2-18F-2-deoxidized-D-glucose synthesis process

Abstract

The invention relates to synthesis technique for common radioactive drug, 2-18F-2- deoxidized -D- glucose (18F-FDG) in PET technique, which comprises: (a) trapping the 18F on column; (b) preparing nucleophilic substitution; (c) nucleophilic fluorinating; (d) trapping the intermediate on column; (e) solid-phase basic hydrolysis; (f) neutralizing and separating. This method can be used in prior main devices, such as TRACERlab FXF-N and TRACERlab Fx FDG; this technique is more rapid, high-effect, and reliable, and can also be used to manufacture new composed module for 18F-FDG.

Description

technical field [0001] The present invention relates to the application field of PET (Positron Emission Tomography, positron emission tomography), be specifically related to the most commonly used radiopharmaceutical 2- 18 F-2-deoxy-D-glucose ( 18 F-FDG) synthesis process. Background technique [0002] PET (Positron Emission Tomography, Positron Emission Tomography) uses the principle of photon collimation and r-scintillation detection technology to detect the photons of annihilation radiation produced by the tracer in vitro. Tomographic images and quantitative physiological parameters are given. At present, PET has become a very important diagnostic tool in clinical work, especially in the early diagnosis of cancer and brain functional imaging. irreplaceable role. [0003] PET imaging must have a positron-emitting radioactive tracer, and its image quality and clinical examination items depend on the quality and type of positron-emitting radiopharmaceuticals. 2- 18 F-2...

AI Technical Summary

Problems solved by technology

But this synthetic technique also has the following disadvantages: (1) due to the need to buy a complete set of raw material kits, especially the need to buy a complete set of separation and purification columns imported at high prices, the production cost is expensive

(2) Accelerator production includes 18 f - Target water, which needs to be transferred to an Erlenmeyer vial before being transferred to a Sep-Pak QMA cartridge, resulting in a small 18 f - loss of radioactivity, and increases the overall synthesis time, and is inconvenient to observe the QMA cartridge trapped 18 f - activity

(3) The total synthesis time is longer, about 28 minutes

The synthesis system simplifies the hydrolysis process, after hydrolysis, no heating and evaporation is required to remove acetonitrile, and high enantiopurity and high radiochemical yield can be obtained. 18 F-FDG, but still has the following disadvantages: (1) need to add acetonitrile logical N several times before the fluorination reaction 2 Azeotropic water removal

(2) After the fluorinated intermediate needs to be mixed with a large amount of water (greater than 25mL), pass through the Sep Pak Plus t The C18 cartridge traps the fluorinated intermediate and rinses with a large amount of water (greater than 20mL) to remove acetonitrile, toxic K222 and unreacted 18 f - , resulting in the loss of a certain amount of fluorinated intermediates, and the toxic substance K222 cannot be completely removed, which brings trouble to the operation and increases the synthesis time

(3) No cation exchange column (H + Type) In addition to the toxic substance K222, the resulting injection may contain trace amounts of K222

(4) The synthesis time is still relatively long, and the shortest is about 23 minutes

(5) Due to the need to purchase a complete set of raw material kits and synthetic sets of plates, the production cost is expensive

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