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Tc marked daunorubicin dithiocarbamate composition and preparation method and applications thereof

A technology of daunorubicin and ammonium sulfate, which is applied in the fields of 99mTc-labeled radiopharmaceutical chemistry and clinical nuclear medicine, can solve the problems of high price, difficulty in popularization and application, etc.

Inactive Publication Date: 2009-11-11
BEIJING NORMAL UNIVERSITY +1
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Problems solved by technology

However, due to the positron nuclides such as 11 C. 18 F, etc. are produced by accelerators, which are expensive and difficult to promote and apply

Method used

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  • Tc marked daunorubicin dithiocarbamate composition and preparation method and applications thereof
  • Tc marked daunorubicin dithiocarbamate composition and preparation method and applications thereof
  • Tc marked daunorubicin dithiocarbamate composition and preparation method and applications thereof

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Embodiment Construction

[0055] Describe the present invention in detail below by embodiment:

[0056] A sort of 99m Tc-labeled daunorubicin dicarbaminate ( 99m Tc-DAUDTC) complexes, including 99m TcN-DAUDTC and 99m TcO-DAUDTC complex, its preparation method is as follows:

[0057] a. Synthesis of ligand DAUDTC:

[0058] 0.01mol daunorubicin hydrochloride (analytically pure) is added in the 50mL there-necked flask, and 4mL of 5mol / L NaOH (analytically pure, produced by Beijing Chemical Plant) methanol solution is added to the reaction vessel, stirred in an ice-water bath, and then Slowly add 0.01molCS dropwise 2 (analytical pure, Xilong Chemical Factory, Shantou City, Guangdong Province), stirred for 2h-3h, and the temperature during the entire reaction process was controlled below 10°C. Then the red solid was obtained by suction filtration, recrystallized with methanol, and the red powder was DAUDTC. Infrared spectrum: v(IR) / cm -1 : 3446.3(-OH), 2924.8(CH 3 ), 2844.3 (CH 2 ), 10...

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Abstract

The invention discloses a Tc marked daunorubicin dithiocarbamate composition, including a composition consisting of TcN-DAUDTC and TcO-DAUDTC, and a preparation method and applications thereof. The composition uses a (Tc-N) nucleus or a (TcO) nucleus as a central nucleus, and has a geometrical configuration of irregular square pyramid, and four sulphur atoms provided by two DAUDTC ligand molecules are positioned at four points of the bottom of the irregular square pyramid. The composition is high in radiochemical purity, and good in stability. The composition of TcN-DAUDTC and TcO-DAUDTC has higher uptake value of tumors and good retention in tumors, and rational target-to-nontarget ratio of inflammation to muscle. Therefore, the composition is a new developer of tumors, with popularization and application values.

Description

Technical field [0001] The present invention relates to 99m Tc labeled radiopharmaceutical chemistry and clinical nuclear medicine technical field, specifically relates to a 99m Tc-labeled daunorubicin dicarbaminate complex, preparation method and application. Background technique [0002] Malignant tumors have become one of the biggest culprits that seriously endanger human health. A large number of experiments have shown that early diagnosis of tumors is very important in the treatment of tumors. 99m Tc has become one of the most commonly used and most promising radionuclides in nuclear medicine examinations due to its good nuclear properties and low cost. Therefore, when PET drugs become a research hotspot, the use of 99m The study of Tc-labeled new tumor radiopharmaceuticals still attracts great attention. exist 99m In the development of Tc tumor imaging agents, there is an interesting phenomenon that drugs commonly used in clinical myocardial perfusion imaging such...

Claims

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Application Information

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IPC IPC(8): C07H15/252C07F13/00A61K51/04A61K103/10
Inventor 张俊波任佳蕾林潇马志伟王学斌唐志刚张现忠陆洁
Owner BEIJING NORMAL UNIVERSITY
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