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Synthesis process of 18F labeled 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 inability to have water components, insoluble polypeptides or proteins, etc., and achieve good specificity Sexual affinity, significant economic and social benefits, simple preparation process

Active Publication Date: 2009-11-18
郭启勇 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Synthesis Using Polyammonium Fluoride as 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. In addition, not only polyammonium fluoride as a phase transfer catalyst needs to provide an additional nucleophilic substitution reaction medium to complete the reaction process, but also polypeptides or proteins cannot be dissolved in organic solvents so that they cannot be completed in one step 18 Synthesis of F-labeled peptide or protein positron radiotracers

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0075] [ 18 F]FB-HYNIC-E-[c[RGDyK] 2 ] The synthesis steps:

[0076] 1. Will be transmitted from the medical cyclotron 18 F ions and water pass to the receiving bottle (1-4Ci);

[0077] 2. Will 18 F ions and water pass to the anion exchange column QMA;

[0078] 3. Using 0.15mL K 2 CO 3 (0.9mg)+0.2mL acetonitrile+0.3mL ionic liquid ([BMIm][OTf]) was eluted from the QMA column 18 F ion and sent to the reaction flask, 4-Formy]-N, N, N-trimethylanilinium triflate 5mg dissolved in 0.5mL DMSO mixture was added to the reaction flask; under the protection of nitrogen or helium, heated at 65 degrees for 3.5 minutes, 90 Heating at 100°C for 10 minutes;

[0079] 4. The precursor (HYNIC-E-[c[RGDyK] 2 ], 2 mg) dissolved in Na 2 HPO 4 Buffer solution (pH8.5), mix thoroughly before adding to the reaction bottle; heat at 65°C for 25 minutes under the protection of nitrogen or helium;

[0080] 5. Cool the temperature to 35°C, then add HCl (1N, 0.5ml) solution into the reaction flas...

Embodiment 2

[0086] [ 18 F] Synthetic steps of FB-RGD:

[0087] 1. Will be transmitted from the medical cyclotron 18 F ions and water pass to the receiving bottle (1-4Ci);

[0088] 2. Will 18 F ions and water pass to the anion exchange column QMA;

[0089] 3. Using 0.15mL K 2 CO 3 (0.9mg)+0.2mL acetonitrile+0.3mL ionic liquid ([BMIm][OTf]) was eluted from the QMA column 18 F ion and sent to the reaction bottle, the mixture of 4-Formyl-N, N, N-trimethylanilinium triflate 5mg dissolved in 0.5mL DMSO was added to the reaction bottle; under the protection of nitrogen or helium, heated at 65 degrees for 3.5 minutes, 90 degrees Heating at low temperature for 10 minutes;

[0090] 4. Dissolve the precursor (c[RGDyK], 2 mg) in Na 2 HPO 4 Buffer solution (pH8.5), mix thoroughly before adding to the reaction bottle; heat at 65°C for 25 minutes under the protection of nitrogen or helium;

[0091] 5. Cool the temperature to 33°C, then add HCl (1N, 0.5ml) solution into the reaction flask;

[...

Embodiment 3

[0097] [ 18 F] Synthetic steps of Galacto-RGD:

[0098] 1. Will be transmitted from the medical cyclotron 18 F ions and water pass to the receiving bottle (1-4Ci);

[0099] 2. Will 18 F ions and water pass to the anion exchange column QMA;

[0100] 3. Using 0.15mL K 2 CO 3 (0.9mg)+0.2mL acetonitrile+0.3mL ionic liquid ([BMIm][OTf]) was eluted from the QMA column 18 F ion and sent to the reaction bottle, the mixture of 4-Formyl-N, N, N-trimethylanilinium triflate 5mg dissolved in 0.5mL DMSO was added to the reaction bottle; under the protection of nitrogen or helium, heated at 65 degrees for 3.5 minutes, 90 degrees Heating at low temperature for 10 minutes;

[0101] 4. Dissolve the precursor (cyclo(-Arg-Gly-Asp-D-Phe-Lys(SAA), 2mg) in 0.5mL DMSO and mix thoroughly before adding to the reaction flask, and then add 1M 0.5mLNaOH; Or heated at 70 degrees for 15 minutes under the protection of helium;

[0102] 5. Cool the temperature to 33°C, then add HCl (1N, 0.5ml) soluti...

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Abstract

The invention belongs to the field of chemical synthesis, and in particular relates to a method for synthesizing 18F labeled positron radioactive tracers using ionic liquids as phase transfer catalysts, which can be carried out in sequence as follows: 1) Transfer 18F ions from an accelerator to a receiving bottle and introduced into an anion exchange column; 2) using strong base and weak acid salt, acetonitrile and ionic liquid to elute the 18F ion in the column and send it to the reaction flask. 4-Formyl-N, N, N-trimethylaniliniumtriflate and DMSO mixture are also added to the reaction flask and heated; 3) the precursor is dissolved in acetonitrile and added to the reaction flask for heating; 4) lower the temperature and adjust the pH 5) the target product of the solution obtained in step 4) is separated and collected. The invention has the characteristics of multi-purpose, large output, high efficiency, short synthesis time and low cost.

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 peptide and protein positron radiotracers. 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,[1 8 F] FDG, [ 18 F] FLT, [ 18 F] acetate, [ 18 F] Choline, etc. as positive radiation tracers have been widely used in the early diagnosis of tumors, cardiovascular and nervous system diseases, treatment plan formulation and curative effect observation. However, currently 18 F-labeled polypeptide or protein-based positron radiotracers are rarely used in clinical practice, especially 18 F-la...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07B59/00C07K7/64C07K16/00C07K19/00C07K14/00A61K51/08A61K51/10A61K101/02
Inventor 郭启勇辛军
Owner 郭启勇
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