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Preparation system and preparation method of Al<18>F-PSMA-BCH

A technology of al18f-psma-bch and preparation system, which is applied in organic chemistry methods, chemical instruments and methods, introduction of heterocyclic compound isotopes, etc., can solve problems such as radiation damage to operators, low labeling rate, and long labeling time, and achieve Effects of improving yield and specific activity, ensuring labeling rate, and ensuring accuracy

Inactive Publication Date: 2020-03-31
BEIJING CANCER HOSPITAL PEKING UNIV CANCER HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, relatively 68 Ga-labeled, conventional 18 The F labeling method has disadvantages such as long labeling time, high reaction temperature, strict anhydrous requirements, and low labeling rate.
[0004] As described in the patent application number 201710368982.3 "Al 18 F-labeled PSMA targeting inhibitor and its preparation method and application", Al 18 The marking of F-PSMA-BCH mainly adopts the method of manual marking, because 18 The output of F manual labeling is limited, and the concentration has a great influence on the labeling rate. During the labeling process, a large number of carrier-free samples are usually loaded and washed. 18 F-, and actually in the marking process, only need to use one-fourth to one-fifth of the amount, so that in the preparation of Al 18 F-PSMA-BCH will need to take out a lot of free carrier-free 18 F-, which greatly increases the radioactivity to which operators are directly exposed, and operators often suffer from radiation damage due to unnecessary overexposure

Method used

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  • Preparation system and preparation method of Al&lt;18&gt;F-PSMA-BCH
  • Preparation system and preparation method of Al&lt;18&gt;F-PSMA-BCH

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Embodiment 1

[0040] see figure 1 , this example provides an Al 18 The preparation system of F-PSMA-BCH comprises the first washing unit, anion exchange column 20, fluorination reaction bottle 6 and purification unit;

[0041] The first washing unit communicates with the anion exchange column 20;

[0042] Anion exchange column 20 is used to capture the 18 f - , the anion exchange column 20 communicates with the fluorination reaction bottle 6 through the first pipeline 10;

[0043] Fluorination reaction bottle 6 built-in contains precursor compound, AlCl 3 And the aqueous solution of pH buffering agent, the Al of fluorination reaction bottle 6 output output by second pipeline 11 18 F-PSMA-BCH aqueous solution, a purification unit is installed on the second pipeline 11;

[0044] Purification unit is used to remove Al from reaction output 18 Free in F-PSMA-BCH aqueous solution 18 f - .

[0045] Depend on figure 1 As can be seen from the shown structure, the present embodiment realiz...

Embodiment 2

[0067] This embodiment is based on Al described in embodiment 1 18 The preparation system of F-PSMA-BCH specifically provides an Al 18 The preparation method of F-PSMA-BCH, see figure 2 ,include:

[0068] S1, capture 18 f - , will capture the 18 f - Adding to the fluorination reaction bottle loaded with the aqueous solution of the precursor compound, AlCl3 and pH buffer to carry out the fluorination reaction;

[0069] S2, remove the Al output from the fluorination reaction bottle after the reaction 18 Free in F-PSMA-BCH aqueous solution 18 f - .

[0070] Further, in step S1 of this embodiment, it includes using an anion exchange column 20 to capture H 18 F target aqueous solution 18 f - , and the 0.4mL of physiological saline loaded in the second vial 2 washes the trapped on the anion exchange column 20 18 f - , so that the captured 18 f - Add it into the fluorination reaction bottle 6, wherein, using 0.4mL physiological saline can ensure the minimum volume, a...

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Abstract

The invention relates to the technical field of medicinal chemistry, and provides a preparation system and a preparation method of Al18F-PSMA-BCH. The preparation system comprises a first flushing unit, an anion exchange column, a fluorination reaction bottle and a purification unit, wherein the first flushing unit is communicated with the anion exchange column; the anion exchange column is communicated with the fluorination reaction bottle through a first pipeline; the fluorination reaction bottle is loaded with an aqueous solution containing a precursor compound, AlCl3 and a pH buffer agent;the fluorination reaction bottle outputs the produced aqueous Al18F-PSMA-BCH solution through a second pipeline; and a purification unit is installed on the second pipeline. According to the invention, 18F<-> in a target aqueous solution is captured through the anion exchange column, and free 18F<-> in the produced aqueous solution output through a reaction is removed through the purification unit, so the yield and the specific activity of a labeled product are improved, the purity of the obtained produced aqueous solution is high, and the influence of the free 18F<-> on the diagnosis resultof a patient is correspondingly reduced.

Description

technical field [0001] The invention relates to the technical field of medicinal chemistry, in particular to an Al 18 Preparation system and preparation method of F-PSMA-BCH. Background technique [0002] At present, prostate cancer is one of the important diseases threatening men's health. In my country, the incidence of prostate cancer is increasing year by year, and most patients are diagnosed with advanced prostate cancer. Early diagnosis and early treatment have always been an important means to improve the cure rate of tumors and the survival rate of patients. [0003] Prostate-specific membrane antigen (PSMA) is specifically highly expressed in prostate cancer and its metastatic cells, and is significantly related to the malignancy of the tumor. In recent years, small molecule probes targeting PSMA have been extensively studied, among which 68 Ga and 18 F-labeled molecular probes were predominant. compared to 68 For Ga, 18 F has its unique advantages, such as ...

Claims

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Application Information

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IPC IPC(8): C07D255/02C07B59/00
CPCC07B59/002C07B2200/05C07D255/02
Inventor 杨志刘特立朱华杨建华
Owner BEIJING CANCER HOSPITAL PEKING UNIV CANCER HOSPITAL
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