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 the reaction. In order to remove this K222, the prior art uses HPLC purification methods, which are cumbersome and take a long time. The half-life of F-18 is about 110 minutes, prolonging the reaction time will reduce the synthesis efficiency; (3) In addition, when using preparative HPLC separation, there will be more radioactivity loss on the column, which reduces the synthesis efficiency and the workload is heavy, so it is not suitable for promotion.

Images