Novel pyrazolo[1,5-a]pyrimidines compound for labeling 18F instead of p-benzenesulfonyloxy and preparation and application

Abstract

The invention relates to a novel pyrazolo[1,5-a]pyrimidines compound for labeling 18F with p-benzenesulfonyloxy as the label locus, which is characterized in that the compound has matrix structure 3-cyanopyrazolo[1,5-a]pyrimidines; the fifth position of the matrix structure has substituents R which are respectively methyl and chloromethyl; and the amino on the seventh position is connected with fluorine-18 by a carbon chain with carbon atom number of n and has structure shown in the formula A. The compound is simple to synthesize and label and easy to operate. The compound maintains higher concentration and longer time in the tumor tissues, while the compound absorbs less or is fast in elimination in the normal tissues and blood, and especially has high tumor / blood ratio and tumor / muscle tissue ratio. The invention also relates to application of the compound as the PET brain tumor imaging agent.

Description

Technical field: The invention relates to a new type of toluenesulfonyloxy group as a leaving group 18 F-labeled pyrazolo[1,5-a]pyrimidine compound, its chemical preparation method and its application as a tumor (especially brain tumor) imaging agent for positron emission tomography (PET). Background technique: The early diagnosis of tumors is a hot topic in today's medicine, and positron emission tomography (PET) has received great attention as an increasingly popular means, so the breakthrough of early diagnosis of tumors depends on PET tumor imaging agents development. radionuclide 18 F is very suitable as an imaging nuclide for PET because of its excellent nuclide properties. Tumor occurrence is directly related to the cell cycle. Cyclin E and cyclin-dependent protein kinase 2 (CyclinE-CDK 2 ) complex in cell cycle G 1 It is directly related to the transition point of / S phase, which is the downstream target gene of various oncogenes, and plays a key role in the ...

AI Technical Summary

Problems solved by technology

Although 18 F-labeled pyrazolo[1,5-a]pyrimidines have not been reported as PET tumor imaging agents, but CDK 2 Overexpressed in tumor cells, as a CDK 2 Inhibitors of pyrazolo[1,5-a]pyrimidines 18 After F labeling, it has the potential to become a specific and targeted PET tumor imaging agent