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Preparation method and application of 99mTc-marked hydrazino nicotinamide-folate complexs

A nicotinamide-based, 99mtc technology, used in the fields of radiopharmaceutical chemistry and clinical nuclear medicine, can solve the problem of low absolute uptake by tumors

Inactive Publication Date: 2011-07-20
BEIJING NORMAL UNIVERSITY +1
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  • Abstract
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Problems solved by technology

Literature report 99m Tc-HYNIC-folate has good target-to-non-target ratios such as tumor / blood, tumor / meat, etc., but the absolute tumor uptake value in the KB tumor-bearing mouse model is low, and the background of liver, spleen, etc. is high ( W. Guo, G. H. Hinkle, R. J. Lee, 99m Tc-HYNIC-folate: a novel receptor-based targeted radiopharmaceutical for tumor imaging. J Nucl Med1999; 40: 1563-1569; Liu Liqin, Wang Shizhen, etc. Folate receptor tumor imaging agent 99m Synthesis and animal imaging of Tc-hydrazinyl nicotinamide hydrazide-folic acid. Chinese Academy of Medical Sciences Journal. 2006; 28:786-789 Chinese Academy of Medical Sciences Journal)

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  • Preparation method and application of 99mTc-marked hydrazino nicotinamide-folate complexs
  • Preparation method and application of 99mTc-marked hydrazino nicotinamide-folate complexs
  • Preparation method and application of 99mTc-marked hydrazino nicotinamide-folate complexs

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Embodiment Construction

[0018] Describe the present invention in detail below by embodiment: a kind of 99m Tc-labeled hydrazinonicotinamide-folate complex:

[0019] Its structural formula is:

[0020]

[0021] 99m The preparation method of the Tc-labeled hydrazinonicotinamide-folate complex is as follows:

[0022] a. Synthesis of ligand hydrazinonicotinamide-folate (HYNIC-NHHN-Folate):

[0023] Dissolve 520mg Folate-NHHN and 532mg NHS-HYNIC-Boc in 25mL dimethyl sulfoxide, add 10mL pyridine, and react at room temperature for 16h. The reacted solution was slowly dripped into 500 mL of ether, and the resulting orange-red precipitate was collected by centrifugation, washed with ether (3×5 mL) and dichloromethane (3×5 mL) respectively, and dried in vacuo to obtain 363 mg of orange-red solid with a yield of 48.8 mg. %.

[0024] Its H NMR spectrum ( 1 HNMR, DMSO-d 6 )for:

[0025] δ: 8.94(s, 1H), 8.65(s, 1H), 8.53(s, 1H), 8.19(m, 2H), 7.85(m, 2H), 6.98(m.1H), 6.61(d, J=8.3 Hz, 2H), 4.48(d, J=5.4...

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Abstract

The present invention discloses a preparation method and application of a 99mTc-marked hydrazino nicotinamide-folate coordination compound. In the preparation method, the target coordination compound is obtained through two steps of synthesizing ligand hydrazino nicotinamide-folate and marking the hydrazino nicotinamide-folate by 99mTc. The coordination compound has the advantages of high hydrazino nicotinamide-folate, good stability, low cost, high tumor uptaking, good detention and good target / non-target ratio of tumor / blood, tumor / muscle and the like and can be used for preparing a tumor developer as a novel 99mTc-marked folate receptor.

Description

Technical field [0001] The present invention relates to 99m The field of Tc-labeled radiopharmaceutical chemistry and clinical nuclear medicine technology, specifically relates to a 99m Preparation method and application of Tc-labeled hydrazinonicotinamide-folate complex. Background technique [0002] In the field of medical radiopharmaceutical chemistry, the folate (NHHN-Folate) receptor is a glycoprotein linked to the cell membrane by the polysaccharide phosphatidylinositol. The expression of folate receptor is highly conserved in normal healthy cells, but it is highly expressed in many malignant tumors derived from epithelial tissue, such as ovarian cancer, breast cancer, endometrial cancer, lung cancer, nasopharyngeal cancer and other tumors. Folate receptors have high affinity and specificity for folate analogs such as folic acid, methotrexate, and 5-methyltetrahydrofolate, and can mediate the endocytosis of these substances into cells. Using this characteristic tran...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07F13/00A61K51/04A61K103/10
Inventor 陆洁庞燕郭红娟王学斌张现忠张俊波唐志刚
Owner BEIJING NORMAL UNIVERSITY
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