the pre-cooled (-10°C, the same below) carbon-14 homolabeled benzene (10 μCi) in ethanol (0.1 mL) was transferred to a pre-cooled ampoule (1.5 mL), Then add pre-cooled aqueous sodium hydroxide solution (0.01M, 2.00mL) into the ampoule, and then heat the top opening of the ampoule with a heat gun to melt and seal it tightly to obtain a sealed reaction system. Gently shake the sealed ampoule to mix the contents of the bottle evenly.

[0031] The sealed ampoules obtained above are fixed on a support, and sent into a 10 MeV electron accelerator together with a conveyor belt for electron beam irradiation. The control irradiation dose is 150kGr. After the irradiation, the carbon-14 labeled phenol sodium salt solution sealed in the ampoule was obtained. According to HPLC-FSA and LSC analysis, the radiochemical yield of the reaction was 28%.

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Abstract

The invention provides a preparation method of radioisotope carbon-14 labeled phenol alkali metal salt. The method is characterized in that under the conditions of normal temperature, normal pressure, no catalyst and air isolation, a mixed solution of carbon-14 labeled benzene, alkali and a solvent is irradiated by electron beams generated by a 10MeV electron accelerator to obtain a target object. The method is a one-step reaction and is simple and safe to operate, the loss of radioactive substances is small, and the quality guarantee period of a target object is long. The target object obtained by the invention can be used for preparing benzene ring carbon-14 labeled tracers required in radiopharmacokinetic research, in particular to high-specific-activity benzene ring carbon-14 markers of small-molecule chemical candidate drugs with extremely low administration dosage and chemical synthesis candidate drugs with relatively large relative molecular mass (greater than 2000).

Description

technical field [0001] The invention belongs to the field of organic radiation chemical synthesis, and in particular relates to a preparation method of carbon-14 labeled phenol alkali metal salt. Background technique [0002] The biomedical industry is one of the important components of my country's national economy. It is not only closely related to people's life and health, but also closely related to the national economy, people's livelihood and national security. Radiopharmacokinetic studies such as tissue distribution, material balance and metabolite identification in preclinical animal tests and clinical human trials of candidate new drugs are indispensable and important links for new drugs to enter the market. first element. Radioisotope labeling of candidate new drugs is a necessary tracer for carrying out radiopharmacokinetic studies of candidate new drugs, and radioisotope carbon-14 is the preferred radionuclide for the preparation of tracers [Radiolabeled absorpt...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C37/64C07C39/235A61K51/04A61K101/00
CPCC07C37/64A61K51/04C07B2200/05C07C39/235
Inventor 杨征敏马双江王国通
Owner 浙江爱索拓标记医药科技有限公司
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