Method of fabricating [F-18]FEONM

Abstract

A PET imaging agent is made, by at first, washing out fluoride ions (F-18) adhered on an ion exchange resin to a reaction vessel with potassium carbonate/Kryptofix 2.2.2 in acetonitrile-water. After processing the first azeotropic distillation with helium while water is removed, the temperature is cooled down. Then, acetonitrile is added to the reaction vessel to be heated up. After processing the second azeotropic distillation with helium while water is removed, the temperature is cooled down and excess water is extracted. A precursor is then added to the reaction vessel to be heated up for processing a fluorination reaction. The reaction mixture obtained after the fluorination reaction is cooled down to be flown through a solid-phase extraction column with waste drained into a waste tank. Then, ethanol is used to wash out a product, i.e. [F-18]FEONM, adsorbed by the column, to be collected in a collection vial.

Claims

1. A method of fabricating FEONM, 2-(1-{6-[(2-2′-[F-18]Fluoroethoxyethyl)(methyl)amino]-2-naphthyl}ethylidene)malononitrile ([F-18]FEONM), comprising steps of: (a) washing out fluoride ions (F-18), being adhered on an ion exchange resin, with potassium carbonate/2.2.2 cryptand in acetonitrile-water into a reaction vessel; (b) heating said reaction vessel to be heated to a temperature of 75-115 celsius degrees (° C.), cooling said temperature down to 40-60° C. and excluding water after processing a first azeotropic distillation with helium; (c) adding acetonitrile to said reaction vessel to be heated to a temperature of 75-115° C., cooling said temperature down to 40-60° C. and excluding water after processing a second azeotropic distillation with helium; (d) adding a precursor to said reaction vessel to be heated to a temperature of 90-130° C. to process a fluorination reaction for 10-20 minutes to obtain a reaction mixture; and (e) after said fluorination reaction, cooling down a temperature of said reaction mixture to 40-60° C. followed by flowing said reaction mixture through a solid phase extraction column with waste drained into a waste tank and washing out a final product of [F-18]FEONM, being adhered on said column, with ethanol to be collected in a collection vial.

2. The method according to claim 1, wherein, in step (b), said fluorinating agent is fluoride ions (F-18)/potassium carbonate/2.2.2 cryptand.

3. The method according to claim 1, wherein, in step (d), said precursor has a formula as follows: ##STR00003##

4. The method according to claim 1, wherein, in step (e), said final product of [F-18]FEONM has a formula as follows: ##STR00004##

Description

BRIEF DESCRIPTION OF THE DRAWING(S)

(1) The present invention will be better understood from the following detailed description of the preferred embodiment(s) according to the present invention, taken in conjunction with the accompanying drawing(s), in which

(2) FIG. 1 is the flow view showing the preferred embodiment according to the present invention; and

(3) FIG. 2 is the view showing the fluorination reaction.

DESCRIPTION OF THE PREFERRED EMBODIMENT

(4) The following description of the preferred embodiment is provided to understand the features and the structures of the present invention.

(5) Please refer to FIG. 1 and FIG. 2, which are a flow view showing a preferred embodiment according to the present invention; and a view showing a fluorination reaction. As shown in the figures, the present invention is a method of fabricating [F-18]FEONM, comprising the following steps:

(6) (a) Ion exchange 11: Fluoride ions (F-18) adhered on an ion exchange resin are washed out into a reaction vessel with potassium carbonate/Kryptofix 2.2.2 in acetonitrile-water.

(7) (b) First azeotropic distillation 12: The reaction vessel that contains fluoride ions (F-18)/potassium carbonate/Kryptofix 2.2.2 in acetonitrile-water will be heated to a temperature of 95 celsius degrees (° C.). After the first azeotropic process is processed with helium and water is excluded, the temperature is cooled down to 50° C.

(8) (c) Second azeotropic distillation 13: Acetonitrile is added to said reaction vessel to be heated to a temperature of 95 Celsius degrees (° C.). After the second azeotropic distillation is processed with helium and water is excluded, the temperature is cooled down to 50° C.

(9) (d) Fluoridation reaction 14: A precursor 1 is added to said reaction vessel to be heated to a temperature of 110° C. to process a fluorination reaction for 15 minutes to obtain a reaction mixture. Therein, the precursor 1 has a formula as follows:

(10) ##STR00001##

(11) (e) Purification 15: A temperature of the reaction mixture obtained after the fluorination reaction is cooled down to 50° C., the reaction mixture will be passed through a solid phase extraction column for processing solid phase extraction (SPE) with waste drained into a waste tank. Then, ethanol is obtained to wash out a final product of [F-18]FEONM, being adhered on the column, to be collected in a collection vial. Therein, the final product of [F-18]FEONM has a formula as follows:

(12) ##STR00002##

(13) Thus, a novel method of fabricating [F-18]FEONM is obtained.

(14) To sum up, the present invention is a method of fabricating [F-18]FEONM, where [F-18]FEONM, a PET imaging agent for the diagnosis of Alzheimer's disease, can be easily produced with time saved and production efficiency improved.

(15) The preferred embodiment herein disclosed is not intended to unnecessarily limit the scope of the invention. Therefore, simple modifications or variations belonging to the equivalent of the scope of the claims and the instructions disclosed herein for a patent are all within the scope of the present invention.