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Carbon-11 labeled N-methyldopamine hydrochloride and preparation method thereof

A methyl dopamine and labeling technology, which is applied in the preparation of amino-substituting functional groups, organic chemistry, radioactive carriers, etc., can solve the problems of low yield, high cost of electrophilic synthesis, and difficult synthesis, and achieve small radiation side effects and strong affinity , Synthesize simple and easy effects

Inactive Publication Date: 2013-09-04
何玉林 +1
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

But due to the synthesis of 6- 18 F-Fluourodopamine requires special equipment, the cost of electrophilic synthesis is high, the synthesis is difficult, and the yield is low, so it has not been widely used

Method used

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  • Carbon-11 labeled N-methyldopamine hydrochloride and preparation method thereof
  • Carbon-11 labeled N-methyldopamine hydrochloride and preparation method thereof
  • Carbon-11 labeled N-methyldopamine hydrochloride and preparation method thereof

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Embodiment 1

[0031] Example 1 Preparation of N-methyldopamine labeled with carbon-11

[0032] one. 11 C-N-CH 3 -Synthesis of Dopamine

[0033] 1. 11 C- 11 CH 3 Preparation of I

[0034] produced by the cyclotron 11 C-CO 2 It is transported into the chemical reactor and mixed with hydrogen, and reacted at 400°C under the action of Ni catalyst to form 11 CH 4 ; 11 CH 4 React with sublimated iodine at a high temperature of 730°C to generate carbon-11 labeled methyl iodide ( 11 CH 3 I), 11 CH 3 I enters the reaction bottle under the flow rate of 20 mL / min in the helium flow, and 0.4 mL of acetone is placed in the reaction bottle, and placed in the cold hydrazine of minus 20 degrees, finally obtaining 200mCi of carbon-11 methyl iodide acetone solution, wherein The chemical amount of methyl iodide is 2.88ug (when the carbon-11 methyl iodide acetone solution is 300mCi, the chemical amount of methyl iodide is 4.32ug): .

[0035] 2. 11 CH 3 I react fully with 3 mg (3-6 mg) d...

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Abstract

The invention relates to a radioactive compound labeling technology in the field of positron imaging agents, in particular to a method for synthesizing carbon-11 labeled N-methyldopamine hydrochloride. The preparation method comprises the following steps of: A, fully reacting 200 to 300mCi of carbon-11 methyl iodide (II) with 3 to 6mg of dopamine hydrochloride (III) dissolved and neutralized by excessive 0.1mol / L sodium bicarbonate solution at the temperature of between 70-85DEG C, and cooling to room temperature to obtain reaction liquid; and B, blowing the reaction liquid in the step A to dryness, separating, collecting a substance with a radioactive component, wherein the radioactive component is the carbon-11 labeled N-methyldopamine hydrochloride (I). The carbon-11 labeled N-methyldopamine hydrochloride has strong affinity with a dopamine transporter and a norepinephrine transporter, can early discover the change of cardiac sympathetic nerves, and provides a strong evidence for early diagnosis and treatment of heart disease; and the preparation method is simple and practicable, good in repeatability, low in synthetic cost and stable in yield.

Description

technical field [0001] The invention relates to a radioactive compound labeling technology in the field of positron imaging agents, in particular to carbon-11 labeled N-methyl dopamine and a preparation method thereof. Background technique [0002] Normal cardiovascular function depends on innervation of the heart. The adaptability of the heart to the hemodynamic demands of the body under physiological and pathological conditions (especially the rhythm, conduction, and contractility of the heart) is largely regulated by the autonomic nervous system (ANS). In various heart diseases (such as acute and chronic myocardial ischemia, myocardial infarction, arrhythmia, hypertension, diabetes, hypertrophic cardiomyopathy, and familial autonomic dysfunction, etc.), changes in cardiac ANS occur when the heart has obvious structural and Before abnormal function, it cannot be observed by conventional morphological and functional detection methods. Therefore, establishing an evaluation...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C211/27C07C209/08A61K51/04A61K101/00
Inventor 何玉林王雪梅王城白侠张凯秀贾日东包宝亮郝喜燕
Owner 何玉林
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