Synthesis method of < 18 > F-labeled benzamide dopamine receptor imaging agent
A technology of benzamide and synthesis method, applied in the direction of organic chemistry method, chemical instrument and method, in vivo radioactive preparation, etc., can solve the problems of complex synthesis method, difficult automatic production, low radiochemical yield, etc., and achieve high synthesis efficiency , easy mass production, and the effect of promoting mass production
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Embodiment 1
[0048] of this embodiment 18 A synthetic method of an F-labeled benzamide dopamine receptor imaging agent, such as figure 1 and image 3As shown, it includes a multifunctional synthesis module, which automatically synthesizes a benzamide-based dopamine receptor imaging agent, and the benzamide-based dopamine receptor imaging agent is purified by a C18 solid phase extraction column. The synthetic method comprises the following steps:
[0049] Step1: Prepare the reaction bottle, rinse it with deionized water for 5 minutes, and then dry it;
[0050] Step 2: Produced using a cyclotron 18 F ions were captured by a QMA anion exchange column;
[0051] Step3: Prepare 0.15ml-0.3ml aqueous potassium carbonate solution and 0.6ml-0.8ml aminopolyetheracetonitrile solution, wherein the molar concentration of potassium carbonate aqueous solution is kept at 0.3mol / L-0.45mol / L, and the molarity of aminopolyetheracetonitrile solution is maintained at 0.3mol / L-0.45mol / L. The concentration i...
Embodiment 2
[0074] This embodiment also provides a process for determining the radiochemical purity, such as figure 2 shown, including the following steps:
[0075] S1: Prepare the final product sample, prepare two groups according to the measurement method, sample A and sample B, each group of three samples, the three samples of a single group are placed at room temperature for 1h, 3h and 6h respectively, so as to obtain six samples;
[0076] S2: Spot sample A on one end of the silica gel paper, and use dichloromethane and methanol as the developing agent to expand upward, and the mass ratio of the two is 9:1;
[0077] S3: After drying, use a thin-layer scanner to detect, measure the radiochemical purity, and record the value;
[0078] S4: Enable C18 reversed-phase column, the mobile phase adopts acetonitrile solution, aqueous solution and triethylamine, and its mass ratio is 70:45:0.15;
[0079] S5: Take sample B for injection, measure the radiochemical purity, and record the value. ...
Embodiment 3
[0082] In this embodiment, as figure 1 Shown, positron emission tomography PET / CT images of normal healthy subjects and Parkinson's disease patients. like Figure 4 shown, normal healthy subjects and Parkinson's disease patients intravenously 18 F-Fethypride injection 370±185MBq, rest in bed for 1-1.5h, perform PET / CT scan, and reconstruct the PET / CT image with software. In normal and healthy subjects, the distribution of radiation in each lobe of bilateral cerebral cortex, basal ganglia, and thalamus is even and symmetrical, and there is no sparse or defective area of radioactive distribution. Most obvious.
[0083] To sum up, the embodiments of the present invention provide 18 F-labeled benzamide dopamine receptor imaging agents, namely 18The synthesis method of F-Fethypride is a nucleophilic substitution reaction synthesis method. Semi-preparative HPLC is used for purification, which can effectively remove impurities, not only has high synthesis efficiency, but also ...
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