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99mTc-labelled isonitrile-containing glucose derivative and preparation method and application thereof

A glucose derivative, isonitrile-containing technology, used in the fields of radiopharmaceutical chemistry and clinical nuclear medicine, can solve the problems of limited wide application and expensive diagnosis costs

Active Publication Date: 2017-10-13
BEIJING SHIHONG PHARMACEUTICAL CO LTD +1
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Problems solved by technology

[0003] At present, the most clinically used tumor imaging agents are 18 F-fluorodeoxyglucose ( 18 F-FDG), the imaging effect is better, but its relatively expensive diagnostic cost limits its wide application to a certain extent, especially in economically underdeveloped countries and regions.

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  • 99mTc-labelled isonitrile-containing glucose derivative and preparation method and application thereof

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Embodiment Construction

[0063] Describe the present invention in detail below by embodiment: a kind of 99m Tc-labeled isocyanide-containing glucose derivatives, the general structure of which is [ 99m Tc-(CNDG) 6 ] + , its preparation steps are as follows:

[0064] a: Synthesis of Ligand CNDG::

[0065] Weigh an appropriate amount of glucosamine hydrochloride into a 25mL round bottom flask, add anhydrous methanol to dissolve, then add an appropriate amount of NaOH, and stir at room temperature for 30min. Afterwards, the reaction bottle was placed in an ice-water bath, and an appropriate amount of methanol solution containing compound (II) was slowly added dropwise under stirring. After the dropwise addition, the reaction was continued under an ice-water bath for 3 hours. After the reaction was completed, the solvent was distilled off under reduced pressure, and purified by column chromatography. (Dichloromethane-methanol) to obtain the ligand CNDG:

[0066] Concrete synthetic route is:

[0067]...

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Abstract

The invention discloses a 99mTc-labelled isonitrile-containing glucose derivative and a preparation method and an application of the 99mTc-labelled isonitrile-containing glucose derivative, wherein the general molecular formula of the 99mTc-labelled isonitrile-containing glucose derivative is [99mTc-(CNDG)6]+. The derivative takes 99mTc+ as a central core, an isonitrile carbon atom in the CNDG and 99mTc (I) coordinate to form hexa-coordination compound [99mTc-(CNDG)6]+. The [99mTc-(CNDG)6]+ derivative is prepared through the synthesis of the ligand CNDG and the preparation of a CNDG freeze-drying medicine box. The derivative is good in stability and convenient in preparation, is higher in uptake and excellent in retention on a tumor part, is high in tumor / target-to-nontarget ratio, is a high-performance novel 99mTc-labelled isonitrile-containing glucose derivative used for tumor imaging, and is convenient to popularize and apply.

Description

technical field [0001] The invention belongs to the technical field of radiopharmaceutical chemistry and clinical nuclear medicine, and specifically relates to a 99m Tc-labeled isocyanide-containing glucose derivative, preparation method and application. Background technique [0002] At present, in the field of clinical medicine, malignant tumors have become the number one killer that threatens human health and life. The annual incidence and mortality of tumors are still on the rise. Early diagnosis, early treatment and personalized treatment of tumors are the key to reducing tumor deaths. the most effective measure. Traditional non-invasive tumor detection and imaging methods such as X-ray method, CT, MRI, etc., mainly focus on imaging the morphology and structure of organs under pathological conditions, while nuclear medicine molecular imaging techniques such as positron emission tomography (PET) And single photon emission tomography (SPECT) can reflect the physiological...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H13/04C07H1/00A61K51/04A61K103/10
CPCA61K51/0491C07H1/00C07H13/04
Inventor 张俊波张旭冉甘倩倩邵欣王学斌唐志刚陆洁张站斌
Owner BEIJING SHIHONG PHARMACEUTICAL CO LTD
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