2-metridazloe derivative as well as application and preparation method thereof

Abstract

The invention discloses a radioactive drug and a preparation method thereof. The compound is fluo-polyethylene glycol-triazole ring-methylene-2metridazloe, and the structural general formula of the compound is disclosed in the specification, wherein n is 1-10, and F is 18F. The preparation method comprises the following steps of: adding 2-metridazloe, propargyl bromide and K2CO3 to CH3CN; heating for refluxing; adding a product obtained after sufficient reaction, a product obtained by adding di-p-tolyl-sulphonate of polyethylene glycol and NaN3 to DMF (Dimethyl Formamide) and heating with boiled water, CuI and Et3N to THF (Tetrahydrofuran); and finally carrying out a clink reaction on the two products to finally obtain a [18F]FPEGn-TAN solution.

Description

technical field The invention relates to radiopharmaceuticals and a preparation method thereof, in particular to a class of radioactive 2-nitroimidazole derivatives and a preparation method thereof. Background technique Cardiovascular disease, malignant tumor (cancer), and cerebrovascular disease occupy the top ten list of the world's top ten deadly diseases. As far as tumor treatment is concerned, satisfactory results are still not achieved. Hypoxia means that the oxygen concentration of the tissue is between normal and anaerobic, and the function is abnormal without obvious morphological changes. It is an important feature of many major diseases and widely exists in cardiovascular diseases, tumors, and cerebrovascular diseases. In serious diseases such as diseases, the determination of tissue oxygen level is of great significance for the clinical treatment of these diseases. The most important application value of radiopharmaceuticals is the study of biochemical changes...

AI Technical Summary

Problems solved by technology

Hypoxic tissues that have been reported in the literature so far 18 Most F-PET imaging agents are 2-nitroimidazole derivatives, including 18 FMISO, 18 FETNIM, 18 FETA, 18 F-EF5, 18 F-EF3, 18 F-EF1, 18 FRP-170, 18 FAZA etc. (show 1), wherein 18 FMISO has been widely used in clinical research, but 18 The clinical imaging performance of FMISO is not ideal. The main problems include high uptake in normal background tissue, slow non-specific binding and clearance, resulting in a long time interval between injection and imaging, and neurotoxicity.

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