Method of fabricating [F-18]FEONM

Patent metadata

Field	Value
Publication number	US-9789207-B1
Application number	US-201615184129-A
Country	US
Kind code	B1
Filing date	Jun 16, 2016
Priority date	Jun 16, 2016
Publication date	Oct 17, 2017
Grant date	Oct 17, 2017

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.

First claim

What is claimed is:

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:

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

Assignees

• Inst Nuclear Energy Res Atomic Energy Council Executive Yuan Roc

Inventors

• Huang Li-Yuan
• Tu Yean-Hung
• Chen Jenn-Tzong
• Shiue Chyng-Yann

Classifications

• A61K49/0052 Primary

  Small organic molecules (oligomers, polymers, dendrimers A61K49/0054) · CPC title

• C07B2200/05

  Isotopically modified compounds, e.g. labelled · CPC title

• C07C255/09

  containing at least two cyano groups bound to the carbon skeleton · CPC title

• C07C253/30

  by reactions not involving the formation of cyano groups · CPC title

• A61K51/04

  Organic compounds · CPC title