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A kind of method for preparing gadobutrol

A technology for gadobutrol and compounds is applied in the field of preparing high-purity gadobutrol, can solve problems such as complex methods, and achieve the effects of being environmentally friendly, mild and fast in reaction, and reducing safety risks.

Active Publication Date: 2020-03-27
CHEN STONE GUANGZHOU CO LTD
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the methods disclosed in the cited references are complicated and high-purity gadobutrol cannot be prepared therefrom

Method used

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  • A kind of method for preparing gadobutrol
  • A kind of method for preparing gadobutrol
  • A kind of method for preparing gadobutrol

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Embodiment Construction

[0065] Hereinafter, the preparation method of gadobutrol of the present invention will be described in detail.

[0066] According to the preparation method of gadobutrol of the present invention, its synthetic route is as follows:

[0067]

[0068] The preparation of embodiment gadobutrol

[0069] Step 1: 2,2',2''-(10-(1,3,4-trihydroxybutan-2-yl)-1,4,7,10-tetraazacyclododecane-1, Preparation of 4,7-triyl)triacetonitrile

[0070] (1) Use bromoacetonitrile

[0071]

[0072] Add 500 mL of acetonitrile into a 1000ml reaction flask, and add 50 g (0.1184 mol) of 3-(1,4,7,10-tetraazacyclododecane-1-yl)butane-1 into the reaction flask while stirring, 2,4-triol 4 hydrochloride, add 163g (1.184mol) potassium carbonate to the reaction flask at room temperature, and slowly add 42.6g (0.3552mol) bromoacetonitrile to it. After adding the materials, heat the temperature of the materials in the reaction bottle to 50°C to 55°C, and keep stirring at this temperature for the reaction. ...

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Abstract

The invention relates to a method for preparing high-purity Gadobutrol. The method uses 3-(1,4,7,10-tetraazacyclododecane-1-yl)butane-1,2,4-triol to react with bromoacetonitrile or bromoacetamide, anobtained intermediate is hydrolyzed under an alkaline condition, and a hydrolysate is complexed with a gadolinium ion source to obtain the high-purity Gadobutrol. The preparation process of the methodis simple and mild, and the method is suitable for large-scale process production.

Description

technical field [0001] The invention relates to a method for preparing high-purity gadobutrol. Background technique [0002] In the field of gadolinium-containing contrast agents, gadobutrol is sold commercially around the world under the tradename Gadovist or Gadavist. It is a new class of powerful magnetic resonance imaging contrast agent approved for contrast-enhanced magnetic resonance imaging (CE-MRI) diagnosis of multiple parts of the human body, including the brain, spinal cord, blood vessels, liver and kidneys. In addition, gadobutrol contains a high concentration of ionic T1-relaxation potency. Given its high concentration and high relaxivity potency, it exhibits the highest short T1 potency per mL of all gadolinium-containing contrast agents. This results in excellent image quality and the practical advantage of using a smaller dose. [0003] Gadobutrol represented by the following formula 1 is a nonionic complex composed of gadolinium (III) and a macrocyclic li...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D257/02
CPCC07D257/02
Inventor 梁龙赖英杰龙翔天谭俊荣卢彪谢德逊
Owner CHEN STONE GUANGZHOU CO LTD
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