Basic hydrolysis process for preparing 2-fluoro [18F]-2-deoxy-beta-D-glucose in single tube FDG acidic hydrolysis apparatus

A technology of acid hydrolysis and alkali hydrolysis, applied to sugar derivatives, sugar derivatives, chemical instruments and methods, etc., can solve the problems of high reaction temperature, low yield, long time, etc., achieve process stability, improve quality, improve yield effect

Inactive Publication Date: 2007-06-06
INST OF FIELD OPERATION SURGERY NO 3 MILITARY MEDICL UNIV PLA
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AI Technical Summary

Problems solved by technology

Although this set of equipment has the advantages of high degree of automation, stable preparation process, and high radiochemical purity of the product, the reaction temperature is high, the time is long, and the yield is low during acid hydrolysis to remove acetyl groups.

Method used

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  • Basic hydrolysis process for preparing 2-fluoro [18F]-2-deoxy-beta-D-glucose in single tube FDG acidic hydrolysis apparatus

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Embodiment Construction

[0015] The present invention will be described in further detail below in conjunction with the accompanying drawings and examples.

[0016] As shown in Figure 1, the single-tube FDG acid hydrolysis equipment produced by CTI Company of the United States is adopted, in which the rubber stopper 9 has 7 conduits, and there are 6 feeding bottles 1, 2, 3, 4, 5, 6, and each feeding bottle is connected correspondingly There are pneumatic valves V04, V08, V10, V12, V05, and V14, among which No. 1, 2, 3, 4, and 6 feeding bottles and corresponding pneumatic valves V04, V08, V10, V12, and V14 use single-tube FDG acid hydrolysis equipment The feeding bottle and pneumatic valve of the first set of synthesis system, the No. 5 bottle and the corresponding feeding valve can be "any group" in the second set of reaction system, here choose "No. 1 bottle, V05 valve". The 6 feeding bottles communicate with the reaction tube 8 through the conduit passing through the rubber stopper 9, and the reacti...

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Abstract

The present invention relates to positive electronic medicine preparation, and is especially basic hydrolysis process for preparing 2-fluoro[18F]-2-deoxy-beta-D-glucose (18F-FDG) in technologically reformed single tube FDG acidic hydrolysis apparatus. The basic hydrolysis process can reach all the quality indexes of 18F-FDG product, including radiochemical pure over 99.0 %, and has shortened preparation time from 50 min to 33 min, raised absolute yield from 40-45 % to 60-65 %, and stable technological process. Changing from acidic hydrolysis process to basic hydrolysis process makes the main side product changed from 2-chloro-2-deoxy-beta-D-glucose hard to metabolize in human body into glucose, and this raises the safety and effectiveness of the medicine greatly. Clinical application shows that the basic hydrolysis process 18F-FDG has the same clinical effect as the acidic hydrolysis process 18F-FDG.

Description

technical field [0001] This patent relates to the field of preparation of positron radioactive drugs, in particular to a single-tube FDG acid hydrolysis equipment for alkaline hydrolysis to prepare 2-fluoro[ 18 F]-2-deoxy-β-D-glucose ( 18 F-FDG) process. Background technique [0002] 18 F-FDG is the most widely used radiopharmaceutical in PET research, and is widely used in the diagnosis of malignant tumors, the determination of glucose metabolism in the myocardium and brain, etc. Due to its importance and wide applicability, since it was first reported in 1977, many literatures have reported 18 F-FDG preparation, and developed a variety of automated synthesis equipment. The preparation method that generally adopts at present is to synthesize 1,3,4,6-tetra-O-acetyl-2-fluoro[ 18 F]-β-D-mannopyranose ( 18 F-FDG-OAc 4 )which is 18 F-FDG precursor (Hamacher K, J Nucl Med, 1986, 27(2): 235-238.), followed by acid hydrolysis (PadgettHC, Appl Radiat Isot, 1989, 40(5): 433-4...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H5/02A61K51/04A61K101/02
Inventor 李奇明金榕兵范西江
Owner INST OF FIELD OPERATION SURGERY NO 3 MILITARY MEDICL UNIV PLA
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