Process for preparing 18F-FLT and self-contained reagent kit

Abstract

The invention relates to a process for preparing 18F-FLT and a self-contained reagent kit, relating to the preparation of positron medicine and a reagent kit thereof and belonging to the technical field of radiopharmaceuticals and nuclear medicine. The process comprises the following steps of: a, catching 18F- generated by an accelerator by using a QMA column, then leaching the 18F- on the QMA column into a reaction tube by using quaternary ammonium salt TEABC (Triethyl Ammonium Bicarbonate) or a TBAHCO3 (Tetrabutylammonium Hydrogen Carbonate) solution; b, dehydrating the obtained 18F- after being leached in the step a; c, dissolving a precursor MTR-Nos-Boc-LT of 18F-FLT through a protic solvent, and adding into the 18F- obtained in the step b to carry out a nucleophilic fluorination reaction; d, hysrolyzing a nucleophilic fluoride product obtained in the step c through a hydrochloric acid solution, and neutralizing through an alkaline buffer solution; and e, edulcorating a neutralized liquid obtained in the step d to obtain a product 18F-FLT. Compared with the traditional synthesis technology, the process provided by the invention is a 18F-FLT synthesis technology with high efficiency, high stability and high purity, and can be used for making novel 18F-FLT and other positron medicine synthesis modules.

Description

technical field [0001] The invention relates to the preparation of positron medicine and its kit, and belongs to the technical field of radiopharmaceuticals and nuclear medicine. Background technique [0002] Positron emission tomography (PET) is a cutting-edge technology in modern biomedicine. It can display the cell metabolism, cell function, and cell proliferation of the body and lesion tissue at the molecular level. It is a favorable tool for diagnosing tumors and evaluating the biological characteristics of tumors. The commonly used PET tracer is 18F-FDG, but it mainly reflects the glucose metabolism in the body and cannot detect tumors with high specificity and selectivity, and 18F-FDG cannot distinguish between tumors and inflammation. In contrast, imaging DNA synthesis pathways can detect changes in tumor cell proliferation and distinguish tumors from inflammation, allowing tumor-specific diagnosis. [0003] 18F-FLT is a thymidine analog, which can enter human cells...

AI Technical Summary

Problems solved by technology

[0007] However, there are obvious deficiencies in the existing synthesis process of 18F-FLT: (1) The synthesis efficiency is generally low. In order to improve the synthesis efficiency, the amount of precursor required is large (30-40mg mostly) and the reaction is slow, while the 18F-FLT The precursor is expensive, and increasing the amount of the precursor will increase the synthesis cost; (2) K222, which is highly toxic, needs to be added to t...

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