Synthesis method of radioactive isotope carbon-14 labeled Dufulin

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 radiochemical synthesis, and in particular relates to a radioactive isotope carbon-14 labeled poisonous fluorophos ( N -[2-(4-Methyl[phenyl-U- 14 C 6 ]Benzothiazolyl)]-2-amino-2-fluorophenyl- O , O - the synthetic method of diethylmethyl phosphonate). Background technique [0002] Dufulin (Dufulin, N -[2-(4-Methylbenzothiazolyl)]-2-amino-2-fluorophenyl- O , O -Diethylmethylphosphonate) is a new type of plant antiviral agent with intellectual property rights created by the Fine Chemical Research and Development Center of Guizhou University. It was officially registered in China in December 2015. It belongs to fluorine-containing α-aminophosphine Ester compounds have good control effects on viral diseases of plants such as tobacco, rice, cucumber and tomato. At present, studies on the absorption, distribution, transfer, residue of pentadophos in plants and its environmental behavior in water and soil are cu...

AI Technical Summary

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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