Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

N-(2-fluoro [18F] ethyl) dopamine developer and preparation method thereof

A dopamine and imaging agent technology, applied in the field of N-dopamine imaging agent and its preparation, can solve the problems of difficult synthesis, low yield, high cost, etc., and achieve stable synthesis yield, good repeatability, and strong affinity Effect

Pending Publication Date: 2021-09-28
何玉林
View PDF1 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since the synthesis of 6-18F-Fluourodopamine requires special equipment, the cost of electrop

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • N-(2-fluoro [18F] ethyl) dopamine developer and preparation method thereof
  • N-(2-fluoro [18F] ethyl) dopamine developer and preparation method thereof
  • N-(2-fluoro [18F] ethyl) dopamine developer and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Embodiment 1: One, N-(2-fluoro [18F] ethyl) dopamine imaging agent and preparation method thereof

[0044] An N-(2-fluoro[18F]ethyl) dopamine imaging agent, characterized in that: the chemical structural formula of the imaging agent is shown in formula (I):

[0045] .

[0046] The preparation method of the N-(2-fluoro[18F]ethyl)dopamine imaging agent is characterized in that: the preparation method specifically comprises the following steps:

[0047] (1) The fluoride ion (18F-) produced by the cyclotron is introduced into the chemical synthesizer and captured on the anion trap column (QMA), and the 18F- is eluted with K2CO3 / K2.2.2 solution to the reaction tube, and then added to dry acetonitrile to azeotrope remove water;

[0048] (2) Add 1 mL of acetonitrile solution containing 5-10 mg of 1,2-bis(p-toluenesulfonyloxy)ethane with the structural formula shown in formula (II) and react at 85-105°C for 5-10 minutes, and cool the reaction solution to 60 ℃;

[0049] ...

Embodiment 2

[0063] Embodiment 2: two, 18 Biodistribution of F-FEDA

[0064] 18 The biological distribution characteristics of F-FEDA meet the requirements as an imaging agent, which is illustrated by the organ distribution experiment in mice.

[0065] Take 30 Kunming mice, half male and half male, and randomly divide them into 5 groups, 6 mice in each group, and inject the filtrate filtered by sterile membrane respectively, namely 18 F-FEDA 7.4MBq (volume ≤ 0.2mL), a group of animals were killed at 2, 10, 20, 30, 60min total 5 time points, heart, lung, liver, spleen, kidney, stomach, intestine, brain, Weigh 11 major organs such as muscle, bone, and blood, measure the radioactive count with a gamma counter, and calculate the percent injection dose rate per gram of tissue (%ID / g, radioactive count per gram of tissue or organ / injected into mice) Total radioactivity count × 100%).

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The invention relates to an N-(2-fluorine [18F] ethyl) dopamine developer and a preparation method thereof. The preparation method comprises the following steps: (1) transferring fluorine ions (18F <->) produced by a cyclotron into a chemical synthesizer, capturing in anion capturing, eluting, adding acetonitrile, and azeotropic to remove water; (2) adding an acetonitrile solution as shown in a formula (II) to react; (3) adding a dimethyl sulfoxide solution of dopamine to react; and (4) performing high-performance liquid phase separation and purification, and collecting the required radioactive component N-(2-fluorine [18F] ethyl) dopamine. The developer has strong affinity with a dopamine transporter and a noradrenaline transporter, and can be used for discovering changes of heart sympathetic nerves at an early stage, so that powerful evidence is provided for early diagnosis and treatment of heart diseases; the preparation method is good in repeatability and stable in synthesis yield.

Description

technical field [0001] The invention belongs to the technical field of positron nuclide imaging agents, and relates to a labeling technology for radioactive compounds (preparations containing radioactive substances), in particular to N-(2-fluoro[18F]ethyl) dopamine imaging agents and its Preparation. Background technique [0002] Normal cardiovascular function depends on innervation of the heart. The adaptation of the heart to the hemodynamic demands of the body under physiological and pathological conditions (especially the rhythm, conduction and contractility of the heart, etc.) is largely regulated by the autonomic nervous system (ANS). In various heart diseases (such as acute and chronic myocardial ischemia, myocardial infarction, arrhythmia, hypertension, diabetes, hypertrophic cardiomyopathy, and familial autonomic dysfunction, etc.), changes in cardiac ANS occur when the heart has obvious structural and Before abnormal function, it cannot be observed by conventional...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): C07C215/52C07C213/08A61K51/04A61K101/02
CPCC07C215/52A61K51/0406
Inventor 何玉林王相成周伟娜张国建白侠王雪梅杨宏娟
Owner 何玉林
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com