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Technetium-99m labeled isonitrile-containing folic acid derivative as well as preparation method and application thereof

A folic acid derivative, 99mtc technology, which is applied in the field of technetium-99m-labeled isonitrile-containing folic acid derivatives and its preparation, can solve the problems of limited wide application, high absorbed dose of renal irradiation, kidney damage and the like

Active Publication Date: 2021-07-23
BEIJING NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

According to research findings, although the currently reported radiopharmaceuticals targeting folic acid receptors have high uptake in the tumor site and can clearly identify the location of the tumor, the uptake of these drugs in the kidney is very high, resulting in the absorption of radiation received by the kidney. Excessive doses can damage the kidneys, and most drug preparations require high-performance liquid chromatography purification, which limits the wide application of these drugs in clinical practice

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  • Technetium-99m labeled isonitrile-containing folic acid derivative as well as preparation method and application thereof
  • Technetium-99m labeled isonitrile-containing folic acid derivative as well as preparation method and application thereof
  • Technetium-99m labeled isonitrile-containing folic acid derivative as well as preparation method and application thereof

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Embodiment Construction

[0043] Describe the present invention in detail below by embodiment: a kind of [ 99m Tc-(CNMBFA) 6 ] + Complexes:

[0044] a. Synthesis of ligand CNMBFA:

[0045] Weigh 0.145g (0.3mmol) of compound 1 in a 25mL round bottom flask, add an appropriate amount of dimethyl sulfoxide (DMSO) to dissolve, then add 0.130g (0.33mmol) of sodium hydroxide, and add 0.116g (0.36mmol) of sodium hydroxide under nitrogen protection. ) Compound 2 (m=1, n=1), reacted at room temperature for 6h under dark conditions. After the reaction, the ligand CNMBFA was obtained after repeated washing with cold ether and vacuum drying. 1 H-NMR(400MHz,DMSO)δ(ppm):δ8.59(m,1H),7.70–7.48(m,2H),7.23(m,5H),6.66–6.52(m,1H),4.76(s ,2H),4.49–4.36(m,1H),3.29(s,4H),3.06(s,4H),1.92–1.52(m,2H),1.04(d,J=6.9Hz,2H); IR( KBr) / cm -1 :2150.72(-NC);HR-MS(ESI)for C 31 h 33 N 10 o 6 :found641.2583, calcd 641.2579.

[0046] b.[ 99m Tc-(CNMBFA) 6 ] + Preparation of complexes

[0047] Dissolve 2.6mg of sodium citrate ...

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Abstract

The invention discloses a [99mTc-(CNMBFA) 6]<+> complex as well as a preparation method and an application thereof. The [<99m> Tc-(CNMBFA) 6] <+> complex is obtained by two steps of synthesis of a ligand CNMBFA and preparation of the [<99m>Tc-(CNMBFA) 6]<+> complex. The complex is simple to prepare, high in radiochemical purity and good in stability, has specific uptake at a tumor part of a nude mouse with KB tumor, is relatively low in kidney uptake, reduces the injury effect on the kidney, and is a novel tumor imaging agent which is excellent in performance and is targeted to a folate receptor.

Description

technical field [0001] The invention belongs to the technical field of radiopharmaceuticals, and particularly relates to a technetium-99m-labeled isocyanide-containing folic acid derivative, a preparation method and application thereof. Background technique [0002] Tumor is a kind of disease caused by uncontrolled continuous proliferation of body cells under the influence of various factors. In terms of development, tumors can be divided into benign tumors and malignant tumors, and malignant tumors are also called cancers. At present, cancer has become the second largest killer of human health after cardiovascular and cerebrovascular diseases. In recent years, nuclear medicine imaging has the advantages of simplicity, sensitivity, specificity, safety, non-injury, and easy repetition. It can detect molecular biological behaviors and pathophysiological changes in the body, and has become a large category of detection methods for tumor diagnosis. With the widespread use of S...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F13/00C07D475/04C07B59/00A61K51/04A61K103/10
CPCC07F13/00C07D475/04C07B59/004A61K51/0482C07B2200/05Y02P20/55
Inventor 张俊波冯俊红张旭冉阮晴王学斌唐志刚陆洁张站斌
Owner BEIJING NORMAL UNIVERSITY
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