<18>F-labeled fluoropyridylformylglycine, and preparation method and application thereof

Abstract

The invention provides an <18>F-labeled fluoropyridylformylglycine, and a preparation method and an application thereof, and belongs to the technical field of radioactive medicinal chemistry. The <18>F-labeled fluoropyridylformylglycine is 6-[<18>F]-fluoro-3-pyridylformylglycine, 5-[<18>F]-fluoro-2-pyridylformylglycine or 4-[<18>F]-fluoro-2-pyridylformylglycine. The <18>F-labeled fluoropyridylformylglycine provided by the invention has an excellent stability and good biological properties, and has no adverse effects on organisms after decaying. Results of in-vivo distribution test show that the <18>F-labeled fluoropyridylformylglycine is mainly taken in by the kidney and immediately excreted, and the <18>F-labeled fluoropyridylformylglycine is almost completely discharged into the bladder10 min after being injected into a mouse, so the <18>F-labeled fluoropyridylformylglycine is particularly advantageous for the renal function evaluation of renal lesions.

Description

technical field [0001] The invention relates to the technical field of radiopharmaceutical chemistry, in particular to a 18 F-labeled fluoropicolilylglycine, its preparation method and application. Background technique [0002] Positron emission tomography (PET) technology is an important means of diagnosing diseases based on the molecular level. Due to its good spatial resolution and quantitative analysis advantages, it has been widely used and affirmed in clinical and scientific research. However, at present, the equipment for imaging the urinary system in the field of nuclear medicine still stays on SPECT, and the main imaging agent is still 99m Tc-DTPA and 99m Tc-MAG3. 99m Since Tc-DTPA is almost completely excreted from the plasma through the glomerulus, its main function is to determine the glomerular filtration rate (GFR) clinically. However, due to the limitations of SPECT imaging equipment, the clinical determination of GFR is not very accurate. Part of the reas...

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Problems solved by technology

but 99m Tc-MAG3 with 131 I-OIH is similar in terms of renal imaging, unable to obtain high-quality renal images

Therefore, compared with PET / CT, the above SPECT techniques using corresponding imaging drugs are incomparable in terms of imaging quality and precise quantitative analysis.

Based on the above reasons, many experts and scholars at home and abroad are committed to developing a new type of imaging agent with biological properties suitable for renal PET / CT scanning, in order to replace the shortcomings of traditional imaging equipment and imaging agents for kidney imaging. then 15 O-H 2 O. 13 N-NH 3 , 82 Rb-Rb 1 , 62 CuCu(II)pyruvaldehydebis-(N-4-methylthiosemicarbazonato), 62 Cu-Cu(II)ethylglyoxal bis(thiosemicarbazone), 68 Ga-Ga-ethylenediaminetetraacetic acid, 55 Co-Co-ethylenediamine tetraacetic acid and 18 Positron imaging agents such as F-NaF have been applied one after another, but due to the short half-life or high cost of these imaging agents, they have not been really used clinically to serve patients.

In recent years, Vibhudutta Awasthi et al. have developed a new kidney imaging agent p- 18 F-fluorohippurate ( 18 F-PFH), this imaging agent has ideal biological characteristics, it is almost excreted by the urinary system, and 131 Compared with I-OIH, it shows a higher kidney / background ratio, and does not go through the metabolism of the liver and biliary system, and the uptake of other tissues and organs except the kidney is relatively low, and the imaging effect of the kidney is quite ideal, but 18 F-PFH synthesis steps are cumbersome and take a long time, resulting in a decline in yield

Based on the above research results, Vibhudutta Awasthi et al. have developed another imaging agent with similar structure 18 F-CNPFH, compared to 18 The synthesis steps of F-PFH are relatively simple, but due to the metabolism of the imaging agent in the liver and biliary system, the background around the kidney is relatively high, and the imaging effect is not very ideal

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