Radioactive fluorine labeled Larotrectinib compound and preparation method thereof

A compound and labeling technology, which can be used in radioactive carriers, chemical instruments and methods, compounds of Group 4/14 elements of the periodic table, etc., and can solve problems such as no more effective technical means.
CN109705124AActive Publication Date: 2019-05-03SHANGHAI UNIV OF MEDICINE & HEALTH SCI
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Patent Information

Authority / Receiving Office
CN ยท China
Patent Type
Applications(China)
Current Assignee / Owner
SHANGHAI UNIV OF MEDICINE & HEALTH SCI
Publication Date
2019-05-03

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Abstract

The invention relates to a radioactive fluorine labeled Larotrectinib compound and a preparation method thereof, in particular, an in vivo imaging agent for Trk receptor subtype in refractory solid tumors, the present invention provides a radiofluorocompound 18F-Larotrectinib and 18F-Larotorectinib analogues based on a novel inhibitor Larotrectinib for tyrosine receptor kinase (TRK), and more particularly a preparation method of the Larotrectinib and its analogue radioactive fluorine-18 labeled compound 18F-Larotdirectinib and its 18F-Larotorectinib analogue. Compared with the prior art, the invention has the advantages of fast reaction speed, relatively mild condition, simple operation, short reaction time and simple post-treatment, and the prepared carrier-free radioactive label compounds have high radiochemical purity and positron emission characteristics, and PET-CT positron emission tomography can be used, so as to visually display the distribution of Larotrectinib compounds and their analogues in vivo and tumors, and a new imaging agent for early diagnosis of tumors is provided.
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Description

technical field

[0001] The invention relates to the field of chemical drug synthesis, especially in vivo imaging agents of Trk receptor subtypes in refractory solid tumors, in particular to a radioactive fluoride based on a novel inhibitor of tyrosine receptor kinase (TRK), Larotrectinib compound 18 F-Larotrectinib and its 18 F-Larotrectinib analogue, more particularly to a kind of Larotrectinib and its analogue radioactive fluorine-18 labeled compound 18 F-Larotrectinib and its 18 Process for the preparation of F-Larotrectinib analogues. Background technique

[0002] Larotrectinib was developed by Loxo Oncology as a broad-spectrum tumor drug for all tumor patients expressing tropomyosin receptor kinase (TRK). With strong selectivity, larotrectinib can inhibit tumor growth by inhibiting the TRK signaling pathway. Larotrectinib is an oral potent TRK inhibitor with consistent and durable antitumor activity in TRK fusion tumors, applicable to a wide range of patient ages a...

Claims

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