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Precursor compound of PET tracer agent and application of precursor compound

A technology of compounds and compositions, applied in the field of precursor compounds of positron emission tomography imaging agents and their preparation, can solve the problems of low radiochemical yield, poor in vivo stability, and high radioactive uptake

Active Publication Date: 2021-01-08
NANFANG HOSPITAL OF SOUTHERN MEDICAL UNIV
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  • Abstract
  • Description
  • Claims
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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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  • Precursor compound of PET tracer agent and application of precursor compound
  • Precursor compound of PET tracer agent and application of precursor compound
  • Precursor compound of PET tracer agent and application of precursor compound

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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 a PET agent and a preparation method and application of the precursor compound, which belong to the field of radiopharmaceutical labeling. The PET agentand the compound are simple to prepare, short in preparation time and high in radiochemical yield, have the advantages of good in-vivo and in-vitro stability, high specificity, high intake and the like, and can be used for accurately and stably detecting and positioning tumor or inflammatory parts.

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 Applications(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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