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a synthetic 18 f-flt method

A 18F-FLT, 18F technology, applied in organic chemical methods, chemical instruments and methods, pharmaceutical formulations, etc., can solve the problems of slow drying speed, long time consumption, small evaporation area, etc., to save synthesis time, avoid product loss, The effect of improving the synthesis yield

Active Publication Date: 2020-05-19
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The existing thermal evaporation dehydration drying technology, due to the small evaporation area, the drying speed is slow, it takes a long time, and the drying 18 Reagent F agglomerates and blows off, which is not conducive to rapid mixing and full reaction with the labeled substrate
When drying the intermediate, similar agglomeration and blowing phenomenon will also occur, which is not conducive to the rapid mixing and full reaction of the reactants, and leads to product loss

Method used

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  • a synthetic <sup>18</sup> f-flt method
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  • a synthetic <sup>18</sup> f-flt method

Examples

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Effect test

Embodiment 1

[0033] Example 1 Preparation of inner wall modified glass microtubes

[0034] Sonicate a glass microtube with a length of 10 cm and an inner diameter of 1.5 mm in deionized water, ethanol, acetone, and deionized water for 10 min, then immerse in a concentrated sulfuric acid-hydrogen peroxide mixed solution (volume ratio 1:1) for ultrasonic treatment for 15 min, and place it for 1.5 h Afterwards, immerse in deionized water for ultrasonic cleaning for 10 minutes, repeat ultrasonication with deionized water twice, and dry in an oven at 120°C for 2 hours before use.

[0035] Add 0.408g cetyltrimethylammonium bromide to the round bottom flask, add 200mL deionized water and 1.2mL 2mol / L NaOH solution, stir and heat to 70°C, add 2mL tetraethyl orthosilicate (TEOS), stir Reaction 1h. The reaction solution was filled into glass microtubes and dried in an oven at 120 °C for 1 h. After sintering at 500°C for 2h in a muffle furnace, take it out. Immerse in deionized water and ultrasoni...

Embodiment 2

[0037] Example 2 Preparation of inner wall modified glass microtubes

[0038] Compared with Example 1, this example differs only in that the size of the glass microtube is 10 cm in length and 2 mm in inner diameter; other pretreatment and inner wall modification methods are the same. The morphology of the modified tube wall in this example is similar to Example 1.

Embodiment 3

[0039] Example 3 Preparation of inner wall modified glass microtubes

[0040] Compared with Example 1, this example differs only in that the size of the glass microtube is 10 cm in length and 2.5 mm in inner diameter; other pretreatment and inner wall modification methods are the same. The morphology of the modified tube wall in this example is similar to Example 1.

[0041] In the present invention, dry in the glass microtube of above-mentioned tube wall modification 18 The operation steps of F ion reagent are as follows:

[0042] will be transmitted from a medical cyclotron 18 The F ions and water pass to the receiving bottle. Start the automatic control system, the 18 F ions and water are passed to the anion exchange column (QMA), and the 18 F ions are enriched on the QMA column, while oxygen-enriched water is collected in the recovery bottle. Transfer 1 mL of K222 / K 2 CO 3 Acetonitrile / water solution (K222, 15mg / mL; K 2 CO 3 , 1.2mg / mL; the volume ratio of aceton...

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Abstract

The invention discloses a method for microtubule synthesis of 18F-FLT, and relates to quick and efficient preparation of a positive electron radioactive drug. The invention is characterized in that ina microtubule whose inner wall is modified, 18F ion reagent is quickly dried, and 18F replacement label and hydrolysis reaction are completed in the microtubule. Since the adsorption area of the inner wall of the modified microtubule is increased, 18F reagent solution injected into the microtubule is paved in the tube wall under the driving of air flow to form liquid film, evaporation area is increased, and meanwhile hot air flow is facilitated to pass from a hollow pipe so as to achieve quick drying. The adsorption effect of the tube wall can prevent the dried 18F reagent from caking and blowing away, and facilitates sufficient mixing with the reaction reagent. Two-step synthesis reaction of 18F replacement label and hydrolysis is completed in the microtubule, thereby saving time and improving synthesis yield of 18F-FLT.

Description

technical field [0001] The present invention relates to a synthesis method of positron radioactive medicine, in particular to an imaging agent for positron tomography (PET) diagnosis 18 F-3'-deoxythymidine ( 18 F-FLT) rapid synthesis method. Background technique [0002] PET (positron emission tomography, positron emission tomography) is a new non-invasive molecular imaging technology in nuclear medicine. It uses the principle of radioactive tracer and uses different radioisotope-labeled imaging agents (PET imaging agents). Sensitive display of physiological and biochemical changes in tissues and organs. The imaging agent is the key to PET and nuclear medicine. The imaging agent used in PET is radionuclide 11 C. 13 N. 15 O. 18 F and other labeled drugs, due to the short half-life of the radionuclide used, cannot be purchased and stored as commodities. Therefore, when performing PET imaging, it is necessary to label and synthesize the PET imaging agent as soon as possib...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07H19/06C07H1/00C07B59/00A61K51/04A61K101/02
CPCA61K51/0491C07B59/005C07B2200/05C07H1/00C07H19/06
Inventor 雷鸣张宏
Owner ZHEJIANG UNIV