Terminal amino oxyethylene block polymer modified Gd coordination compound and its synthesis process

Abstract

Terminal amino oxyethylene block polymer modified Gd coordination compound and its synthesis process belongs to the field of medicine and chemical synthesis technology. The coordination compound is synthesized through the reaction of diethyl triamino pentaacetic anhydride and polyoxyethylene with double terminal amino radical to obtain coarse terminal amino polymer; purification; reaction of refined coordination compound and gadolinium trichloride; purification to obtain the product terminal amino oxyethylene block polymer modified Gd coordination compound. The product has high relaxation rate, long time of staying in body and high water solubility, and can meet the requirement as intravenous injected contrast medium.

Description

technical field [0001] The invention relates to a gadolinium complex modified by amino-terminated block polyoxyethylene and a synthesis method thereof, belonging to the technical fields of medicine and chemical synthesis. Background technique [0002] Magnetic resonance imaging is the latest medical imaging technology. The problem it faces is how to improve the imaging sensitivity and image clarity. The use of magnetic resonance imaging contrast agent is an effective way to solve this problem. Magnetic resonance imaging contrast agents are generally complexes of paramagnetic metal ions, and the ligands are mostly linear and cyclic compounds containing polyamino groups and polycarboxylates. Among metal ions, gadolinium ions have the strongest paramagnetism. Compared with small molecular paramagnetic metal ion complexes, macromolecular paramagnetic metal ion complexes not only have the advantage of higher relaxation rate, but also can be used for angiography. Therefore, macrom...

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Problems solved by technology

However, the molecular weight of gadopentetate meglumine is small, the excretion is too fast, and the elimination half-life is about 20 to 100 minutes; this reagent has no tissue and organ selectivity, and is almost completely excreted through the liver, so the imaging effect on the hepatobiliary system is not ideal; If the speed is too fast, the MRI of the brain and spinal cord needs to be administered again within 30 minutes; to judge whether the patient is an adult lesion or a tumor recurrence, it is necessary to increase the dosage; increasing the dosage of the drug increases the amount of detoxification of the human body and improves Possibility of negative effects; gadopentetate dimeglumine contrast agent has no targeting, it is a contrast agent with non-specific distribution, and the distribution in various tissues is mainly due to the difference in tissue blood supply and microvascular permeability different; it cannot pass through the complete blood-brain barrier, nor can it enter other tissues of the capillary barrier, such as the spinal cord, eye and testis; Thus limited to plasma transport; gadopentetate dimeglumine is unsuitable for imaging cardiac and vascular disease, and so-called contrast-enhancing agents for blood pool imaging are usually used, which typically require very slow elimination

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