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Molecular probe imaging agent and preparation method thereof

A technology of molecular probes and imaging agents, applied in the fields of radiopharmaceutical chemistry and clinical nuclear medicine, can solve the problems of high false positive and false negative rates, unfavorable disease treatment, etc., and achieve the effect of improving organs

Active Publication Date: 2019-07-23
SUZHOU INST OF BIOMEDICAL ENG & TECH CHINESE ACADEMY OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the false positive and false negative rates are still high, which is not conducive to the treatment of diseases

Method used

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  • Molecular probe imaging agent and preparation method thereof
  • Molecular probe imaging agent and preparation method thereof
  • Molecular probe imaging agent and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] A molecular probe imaging agent, the molecular probe imaging agent is Tc-N 2 o 3 SPECT, the Tc-N 2 o 3 The chemical structural formula of SPECT imaging agent is as follows:

[0039] ,

[0040] Wherein, Et is ethyl.

[0041] The preparation method of the molecular probe imaging agent, the synthetic route of the preparation method is as follows:

[0042]

[0043]

[0044]

[0045] The preparation method of described molecular probe imaging agent comprises the following steps:

[0046] (1) Synthesis of compound 1:

[0047] 1.0 g of o-hydroxybenzyl alcohol was mixed with 50 mL of dichloromethane, then 5 drops of trifluoromethanesulfonic acid and excess isobutylene were added dropwise, stirred at -76°C for 5 hours, the reaction solution was stirred to room temperature, washed with water and dilute acetic acid respectively, The organic layer was separated, dried and evaporated to remove the organic liquid, re-dissolved in 30 mL of dichloromethane, and adde...

Embodiment 2

[0061] A molecular probe imaging agent, the molecular probe imaging agent is Tc-N 2 o 3 SPECT, the Tc-N 2 o 3 The chemical structural formula of SPECT imaging agent is as follows:

[0062] ,

[0063] Wherein, Et is ethyl.

[0064] The preparation method of the molecular probe imaging agent, the synthetic route of the preparation method is as follows:

[0065]

[0066]

[0067]

[0068] The preparation method of described molecular probe imaging agent comprises the following steps:

[0069] (1) Synthesis of compound 1:

[0070] 1.24 g of o-hydroxybenzyl alcohol was mixed with 100 mL of dichloromethane, then 5 drops of trifluoromethanesulfonic acid and excess isobutylene were added dropwise, stirred at -76°C for 5 hours, the reaction solution was stirred to room temperature, washed with water and dilute acetic acid, respectively, Separate the organic layer, evaporate the organic liquid after drying, re-dissolve in 50 mL of dichloromethane, and add 2.0 g of ma...

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Abstract

The invention discloses a molecular probe imaging agent and a preparation method thereof. The molecular probe imaging agent is Tc-N2O3 SPECT (single-photon emission computed tomography), and the chemical structural formula of the imaging agent Tc-N2O3 SPECT is shown in the specification, wherein Et is ethyl. The preparation method of the imaging agent adopts a synthetic route shown in the specification. The molecular probe imaging agent can remarkably improve phenomena that the conventional imaging agent is more absorbed in organs, especially in liver of an organism, is often decomposed, consumes longer time to be completely eliminated from the organism and the like, and can also increase the positive rate and the accuracy rate of the conventional imaging agent in early diagnosis of cancers such as breast cancer, melanoma, cervical cancer, carcinoma of vulva, colorectal cancer and the like.

Description

technical field [0001] The invention relates to the fields of radiopharmaceutical chemistry and clinical nuclear medicine, in particular to a molecular probe imaging agent and a preparation method thereof. Background technique [0002] Disease diagnosis is generally divided into two types: in vitro and in vivo. Although in vitro diagnosis is fast and convenient, its accuracy is poor, and in vivo diagnosis is often required for review. In vivo diagnostics are further divided into invasive (painful) and non-in vivo diagnostics (painless). Medical imaging has entered the era of molecular imaging. The research of molecular imaging includes imaging equipment and molecular probes, and the development of new molecular probes is the core of the development of molecular imaging. Generally speaking, positron emission tomography (PET) / single photon emission computed tomography (SPECT) is functional imaging, not anatomical imaging of tissues or organs. PET / SPECT imaging requires the ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K51/04C07F13/00A61K103/10
CPCA61K51/0482C07F13/005
Inventor 彭义杰
Owner SUZHOU INST OF BIOMEDICAL ENG & TECH CHINESE ACADEMY OF SCI