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A microfluidic synthesis 18 f-fmiso method

A 18F-FMISO and microfluidic technology, applied in the direction of organic chemistry, can solve the problems of slow drying speed, long time consumption, unfavorable reactant mixing and full reaction, so as to avoid product loss, improve synthesis yield and avoid crossover pollution effect

Active Publication Date: 2020-06-30
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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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
In addition, existing 18 The fluorination and hydrolysis during the synthesis of F-FMISO are carried out in two reactors respectively, and it takes time to transfer intermediates

Method used

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  • A microfluidic synthesis <sup>18</sup> f-fmiso method
  • A microfluidic synthesis <sup>18</sup> f-fmiso method
  • A microfluidic synthesis <sup>18</sup> f-fmiso method

Examples

Experimental program
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Effect test

Embodiment 1

[0033] The preparation of embodiment 1 inner wall modification glass microtube

[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...

Embodiment 2

[0037] The preparation of embodiment 2 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] The preparation of the inner wall modified glass microtube of embodiment 3

[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 ra...

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Abstract

The invention discloses a method for synthesizing 18F-FMISO through microfluidic and relates to a photographic developer for quickly and efficiently preparing positron emission tomography (PET). The method is characterized in that a 18F ion reagent is quickly dried in a micro-tube with a modified inner wall, and 18F mark substitution and hydrolysis reactions are completed in the micro-tube. The adsorption area is increased through the modified inner wall of the micro-tube, the 18F reagent solution injected into the micro-tube is laid on the tube wall under push of air flow to form liquid film,the evaporation area is increased, hot air flow conveniently passes through a hollow pipe, quick drying is achieved, and the dried 18F reagent can be prevented from caking and being blown away through the adsorption effect of the tube wall, which helps to sufficiently mix the 18F reagent with a reaction reagent; the two-step 18F mark substitution and hydrolysis synthetic reactions are completed in the same micro-tube in sequence, the total synthetic operation time is shortened, and the synthetic yield of 18F-FMISO is increased.

Description

technical field [0001] The invention relates to a synthesis method of a positron radioactive drug, in particular to an imaging agent used in the diagnosis of anoxic tissue positron tomography (PET) 18 F-flumisonidazole ( 18 F-FMISO) 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...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D233/91C03C23/00
CPCC03C23/0095C07D233/91
Inventor 雷鸣张宏
Owner ZHEJIANG UNIV