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A kind of deuterotropane 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: 2022-01-14
JIANGSU INST OF NUCLEAR MEDICINE
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  • Abstract
  • Description
  • Claims
  • Application Information

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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

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  • A kind of deuterotropane derivative and application thereof
  • A kind of deuterotropane derivative and application thereof
  • A kind of deuterotropane derivative and application thereof

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Experimental program
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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]

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Abstract

The invention relates to a deuterated tropine derivative and application thereof, belonging to the technical field of chemistry. The invention provides a deuterotropane derivative [ 18 F] FECNT‑d 4 , this deuterotropane derivative [ 18 F] FECNT‑d 4 Can specifically bind with dopamine transporter, and this deuterated tropine derivative [ 18 F] FECNT‑d 4 It has the advantages of good stability in vivo, slow metabolic degradation, and high affinity for dopamine transporters, and has a very high application prospect in PET imaging of dopamine transporters.

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

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Application Information

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Patent Type & Authority Patents(China)
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
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