Preparation method and application of [<11>C]-omega-mercaptomethyl fatty acid

A mercaptomethyl fatty acid, -11C technology, applied in the field of medicine, can solve the problem of low ratio of myocardial uptake to non-target organs, and achieve the effects of significant economic and social value, simple preparation method and fast clearance rate

Inactive Publication Date: 2016-04-27
HENAN UNIV OF CHINESE MEDICINE
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Problems solved by technology

[0003] For above-mentioned situation, in order to solve the defective of prior art, the purpose of the present invention is exactly to provide a kind of [ 11 The preparation method and application of C]-ω-mercaptomethyl fatty acid can effectively solve the problem of low ratio of myocardial uptake to non-target organs of existing myocardial metabolic imaging agents

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  • Preparation method and application of [&lt;11&gt;C]-omega-mercaptomethyl fatty acid
  • Preparation method and application of [&lt;11&gt;C]-omega-mercaptomethyl fatty acid
  • Preparation method and application of [&lt;11&gt;C]-omega-mercaptomethyl fatty acid

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Embodiment 1

[0026] In the specific implementation of the present invention, [ 11 C]-16-mercaptomethylhexadecanoic acid ([ 11 C]-MTPA) preparation method is:

[0027] The first step: use a cyclotron (HM-12) with a target current of 30 microamps in the atmosphere containing 5% O 2 N 2 in, yes 14 N(p,a)- 11 C carried out proton radiation for 20 minutes, and obtained [26-30GBq or 702-810mCi 11 C]-CO 2 , via N 2 Airflow sent to [ 11 C]-methyl iodide Microlab synthesis module;

[0028] Step 2: Install the Microlab synthesis module in the first glass reaction vial, [ 11 C]-CO 2 LiAlH 4 / THF solution catalytic reduction to [ 11C]-CH 3 O-Al complex, LiAlH 4 / THF solution concentration is 5-40mg / mL, dosage 0.1-0.5mL, then reacts at room temperature in mass concentration 40-60% hydroiodic acid aqueous solution 0.2-0.5mL to obtain [ 11 C]-CH 3 I, the [ 11 C]-CH 3 I blow into the second glass reaction bottle containing 0.5-1mg of 16-mercaptopalmitic acid precursor, 0.4-0.6ml of metha...

Embodiment 2

[0031] In the specific implementation of the present invention, [ 11 C]-14-mercaptomethyltetradecanoic acid ([ 11 C]-MTMA) preparation method is:

[0032] The first step: use a cyclotron (HM-12) with a target current of 30 microamps in the atmosphere containing 5% O 2 N 2 in, yes 14 N(p,a)- 11 C carried out proton radiation for 20 minutes, and obtained [26-30GBq or 702-810mCi 11 C]-CO 2 , via N 2 Airflow sent to [ 11 C]-methyl iodide Microlab synthesis module;

[0033] Step 2: Install the Microlab synthesis module in the first glass reaction vial, [ 11 C]-CO 2 LiAlH 4 / THF solution catalytic reduction to [ 11 C]-CH 3 O-Al complex, LiAlH 4 / THF solution concentration is 5-40mg / mL, dosage 0.1-0.5mL, then reacts at room temperature in mass concentration 40-60% hydroiodic acid aqueous solution 0.2-0.5mL to obtain [ 11 C]-CH 3 I, the [ 11 C]-CH 3 I was blown into the second glass reaction bottle containing 0.5-1 mg of 14-mercaptotetradecanoic acid precursor, 0.4-0...

Embodiment 3

[0036] In the specific implementation of the present invention, [ 11 C]-12-mercaptomethyldodecanoic acid ([ 11 C]-MTDA) preparation method is:

[0037] The first step: use a cyclotron (HM-12) with a target current of 30 microamps in the atmosphere containing 5% O 2 N 2 in, yes 14 N(p,a)- 11 C carried out proton radiation for 20 minutes, and obtained [26-30GBq or 702-810mCi 11 C]-CO 2 , via N 2 Airflow sent to [ 11 C]-methyl iodide Microlab synthesis module;

[0038] Step 2: Install the Microlab synthesis module in the first glass reaction vial, [ 11 C]-CO 2 LiAlH 4 / THF solution catalytic reduction to [ 11 C]-CH 3 O-Al complex, LiAlH 4 / THF solution concentration is 5-40mg / mL, dosage 0.1-0.5mL, then reacts at room temperature in mass concentration 40-60% hydroiodic acid aqueous solution 0.2-0.5mL to obtain [ 11 C]-CH 3 I, the [ 11 C]-CH 3 I was blown into the second glass reaction bottle containing 0.5-1mg of 12-mercaptododecanoic acid precursor, 0.4-0.6ml of...

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Abstract

The invention relates to a preparation method and an application of [<11>C]-omega-mercaptomethyl fatty acid. The problem of low ratio of myocardial uptake to non-target organ uptake of a conventional myocardial metabolism imaging agent can be effectively solved. The method comprises steps as follows: [<11>C]-CO2 for emitting a positive electron has a proton reaction through <14>N (p,a)-<11>C and then a product is sent to a [<11>C]-iodomethane Microlab synthesis module; the Microlab synthesis module is mounted in a first glass flask, the product is reduced into a [<11>C]-CH3O-Al complex, the [<11>C]-CH3O-Al complex reacts in an aqueous hydroiodic acid solution, [<11>C]-CH3I is obtained and is blown to a second glass flask containing omega-mercapto-fatty acid precursors, methyl alcohol and sodium hydroxide through helium flow for reaction, and a reaction mixture is obtained; the reaction mixture is cooled, a solvent is removed through pressure reduction, the reaction mixture is dissolved with a phosphate buffer solution and is filtered, and [<11>C]-omega-mercaptomethyl fatty acid is obtained. The preparation method is simple, the production is easy, [<11>C]-omega-mercaptomethyl fatty acid is effectively applied to preparation of the myocardial metabolism imaging agent, the myocardial imaging is clear, a clear cardiac Micro-PET image can be acquired, and the cost is low.

Description

technical field [0001] The present invention relates to the field of medicine, especially a kind of [ 11 C]-ω-mercaptomethyl fatty acid preparation method and application. Background technique [0002] Myocardial metabolic imaging based on positron emission tomography (PET) has gradually become an important means of non-invasive and accurate diagnosis and prognosis of myocardial ischemia and other diseases reflecting cardiac insufficiency. Despite decades of [ 18 F]-FDG has been used as the gold standard for PET myocardial metabolic imaging, but [ 18 F]-FDG can not accurately distinguish between hypoxic myocardium and normal myocardium. A fatty acid myocardial metabolism tracer that has higher myocardial uptake and can better distinguish diseases such as myocardial hypoxia is particularly important. Over the past few decades, various radionuclides labeled with different fatty acids (except 99m Metallic radionuclides such as Tc) have shown excellent performance as valuabl...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C323/52C07C319/14A61K51/04A61K101/00
CPCA61K51/0402C07C17/16C07C29/159C07C319/14C07C323/52C07C31/04C07C19/07
Inventor 武香香曾华辉
Owner HENAN UNIV OF CHINESE MEDICINE
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