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

Deuterated tropane derivative and application thereof

A technology of tropane and its derivatives, applied in the chemical field, can solve the problems of complex operation, unfavorable animal basic research, and no advantage in popularization and application, and achieve the effects of slow metabolic degradation, good stability in the body, and high application prospects

Active Publication Date: 2021-06-25
JIANGSU INST OF NUCLEAR MEDICINE
View PDF4 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, obviously, this method is extremely complicated in operation. It not only needs to collect images for 180 minutes, but also collects arterial blood samples at a suitable time point (due to individual differences, the time point of blood collection may need to be explored repeatedly), and complex blood sample analysis is required. (analysis of the original drug components in plasma), which is very unfavorable for routine clinical PET examination, has no advantages in popularization and application, and is not conducive to basic research at the animal level
[0009] There are also scholars on other tropane DAT drugs[ 18 F] FE-PE2I conducted a similar PET imaging method study, and the total time for imaging and blood collection was 90 minutes (Sasaki T, et al. J. Nucl. Med. 2012, 53: 1065-1073.), which is still inconvenient Clinical application

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
  • Deuterated tropane derivative and application thereof
  • Deuterated tropane derivative and application thereof
  • Deuterated tropane derivative and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-1

[0049] Embodiment 1-1: A kind of deuterated tropane derivative

[0050] The present embodiment provides a kind of deuterotropane derivative FECNT-d 4 , the deuterotropane derivative FECNT-d 4 has the following structure:

[0051]

Embodiment 1-2

[0052] Embodiment 1-2: A kind of method for preparing deuterated tropine derivatives

[0053] This embodiment provides the deuterated tropane derivative FECNT-d described in embodiment 1-1 4 The preparation method, described method is (deuterotropane derivative FECNT-d 4 For the synthetic route see figure 1 ):

[0054] Under nitrogen protection, 279mg nor-CClT (1mmol) and 222mg FCD 2 cd 2 OTs (1mmol) was dissolved in 8mL of methanol to obtain a mixed solution; 258mg N,N-diisopropylethylamine (DIPEA, 2mmol) was added to the mixed solution, and heated under reflux at 100°C for 24h to obtain a reflux solution; After the liquid was cooled to room temperature (25°C), 5mL NaOH solution (1mol) was added to the reflux liquid, stirred for 1h to react to obtain a reaction liquid; 5mL benzene was added to the reaction liquid, and concentrated under reduced pressure at 60°C to obtain a crude product ; The crude product is purified through silica gel chromatography to obtain deuterotr...

Embodiment 2-1

[0058] Embodiment 2-1: A kind of deuterated tropane derivative

[0059] This embodiment provides a kind of deuterotropane derivative [ 18 F] FECNT-d 4 , the deuterotropane derivatives [ 18 F] FECNT-d 4 has the following structure:

[0060]

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 a deuterated tropine derivative and an application thereof, and belongs to the technical field of chemistry. The invention provides a deuterated tropane derivative [18F]FECNT-d4; the deuterated tropane derivative [18F]FECNT-d4 can be specifically combined with a dopamine transporter, and moreover, the deuterated tropane derivative [18F]FECNT-d4 has the advantages of good in-vivo stability, low metabolic degradation speed and high affinity to the dopamine transporter; and the deuterated tropane derivative [18F]FECNT-d4 has a high application prospect in the aspect of PET imaging of the dopamine transporter.

Description

technical field [0001] The invention relates to a deuterated tropine derivative and application thereof, belonging to the technical field of chemistry. Background technique [0002] The dopamine transporter (DAT) of the central nervous system, also known as dopamine transporter, is a membrane protein located on the presynaptic membrane of dopaminergic neurons (dopaminergic neurons, also known as dopamine neurons). The role is to reverse the transport of dopamine (DA) in the synaptic cleft back to the presynaptic membrane for reuse. DAT plays a key role in the regulation of DA transmitter system. A variety of neurological diseases are associated with changes in DAT density, distribution, and function. Therefore, positron emission tomography (PET) imaging targeting DAT has played an important role in the imaging studies of various neurological diseases, such as Parkinson's disease, ADHD syndrome, drug addiction, depression , Anxiety disorders, etc., especially in the field ...

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): C07D451/02C07B59/00A61K51/04A61K101/02
CPCC07D451/02C07B59/002A61K51/0455C07B2200/05
Inventor 陈正平曹珊珊刘春仪唐婕方毅季林阳黄彩云谢敏浩
Owner JIANGSU INST OF NUCLEAR MEDICINE
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