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Positron emission tomography (PET) diagnostic radioactive drug and preparation method thereof

A radiopharmaceutical and positron tomography technology, applied in the directions of in vivo radioactive preparations, pharmaceutical formulations, preparations for in vivo experiments, etc., can solve the problems of insignificant advantages, inability to meet the requirements of PBRPET imaging research, etc., to reduce in vivo degradation, The effect of increasing steric hindrance and providing sensitivity

Active Publication Date: 2011-03-23
GUANGDONG HUIXUAN PHARMA TECH
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

because 11 C half-life is too short, only 20min, dynamic 11 The advantages of the C-PK11195PET study were not clear; moreover, 11 After C-PK11195 is produced, it can only be used in PET centers with cyclotrons, and cannot meet the needs of PET centers without cyclotrons nearby to carry out PBR PET imaging research.

Method used

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  • Positron emission tomography (PET) diagnostic radioactive drug and preparation method thereof
  • Positron emission tomography (PET) diagnostic radioactive drug and preparation method thereof
  • Positron emission tomography (PET) diagnostic radioactive drug and preparation method thereof

Examples

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Embodiment 1

[0026] N-[ 18 F] the preparation method of fluoroethyl-N-(1-methylpropyl)-1-(2-chlorophenyl) isoquinoline-3-carbamoyl, its preparation steps are as follows:

[0027] (1) Produced by accelerator 18 f - After being captured by the anion column QMA (Waters), it is eluted by the acetonitrile solution of sodium bicarbonate and cryptane K2.2.2, and the eluate is heated to azeotrope with acetonitrile to remove water, the azeotropic temperature is 82°C, and the time is 230 seconds. The cyclotron used may be produced by GE Company of the United States, and the model is PETtrace. Wherein, the component content of the acetonitrile solution of potassium carbonate and cryptane K2.2.2 is as follows:

[0028] Reagent name

Dosage

K 2 CO 3

30mg

pure water

1ml

K2.2.2

130mg

HPLC grade acetonitrile

10ml

[0029] (2) After cooling, add 0.25ml of 1,2-dibromoethane and acetonitrile to the residue, react at 85°C for 5min, cool...

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Abstract

The invention discloses a positron emission tomography (PET) diagnostic radioactive drug, N-[<18>F]fluoroethyl-N-(1-methylpropyl)-1-(2-chlorophenyl)isoquinoline-3-carbamoyl. The preparation method comprises the following steps: using <18>F<-> and 1,2-dibromoethane to react and prepare labeling intermediate 1-bromo-2-[<18>F]fluoroethane, then using 1-bromo-2-[<18>F]fluoroethane and precursor compound nor-PK11195 to perform alkylation reaction and obtain the finished product. In the method of the invention, [<18>F]ethyl structure is introduced in the molecule of PK11195 so as to increase the space steric effect of molecules, reduce the degradation in vivo of ligand molecules and further increase the signal-to-noise ratio of PET and sensitivity in the detection zone and effectively cover theshortage of the existing PET diagnostic radioactive drug.

Description

technical field [0001] The invention relates to the field of preparation methods of radiopharmaceuticals, in particular to a positron tomography diagnostic radiopharmaceutical and a preparation method thereof. Background technique [0002] Peripheral-type benzodiazepine receptors (PBR) are located in the mitochondrial outer membrane of cells in peripheral tissues and organs, including kidneys, intestinal epithelial cells, lungs, heart, and endocrine organs such as adrenal glands, testes, and pituitary glands, and in the central nervous system system. N-methyl-N-(1-methylpropyl)-1-(2-chlorophenyl)isoquinoline-3-carbamoyl (PK11195) is a known important PBR ligand, and its radioisotope Labeled radioligands such as N-[ 11 C] methyl-N-(1-methylpropyl)-1-(2-chlorophenyl) isoquinoline-3-carbamoyl ( 11 C-PK11195) and 123 I-PK11195 has been used in clinical PET and SPECT studies. Because PET imaging technology is superior to SPECT, therefore, PBR PET imaging has gradually replac...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K101/02A61K51/00
Inventor 王明芳
Owner GUANGDONG HUIXUAN PHARMA TECH
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