Novel radioactive labeling method for fluoboric acid compound

Abstract

The invention discloses a novel radioactive labeling method for a fluoboric acid compound. The method comprises the following steps: (1) adopting a proton circular accelerator for performing <18>O(p, n)<18>F reaction and generating <18>F<->; (2) transmitting <18>F<-> into an anion exchange column QMA through a pipeline, thereby capturing by QMA; (3) drying the QMA by blowing N2 and then concentrating and eluting the <18>F<-> with hydrochloric acid and sodium chloride solution till entering into a reaction flask; (4) performing ion exchange reaction on [<19>F] fluoboric acid compound, ethanol solution and the concentrated <18>F<-> at 90 DEG C, and then adding 5mL deionized water into an ion exchange reaction system and performing quenching reaction; and (5) purifying the reaction system through a neutral Al2O3 column, and then dropping into 5mL disodium hydrogen phosphate-citrate buffer solution with pH=7, thereby acquiring [<18>F] fluoboric acid compound solution. According to the invention, the hydrochloric acid and sodium chloride solution are firstly adopted for eluting and concentrating <18>F<->, the eluting efficiency of the <18>F<-> can be guaranteed and the acidic condition in reaction can be guaranteed; the safety factor is high; the residue of organics, such as, polyether polyamine and acetonitrile, need not be checked; the fluoboric acid compound solution can be directly used as an injection solution; the operation is simple; the purification is fast; and the product yield is high.

Description

technical field [0001] [ 18 F] Radiolabeling method. Background technique [0002] Amino acids are essential nutrients for tumor proliferation, and radiolabeling of amino acid compounds to achieve specific imaging of tumors has become a research hotspot in recent years. Only due to the particularity of amino acid structure, traditional radiolabeling methods such as Al 18 F. 68 Ga, 99m Tc, etc. will make relatively large changes to the original molecular structure, which will easily lead to differences in the metabolic behavior of the labeled molecule in vivo. [0003] Fluoroboric acid structure is a structure very similar to α-amino acid structure. Studies have shown that the pharmacokinetic behavior of the compound after replacing the α-amino acid structure with fluoboric acid structure is very similar to that of the original amino acid, so it is possible to replace amino acid compounds with fluoboric acid compounds Radiolabeling is performed for imaging studies of tum...

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