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A kind of synthesis method of radioactive isotope carbon-14 labeling poison fluorophos

A technology of radioisotopes and synthesis methods, applied in the field of radiochemical synthesis, can solve the problems of lack of in-depth research on the metabolic process of toxic fluorine and phosphorus and environmental behavior, and achieve the effects of firm labeling, high chemical purity, and not easy to fall off.

Active Publication Date: 2020-11-03
浙江爱索拓标记医药科技有限公司
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Problems solved by technology

At present, studies on the absorption, distribution, transfer, residue of pentadophos in plants and its environmental behavior in water and soil are currently limited to the detection of parent compounds by chromatography or chromatography-mass spectrometry, and rarely involve other Metabolism / degradation products; while there is still a lack of in-depth research on the metabolic process and environmental behavior of parafluorophos

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  • A kind of synthesis method of radioactive isotope carbon-14 labeling poison fluorophos
  • A kind of synthesis method of radioactive isotope carbon-14 labeling poison fluorophos
  • A kind of synthesis method of radioactive isotope carbon-14 labeling poison fluorophos

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[0024] The following examples are given to illustrate the present invention. The implementation examples are only used to further illustrate the present invention, and do not represent the protection scope of the present invention. Non-essential modifications and adjustments made by others according to the present invention still belong to the protection scope of the present invention.

[0025] At room temperature under a CO atmosphere, trifluoroacetic acid (10 mL) was added to a mixture containing potassium persulfate (1650 mg) and palladium acetate (261 mg), stirred, and then [U- 14 C 6 ] Benzene (65.6 mCi, 25.5 mCi / mmol). Vigorous stirring was continued at atmospheric pressure for 10 h. After the reaction is completed, concentrate the reaction solution to dryness, add water, adjust the pH to 13 with NaOH aqueous solution, extract the aqueous phase with methyl tert-butyl ether to remove impurities, adjust the pH to 1 with concentrated hydrochloric acid, extract with ethyl ...

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Abstract

The invention belongs to the field of radiochemical synthesis, and particularly relates to a synthesis method of radioactive isotope carbon-14 labeled Dufulin (N-[2-(4-methyl[phenyl-U-<14>C<6>]benzothiazolyl)]-2-amino-2-fluorophenyl-O,O-diethylmethylphosphonate). According to the method, a feasible and economic method is provided for synthesizing the carbon-14 label of a benzene ring in a benzothiazole fragment in a chlorpyrifos molecule for the first time. The method is characterized in that radioactive isotope carbon-14 labeled benzene is used as a radioactive isotope raw material, and the target product carbon-14 labeled Dufulin is obtained by carrying out reactions such as benzene carboxylation, methylation, amination, cyclization, nucleophilic substitution and the like. The carbon-14labeled Dufulin disclosed by the invention can be used as a radioactive tracer, and is mainly used in research of metabolism and residue of Dufulin in organisms (plants, mammals and poultry) and in research of environmental behaviors of the Dufulin in soil and water bodies; and meanwhile, the invention establishes a preparation method of some carbon-14 containing synthetic building blocks.

Description

technical field [0001] The invention belongs to the field of radioactive chemical synthesis, and in particular relates to a radioactive isotope carbon-14 labeled poison fluorophos (N-[2-(4-methyl[phenyl-U- 14 C 6 ]Benzothiazolyl)]-2-amino-2-fluorophenyl-O, O-diethylmethylphosphonate) synthesis method. Background technique [0002] Dufulin (N-[2-(4-methylbenzothiazolyl)]-2-amino-2-fluorophenyl-O,O-diethylmethylphosphonate) was purchased from Guizhou University The new type of plant antiviral agent with intellectual property rights created by the Fine Chemical Research and Development Center was officially registered in China in December 2015. It belongs to fluorine-containing α-aminophosphonate compounds and is effective against tobacco, rice, cucumber and tomato. It has good control effect on viral diseases of plants. At present, studies on the absorption, distribution, transfer, residue of pentadophos in plants and its environmental behavior in water and soil are current...

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F9/6541C07B59/00
CPCC07B59/002C07B2200/05C07F9/6541
Inventor 杨征敏周兵见才广张贵华许亚军
Owner 浙江爱索拓标记医药科技有限公司
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