Polyoxyethylene kind block polymer ligand and synthesizing process thereof

Abstract

A polyoxyvinyl-kind block polymer ligand used as the medical contrast medium for intravenous injection is prepared through the reaction between the benzoic acid with activated carboxyl or its derivative and the amino terminated block polyoxyethene modified ligand to obtain crude BEN-PEO-DTPA block polymer ligand, and purifying.

Description

technical field [0001] The invention relates to a polyoxyethylene / diethylenetriaminepentaacetic acid (BEN / PEO / DTPA) block polymer ligand containing benzoic acid and its derivatives and a synthesis method, and belongs 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 agents 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 and polycarboxyl groups. Among metal ions, gadolinium ions have the strongest paramagnetic properties. Compared with small-molecule paramagnetic metal ion complexes, macromolecular paramagnetic metal ion complexes not only have the advantag...

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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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