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

A methyldopamine, labeling technology, applied in the preparation of amino-substituted functional groups, organic chemistry, radioactive carriers, etc., can solve the problems of high electrophilic synthesis cost, high synthesis difficulty, low yield, etc., and achieves strong affinity, simple and easy synthesis. The effect of line and radiation side effects is small

Inactive Publication Date: 2011-08-10
何玉林 +1
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Benefits of technology

This patented method allows for better detection of abnormalities associated with specific neurotransmitters called adrenal medulla or vasospinal cord receptors. It involves injecting certain substances into these tissues through small holes made in their skulls during surgery under conscious control from outside the body. These substance molecules have been labelled with different types of dyes like fluorescein, rhodopsin, cyanines, etc., allowing them to become visible when exposed to light at appropriate wavelengths. By measuring changes caused by these compounds, researchers may diagnose and treat disease more accurately without invasive procedures.

Problems solved by technology

This patented technical problem addressed in this patents relates to developing new compounds capable of detecting specific substances related to neuronal functions during normal or abnormal processes associated with inflammations caused by stress stimuli. These novel chemical entities should ideally provide superior sensitivity and accuracy compared to existing techniques.

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

Examples

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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

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Claims

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Application Information

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Owner 何玉林
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