Synthesis process of 18F lebeled positive electron radioactive tracer with ionic liquid as phase transfer catalyst

A technology of phase transfer catalyst and radioactive tracer, which is applied in radioactive carriers, organic chemical methods, chemical instruments and methods, etc. It can solve the problems of no water component and complicated labeling process, so as to improve work efficiency and shorten the synthesis process , the effect of improving the synthesis efficiency

Active Publication Date: 2007-01-03
郭启勇 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the current clinical 18 F-labeled positron radioactive tracers mainly use polyammonium fluoride (kryptofix / K + 18 f - ) as a phase transfer catalyst (phase transfer catalysis, PTC), the labeling process is relatively complicated, even if the most advanced fully automated positron radioactive tracer synthesis system is used, 18 The F-FDG synthesis process takes at least 25 minutes and requires strict drying techniques before and during the synthesis
Synthesis using polyammonium fluoride as a phase transfer catalyst 18 The biggest problem with F-labeled positron radioactive tracers is that there should be no water in the two steps of dehydration and labeling, which brings serious problems to routine clinical work, especially in areas with high air humidity in southern China.

Method used

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  • Synthesis process of 18F lebeled positive electron radioactive tracer with ionic liquid as phase transfer catalyst

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0078] 18 Synthesis steps of F-FDG:

[0079] 1. Will be transmitted from the accelerator 18 F ions and water pass to the receiving bottle (1-4Ci);

[0080] 2. will 18 F ions and water pass to the anion exchange column QMA;

[0081] 3. Use 0.15mL K 2 CO 3 (0.9mg)+0.2mL acetonitrile+0.3mL ionic liquid (BMI) was eluted from the QMA column 18 F ions are sent to the reaction bottle; heated at 65 degrees for 3.5 minutes under the protection of nitrogen or helium;

[0082] 4. Dissolve the precursor (1,3,4,6-tetra-O-acetyl-2-O-trifluromethanesulfonyl-D-mannopyanose (TATM), 25mg) in 0.7mL acetonitrile, mix well and then add to the reaction bottle ;Heating at 100°C for 5 minutes under the protection of nitrogen or helium;

[0083] 5. Lower the temperature to 90°C, add 2ml of water to the reaction flask, cool to 33°C, then add 1M 1mL NaOH for 1.5 minutes to hydrolyze to remove the acetyl protecting group (AcO - );

[0084] 6. Pass the solution through a special FDG alkali hydro...

Embodiment 2

[0089] 18 Synthetic steps of F-FLT:

[0090] 1. Will be transmitted from the accelerator 18 F ions and water pass to the receiving bottle (1-4Ci);

[0091] 2. will 18 F ions and water pass to the anion exchange column QMA;

[0092] 3. Use 0.15mL K 2 CO 3 (0.9mg)+0.2mL acetonitrile+0.3mL ionic liquid (BMI) was eluted from the QMA column 18 F ions are sent to the reaction bottle; heated at 65 degrees for 3.5 minutes under the protection of nitrogen or helium;

[0093] 4. The precursor (3-N-tert-Butoxycarbonyl-(5'-O-(4,4'-dimethoxytripphenylmethyl)-2'-deoxy-3'-o-(4-nitrobenzenesulfonyl)-β-D-threopentofuranosyl )thymine, 30mg) was dissolved in 0.7mL acetonitrile, mixed well and then added to the reaction bottle; heated at 130°C for 15 minutes under the protection of nitrogen or helium;

[0094] 5. Lower the temperature to 100°C, add 1.2mL of 1N HCI to the reaction flask to react for 2 minutes, cool to 33°C, then add 1M 1mL NaOH;

[0095] 6. Pass the solution through an HP...

Embodiment 3

[0100] 18 The synthetic steps of F-ethylcholine:

[0101] 1. Will be transmitted from the accelerator 18 F ions and water pass to the receiving bottle (1-4Ci);

[0102] 2. will 18 F ions and water pass to the anion exchange column QMA;

[0103] 3. Use 0.15mL K 2 CO 3 (0.9mg)+0.2mL acetonitrile+0.3mL ionic liquid (BMI) was eluted from the QMA column 18 F ions are sent to the reaction bottle; heated at 65 degrees for 3.5 minutes under the protection of nitrogen or helium;

[0104] 4. Dissolve the precursor (1,2-bis(tosyloxy)ethane, 20mg) into 0.7mL acetonitrile, mix well and then add to the reaction bottle; heat at 100°C for 15 minutes under the protection of nitrogen or helium;

[0105] 5. When the temperature drops to 33°C, add 2mL eluent into the reaction bottle;

[0106] 6. The solution passes through two series-connected anion exchange columns (characteristics of the columns, hydroxide type) and finally enters the high pressure liquid chromatography (HPLC) column. ...

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Abstract

The present invention belongs to the field of chemical synthesis, and is especially fluorinating and substituting reaction process for synthesizing 18F labeled positive electron radioactive tracer. The process includes the following steps: 1. transferring 18F ion from medical cyclotron and water to accepting bottle and leading to QMA column; 2. eluting 18F ion in QMA column with K2CO3, acetoitrile and ionic liquid, and heating 18F ion in a reactor bottle under protection of inert gas; 3. dissolving the precursor in acetonitrile and adding to the reactor bottle, and heating under protection of inert gas; 4. cooling, hydrolyzing and purifying the solution inside the reactor bottle; and 5. separating and collecting the target product from the solution. The process may adopt microwave heating. The present invention has the features of multipurpose, great yield, high efficiency, stable process, short synthesis period, low cost, etc.

Description

technical field [0001] The invention belongs to the field of chemical synthesis, in particular to a fluorination substitution reaction synthesis 18 F Method for labeling positron radioactive tracers. Background technique [0002] Positron nuclides produced by medical cyclotrons are currently used clinically 15 O. 13 N. 11 C. 18 F 18 F has a half-life of 110 minutes and has become the most clinically valued positron radionuclide. 18 F-labeled positron radiotracers are the most commonly used positron radiotracers for clinical PET / CT, PET and coincident line systems, 18 F-FDG, 18 F-FLT, 18 F-acetate, 18 F-choline, etc. as positive radiation tracers have been widely used in the early diagnosis, treatment plan formulation and curative effect observation of tumors, cardiovascular and nervous system diseases. However, the current clinical 18 F-labeled positron radioactive tracers mainly use polyammonium fluoride (kryptofix / K + 18 f - ) as a phase transfer catalyst (ph...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07B59/00C07H5/02C07H19/073C07C219/06C07D233/91C07C53/10C07C229/36C07D487/04C07D207/06C07J1/00C07D473/18A61K51/04A61K101/02
Inventor 郭启勇辛军
Owner 郭启勇
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