Preparation method and application of a class of aniline quinazoline compounds

A technology of aniline quinazolines and compounds, which is applied in the field of aniline quinazoline compounds and their preparation, can solve the problems of low yield, long labeling time, short half-life, etc., achieve high specific activity of radioactivity, simple and convenient separation, Effects with simple synthesis steps
CN103483277BActive Publication Date: 2015-09-02ZHEJIANG UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
ZHEJIANG UNIV
Publication Date
2015-09-02

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Abstract

The invention provides a class of aniline quinazoline compounds, namely quinazoline-4-aniline-2-(N,N,N-trialkyl) quaternary ammonium salt derivatives, which are radiochemically synthesized into 2-fluoro-18 The substituted derivatives, as precursors of fluorine-18 labeling, can be used in the preparation of tumor positron imaging agents. The imaging agent targets epidermal growth factor and can perform specific tumor imaging. The preparation method of the derivative of the present invention has the following advantages: the synthesis steps are simple, and only one step of fluorine-18 labeling the quaternary ammonium salt precursor is required to obtain the target compound; the radiochemical synthesis time is fast, and only needs 20-25 minutes; the separation is simple and convenient, and HPLC separation is not required , a Sep-Pak C-18 column can be used to obtain a product with a radiochemical purity of more than 98%, while removing the quaternary ammonium salt precursor; the radiochemical yield is high, and the uncorrected yield can reach 40-60%. High specific activity of radioactivity. The general structural formula is: .
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Description

technical field

[0001] The invention belongs to the field of medicine, and in particular relates to a class of aniline quinazoline compounds and their preparation method and application. This class of compounds can be used to radiochemically synthesize a class of positron imaging agents for tumor imaging. Background technique

[0002] Quinazolines are a class of important heterocyclic compounds with a wide range of uses and high biological activity, mainly for EGFR or its tyrosine kinase (EGFR-TK), vascular endothelial growth factor receptor (VEGFR), platelet-derived growth The inhibitory activity of PDGFR, Nerve Growth Factor Receptor (NGFR) and other multiple targets, thus exerting various pharmacological effects such as anticancer, antibacterial, antiviral, etc. In particular, 4-aniline quinazoline compounds are the most active and selective tyrosine kinase inhibitors discovered so far, and the main target of this type of compounds is EGFR. There are several anilinoquina...

Claims

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