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Bipyridine tricarbonyl technetium-99m-marked long-chain fatty acid derivative and application thereof

A technology of long-chain fatty acids and bispyridines, which is applied in the field of long-chain fatty acid derivatives labeled with new bispyridine tricarbonyl technetium-99m, which can solve the problems of slow metabolism and affecting imaging effects, and improve the labeling rate and reduce the Liver background, providing feasibility and operability effects

Inactive Publication Date: 2015-12-30
BEIJING NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] From the literature data, it can be seen that 99m The advantage of Tc-labeled fatty acid myocardial metabolism imaging agent is that it has a higher initial myocardial uptake and rapid myocardial metabolism, but its disadvantage is that its metabolism in the liver is slower, forming a higher liver background and affecting the imaging effect. Therefore, there is still a lot of room for research in the field of myocardial metabolic imaging agents labeled with

Method used

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  • Bipyridine tricarbonyl technetium-99m-marked long-chain fatty acid derivative and application thereof
  • Bipyridine tricarbonyl technetium-99m-marked long-chain fatty acid derivative and application thereof
  • Bipyridine tricarbonyl technetium-99m-marked long-chain fatty acid derivative and application thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] The general structural formula of the novel bispyridine tricarbonyl technetium-99m labeled long-chain fatty acid derivative is:

[0052]

[0053] where A is -CH 2 or E is -CH 2 or no a , n b are positive integers, n a 1-16, n b is 0 or 1, and when n b When it is 1, R is S, O or N.

[0054] As a further preferred embodiment, n b is 0, A is -CH 2 , E is -CH 2 or , the structure of the long-chain fatty acid derivative labeled with bispyridine tricarbonyl technetium-99m is: Among them, n a It is a positive integer of 4-12;

[0055] As a further preferred embodiment, the structure of the long-chain fatty acid derivative labeled with bispyridine tricarbonyl technetium-99m is: Among them, n a It is a positive integer of 4-12;

[0056] As a further preferred embodiment, n b When it is 1, R is S, O or N, and A is -CH 2 or E is -CH 2 or no a It is a positive integer of 1-16.

[0057] As a further preferred embodiment, n b When it is 1, R is S,...

Embodiment 2

[0062] Embodiment 2: the synthetic route of following compound is:

[0063] 1, where n 1 is 8-16, R is S, O or N;

[0064]

[0065] 2, where n 2 is 8-14, R is S, O or N;

[0066]

[0067] 3. where n 2 is 8-14, R is S, O or N;

[0068]

[0069] 4. where n 2 is 8-14, R is S, O or N;

[0070]

Embodiment 3

[0072] Embodiment 3: Preparation of marker intermediate

[0073] fac-[ 99m Tc(CO) 3 (H 2 O) 3 ] + Preparation of intermediates: Take 5mgNa2CO3, 10mgNaBH4, 15mg sodium potassium tartrate in a 10mL penicillin vial, add 1ml of normal saline to it, shake well, use a 10ml disposable needle to evacuate, pass the gas in the carbon monoxide for 15min, and drain the bottle air, then inject 2mlNa 99m TCO4 The eluate (about 13mci) was continuously heated in an 80°C oil bath for 30min (carbon monoxide gas was passed through during the reaction), cooled to obtain the intermediate [ 99m Tc(CO) 3 (H 2 O) 3 ] + , to be used, the intermediate intermediate [ 99m Tc(CO) 3 (H 2 O) 3 ] + The HPLC diagram is as follows Figure 8 shown.

[0074] Synthetic intermediates of rhenium complexes [NEt 4 ] 2 [Re(CO) 3 Br 3 ] preparation: under nitrogen protection, weigh 505.4mg (1.2mmol) tetraethylamine bromide and 415.2mg (1.0mmol) pentacarbonyl rhenium bromide, add diethylene glycol di...

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Abstract

The invention relates to a bipyridine tricarbonyl technetium-99m-marked long-chain fatty acid derivative and application thereof. The long-chain fatty acid derivative is mainly used as a myocardial imaging agent. According to the long-chain fatty acid derivative, the liver background is lowered mainly through reasonably improving a molecular structure to reduce the lipid solubility of a compound, unsaturated aromatic rings are introduced in long-chain fatty acid, and the beta-oxidation of the fatty acid can be blocked, the myocardial uptake is improved and myocardial retention is prolonged, so as to provide a novel tricarbonyl technetium-99m-marked long-chain fatty acid derivative possibly applied to clinic. Moreover, the marking percentage of the technetium-99m-marked long-chain fatty acid derivative is high, and clinical application feasibility and operability are provided.

Description

technical field [0001] The invention relates to a class of long-chain fatty acid compounds in the fields of organic chemistry and medicinal chemistry, in particular to a novel bispyridine tricarbonyl technetium-99m-labeled long-chain fatty acid derivative and its application. Background technique [0002] Cardiovascular disease, also known as circulatory system disease, includes coronary heart disease, cerebrovascular disease, rheumatic heart disease, congenital heart disease, etc. According to the World Health Organization's 2004 Global Burden of Disease report, cardiovascular disease is the number one killer in the world. In 2004, 17 million people died of cardiovascular disease worldwide. By 2030, the number of deaths is expected to exceed 23 million. [1] . The disease originated from circulatory system lesions of the human body, but is generally closely related to arteriosclerosis, which is caused by the deposition of fat and cholesterol on the inner wall of arteries, t...

Claims

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Application Information

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IPC IPC(8): C07F13/00A61K51/04A61K103/10
Inventor 张华北薛倩倩刘建萍
Owner BEIJING NORMAL UNIVERSITY
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