METHOD FOR PREPARING LIQUID COMPOSITION OF COMPOUND I AND USE THEREOF IN MYOCARDIAL METABOLISM PET IMAGING

Title:

METHOD FOR PREPARING LIQUID COMPOSITION OF COMPOUND I AND USE THEREOF IN MYOCARDIAL METABOLISM PET IMAGING

Document Type and Number:

WIPO Patent Application WO/2023/246830

Kind Code:

A1

Abstract:

The present application provides a method for preparing a myocardial metabolism PET imaging agent, a liquid composition of trans-2-(2-(5-fluoro[18F]tridecyl)cyclopropyl)acetic acid (compound I for short), and use thereof, wherein a crude product containing compound I is purified by high performance liquid chromatography; wherein the mobile phase used in the high performance liquid chromatography purification step comprises ethanol and water. The present application optimizes the experimental process and adjusts the amount of compound I tert-butyl ester precursor to shorten the reaction time required to achieve the same labeling rate, and increases the radioactivity of the initial 18F ions to increase the labeling rate, thereby increasing the yield.

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Inventors:

WANG YUE (CN)
ZHANG YING (CN)
ZHANG AILI (CN)
XU XINSHENG (CN)

Application Number:

PCT/CN2023/101561

Publication Date:

December 28, 2023

Filing Date:

June 21, 2023

Export Citation:

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Assignee:

SINOTAU PHARMACEUTICALS GROUP (CN)

International Classes:

C07C51/09; A61K51/04; C07B59/00; C07C51/47; C07C53/23; C07C67/307; C07C69/635; A61K101/02

Domestic Patent References:

WO2004093650A2

2004-11-04

Foreign References:

CN107198780A	2017-09-26
CN112386949A	2021-02-23
CN101918042A	2010-12-15
US20040253177A1	2004-12-16
CN109200296A	2019-01-15
CN108884083A	2018-11-23
CN112807276A	2021-05-18
CN114773179A	2022-07-22

Other References:

SHOUP TIMOTHY M, ELMALEH DAVID R, BONAB ALI A, FISCHMAN ALAN J: "Evaluation of trans-9-18 F-Fluoro-3,4-Methyleneheptadecanoic Acid as a PET Tracer for Myocardial Fatty Acid Imaging", THE JOURNAL OF NUCLEAR MEDICINE, vol. 46, no. 2, 1 February 2005 (2005-02-01), pages 297 - 304, XP093121313

Attorney, Agent or Firm:

BEIJING CAI HE LAW FIRM (CN)

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