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A kind of precursor compound of pet tracer and application thereof

A compound and composition technology, applied in the field of precursor compound of positron emission tomography imaging agent and its preparation, can solve the problems of low radiochemical yield, high radioactivity uptake, complicated preparation process, etc., and achieve simple preparation and easy operation Simple, short preparation time results

Active Publication Date: 2021-11-09
NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] Targeting Fibroblast Activation Protein: Radiosynthesis and Preclinical Evaluation of an 18 F-labeled FAP Inhibitor (J Nucl Medjnumed.120.242958 published ahead of print April 24, 2020) reported 18 F-labeled FAP compound 18 F-FGlc-FAP (as shown in the structure below), but 18 F-FGlc-FAP has the disadvantages of complex preparation process, long preparation time (90-110 minutes), low radiochemical yield (6%-15%), high radioactive uptake in bone tissue, and poor stability in vivo.

Method used

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  • A kind of precursor compound of pet tracer and application thereof
  • A kind of precursor compound of pet tracer and application thereof
  • A kind of precursor compound of pet tracer and application thereof

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Embodiment Construction

[0013] In the first aspect, the present invention provides a compound of formula (14) or a pharmaceutically acceptable salt thereof,

[0014] ,

[0015] Among them, R 1 for hydrogen or fluorine. In some embodiments, the R 1 for hydrogen. In some embodiments, the R 1 For fluorine.

[0016] In a second aspect, the present invention provides a compound of formula (13) or a pharmaceutically acceptable salt thereof,

[0017] ,

[0018] Among them, R 1 for hydrogen or fluorine. In some embodiments, the R 1 for hydrogen. In some embodiments, the R 1 For fluorine.

[0019] In the third aspect, the present invention provides a preparation method of the compound P-FAPI.

[0020] A preparation method of compound P-FAPI, comprising:

[0021] ,

[0022] The compound of formula (11) reacts with the compound of formula (12) in the first solvent in the presence of the first base and the first condensing agent, removes the first solvent under reduced pressure, then adds ...

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Abstract

The invention provides a precursor compound of PET agent and its preparation method and application, belonging to the field of radiopharmaceutical labeling. The PET agent and compound are simple to prepare, short in preparation time, high in radiochemical yield, and have the advantages of good stability in vivo and in vitro, high specificity, and high uptake, and can accurately and stably detect tumors or inflammatory sites and positioning.

Description

technical field [0001] The invention belongs to the field of radiopharmaceutical labeling, and in particular relates to a precursor compound of a Positron Emission Computed Tomography (PET) agent and a preparation method and application thereof. Background technique [0002] Fibroblast activation protein (FAP) is a membrane serine protease with two activities of dipeptidyl peptidase and collagenase, which can degrade dipeptide and type Ⅰ collagen. FAP is selectively expressed on the surface of stromal fibroblasts in more than 90% of epithelial malignant tumors, including breast cancer, ovarian cancer, lung cancer, colorectal cancer, gastric cancer, pancreatic cancer, skin melanoma, etc. FAP is not only present in tumors, but also expressed in some stromal activated diseases, such as wound healing, scar tissue, osteoarthritis, rheumatoid arthritis, and chronic inflammation such as granulation tissue, liver fibrosis, pulmonary fibrosis, cirrhosis etc., but generally not expre...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D401/14C07D401/12C07D215/50C07F5/06A61K51/04A61K31/4709A61K31/555A61P35/00A61P29/00A61P19/02A61P1/16A61P11/00
CPCA61K51/0455A61K51/0482A61P1/16A61P11/00A61P19/02A61P29/00A61P35/00C07B2200/05C07D215/50C07D401/12C07D401/14C07F5/069
Inventor 胡孔珍唐刚华苏金
Owner NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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