Synthesis of 18F-labeled tracers in hydrous organic solvents
First Claim
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1. A method for synthesizing an 18F-labeled probe the method comprising:
- (1) eluting an amount of 18F with a first solvent comprising a predetermined amount of water and at least one organic polar aprotic solvent, but no organic erotic solvents, the 18F eluting as an 18F solution, the predetermined amount of water being in a range of about 0.1 vol % to about 5.0 vol %; and
(2) using the 18F solution to perform 18F-labeling in the presence of at least one labeling reagent and at least one phase transfer catalyst so as to generate the 18F-labeled probe;
wherein the at least one labeling reagent comprises K2CO3, KHCO3, Cs2CO3, potassium mesylate, potassium oxylate, or tetrabutylammonium bicarbonate;
wherein the water content of the 18F solution during 18F-labeling is in a range of about 0.1 vol % to about 2.0 vol %; and
wherein there is no step of drying the 18F solution starting from a time when the eluting is performed and ending at a time when the 18F-labeling is performed.
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Abstract
A method for synthesizing an 18F-labeled probe. The method includes a step of eluting an amount of 18F with a first solvent which includes a predetermined amount of water and at least one organic solvent. In this step, the 18F elutes as an 18F solution. The method also includes a step of using the 18F solution to perform 18F-labeling in the presence of at least one labeling reagent and at least one phase transfer catalyst so as to generate the 18F-labeled probe. In the method, there is no step of drying the 18F starting from a time when the eluting step is performed and ending at a time when the 18F-labeling step is performed.
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Citations
16 Claims
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1. A method for synthesizing an 18F-labeled probe the method comprising:
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(1) eluting an amount of 18F with a first solvent comprising a predetermined amount of water and at least one organic polar aprotic solvent, but no organic erotic solvents, the 18F eluting as an 18F solution, the predetermined amount of water being in a range of about 0.1 vol % to about 5.0 vol %; and (2) using the 18F solution to perform 18F-labeling in the presence of at least one labeling reagent and at least one phase transfer catalyst so as to generate the 18F-labeled probe; wherein the at least one labeling reagent comprises K2CO3, KHCO3, Cs2CO3, potassium mesylate, potassium oxylate, or tetrabutylammonium bicarbonate; wherein the water content of the 18F solution during 18F-labeling is in a range of about 0.1 vol % to about 2.0 vol %; and wherein there is no step of drying the 18F solution starting from a time when the eluting is performed and ending at a time when the 18F-labeling is performed. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8)
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9. A method for synthesizing an 18F-labeled probe the method comprising:
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(1) eluting an amount of 18F with a solution comprising; (a) a first solvent comprising a predetermined amount of water and at least one organic aprotic solvent, but no organic protic solvents; and (b) at least one labeling reagent comprising K2CO3, KHCO3, Cs2CO3, potassium mesylate, potassium oxylate, or tetrabutylammonium bicarbonate; and (c) at least one phase transfer catalyst; the 18F eluting as an 18F solution, wherein a total amount of water in the 18F solution is in a range of about 0.1 vol % to about 5.0 vol %; and (2) diluting the 18F solution with the organic solvent so as to provide an 18F-labeling solution having a total amount of water in the range of about 0.5 vol % to about 1.5 vol %; (3) using the 18F solution to perform 18F-labeling so as to generate the 18F labeled probe; wherein there is no step of drying the 18F solution starting from a time when the eluting is performed and ending at a time when the 18F-labeling is performed. - View Dependent Claims (16)
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10. A method for synthesizing an 18F-labeled probe the method comprising:
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(1) eluting an amount of 18F with a solution comprising; (a) a first solvent comprising a predetermined amount of water, no organic protic solvents, and at least one organic aprotic solvent, selected from acetonitrile, tetrahydrofuran (“
THF”
), dimethylformamide (“
DMF”
), N methylpyrrolidone (“
NMP”
), and dioxane; and(b) at least one labeling reagent comprising K2CO3, KHCO3, Cs2CO3, potassium mesylate, potassium oxylate, or tetrabutylammonium bicarbonate; and (c) at least one phase transfer catalyst; the 18F eluting as an 18F solution, wherein a total amount of water in the 18F solution is in a range of about 0.1 vol % to about 5.0 vol %; (2) diluting the 18F solution with the organic solvent so as to provide an 18F-labeling solution having a total amount of water in the range of about 0.1 vol % to about 2.0 vol %; (3) using the 18F solution to perform 18F-labeling so as to generate the 18F labeled probe; and wherein there is no step of drying the 18F starting from a time when the eluting is performed and ending at a time when the 18F-labeling is performed. - View Dependent Claims (11, 12, 13, 14, 15)
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Specification