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Technetium-99m marked isonitrile group mating material, preparing process and uses thereof

A complex, -99m technology, which is used in preparations for in vivo experiments, compounds of Group 7/17 elements of the periodic table, pharmaceutical formulations, etc., can solve the imaging effect of susceptible viruses, susceptible to other factors, The preparation method is complex and other problems, to achieve the effect of simple preparation method, good retention and high uptake

Inactive Publication Date: 2004-06-16
BEIJING NORMAL UNIVERSITY
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Problems solved by technology

[0012] It can be seen that the existing relatively successful heart blood pool imaging agents are limited to technetium-99m-labeled red blood cells or biological extract HSA, and there are still problems such as complicated preparation methods, high prices, easy virus infection, and other imaging effects. If a new type of radioactive technetium-99m-labeled heart blood pool imaging agent with the characteristics of simple preparation method, low cost and good imaging effect can be provided, it will have broad application prospects

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  • Technetium-99m marked isonitrile group mating material, preparing process and uses thereof
  • Technetium-99m marked isonitrile group mating material, preparing process and uses thereof
  • Technetium-99m marked isonitrile group mating material, preparing process and uses thereof

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preparation example

[0054] 1. Preparation of ligand CN-R (see Chinese patent application 00107287.0)

[0055] 1) Synthetic route of isonitrile ligands:

[0056] a.

[0057] b.

[0058] In the formula: Py is pyridine, R' is cyclohexyl, 2-methylcyclohexyl, 2,3-dimethylcyclohexyl, 3,3,5-trimethylcyclohexyl, cycloheptyl or cyclooctyl.

[0059] 2) Synthesis of formamide (R'-NHCHO):

[0060] 35.2 mmol of ethyl formate (about 2.60 g) was slowly added dropwise to 40 mmol of primary amine (R′-NH 2 , in the formula: the definition of R' is as described in 1), after the exothermic reaction stopped, the reaction solution was refluxed for 2 hours, and fractionated under reduced pressure with a 25cm Webster fractionating column, and the collected product was colorless, transparent and viscous liquid. Weigh and calculate yield. It was confirmed to be formamide by infrared spectrogram identification. Table 1 lists the yields, boiling points and characteristic peaks of infrared absorption of se...

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Abstract

A isocyanide complex for technetium-99m mark, wherein Tc(I) is arranged to be the central core, the coordinated isocyanide ligand is represented by formula CN-R, wherein R is C6-10 cycloalkyl substituted or unsubstituted by any of 1-4 same or different C1-4 alkyl or alkoxy, the complex is prepared by wet method or freeze-drying method, it can be used as blood pool imaging agent with the advantages of simple preparing process, low price and high ratio of target / non-target.

Description

technical field [0001] The present invention relates to a 99m Tc-labeled radioactive complex, its preparation method and the application of the complex as a heart blood pool imaging agent. Background technique [0002] exist 99m In the field of Tc-labeled radiopharmaceutical chemistry, for 99m Alkyl isonitrile complexes with Tc(I) nucleus as the central core ([ 99m Tc(CNP) 6 ] + ) is very active, and its structural formula is shown in (a). The reported complexes are mainly used as myocardial perfusion imaging agents, such as 99m Tc-TBI (TBI=t-ButyIsonitrile, t-butylisonitrile) (Holman BL, Jones AG, Lister-James J et a1.A newTc-99m-labeled myocardial imaging agent, hexakis (t-butylisonitrile) technetium (I) [Tc -99m-TBI]: initial experience in the human.J Nucl Med, 1984, 25:1350), 99m Tc-CPI (CPI=Carbomethoxyisopropylisonitrile) (Holman BL, Sporn V, Jones AG et a1. Myocardial imaging with technetium-99m-CPI: initial experience in the human. J Nucl Med, 1987, 28: 13 )w...

Claims

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Application Information

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IPC IPC(8): A61K51/00C07F13/00
Inventor 张现忠王学斌
Owner BEIJING NORMAL UNIVERSITY
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