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Simplified One Pot Synthesis of [18F]SFB for Radiolabeling

Technology Benefits

Reduces overall complexity of radiosynthesis Reduces the total probe synthesis time Increases specific activity of final probe Improves radiochemical yields Simplifies and speeds up purification process Ready to automate

Technology Application

Use of [18F]SFB to radiolabel a variety of biomolecules or small molecules to produce radiotracers for biological and medical applications Potential to develop a fully automated system to perform routine [18F]SFB production

Detailed Technology Description

UCLA researchers have developed a novel procedure to synthesize [¹⁸ F]SFB that reduces its inherent complexity, improves radiochemical yields, and reduces the overall reaction time. In contrast to other methods reported in literature, this new process is performed using only one reactor and one solid-phase extraction (SPE) cartridge for final purification. Most importantly, this simplified synthesis is ready to be automated. The development of an automated [¹⁸ F]SFB synthesizer is critical because it will enable many biologists and clinicians worldwide to label biomolecules of interest with fluorine-18 in order to facilitate fundamental biomedical research or drug development.

Supplementary Information

Patent Number: US8487077B2
Application Number: US13063741A
Inventor: Olma, Sebastian | Shen, Clifton Kwang-Fu
Priority Date: 16 Sep 2008
Priority Number: US8487077B2
Application Date: 29 Apr 2011
Publication Date: 16 Jul 2013
IPC Current: C07K000500
US Class: 530328 | 5303913
Assignee Applicant: The Regents of the University of California
Title: Simplified one-pot synthesis of [18F]SFB for radiolabeling
Usefulness: Simplified one-pot synthesis of [18F]SFB for radiolabeling
Summary: For preparing 18 F labeled compounds, preferably 4-[ 18 F]-N-succinimidyl fluorobenzoate ([ 18 F]-SFB) (claimed) useful as an injectable composition to locate abnormal tissue, especially tumors within an animal, including human body, using positron emission tomography.
Novelty: Preparing fluoro-radiolabeled compounds involves deprotecting alkyl/aryl 4-fluoro-radiolabeled fluorobenzoate in basic anhydrous/aprotic solvent to form fluoro-radiolabeled fluorobenzoate salt followed by coupling with activating agent

Industry

Biomedical

Sub Category

Medical Imaging

Application No.

8487077

Others

State of Development

The invention is at the stage of routine use in the inventors laboratories. The current synthesis can be performed reliably.

Background

In the last two decades, N-succinimidyl-4-[¹⁸F]fluorobenzoate ([¹⁸F]SFB) has been used as a radiolabeling tag for small molecules, peptides, proteins, and other biomolecules to yield radiotracers. These radiotracers can be used for in vitro or in vivo biological assays, such as binding studies or positron emission tomography (PET). An obstacle that prevents this labeling procedure from being widely used is that the radiosynthesis of [¹⁸F]SFB is time-consuming and complex. Multiple reaction vessels and several steps are necessary to produce the final tracers. Therefore, there is a need for a simplified synthesis of [¹⁸F]SFB that can increase radiochemical yield and facilitate automation.

Tech ID/UC Case

20363/2009-136-0

Related Cases

2009-136-0

*Abstract

UCLA investigators in the department of Biological Chemistry have developed a high throughput screen to test for novel tyrosine kinase inhibitors that target regulatory protein binding. This assay has the potential to identify lead compounds to treat chronic myelogenous leukemia and other cancers dependent on tyrosine kinase signaling.

*IP Issue Date

Jul 16, 2013

*Principal Investigator

Name: Sebastian Olma

Department:

Name: Kwang Fu Shen

Department:

Country/Region

USA