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Deuterated piperidone as well as preparation method and application thereof

A technology of deuterated piperidinone and piperidinone, which is applied in the field of deuterated piperidinone and its preparation, can solve the problems of secondary injury to patients, inability to track the metabolic process, etc., and achieves reliable results, simple and practical methods, and easy to use. effect of implementation

Inactive Publication Date: 2021-02-05
深圳鼎邦生物科技有限公司
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Problems solved by technology

[0004] In view of the above-mentioned deficiencies in the prior art, the purpose of the present invention is to provide a deuterated piperidone and its preparation method and application, aiming to solve the problem of using 1 haloperidone as a coronary contrast agent in the prior art, which is difficult for patients. The first detection is easy to cause secondary damage, and it cannot be used as a tracking problem for the entire metabolic process

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  • Deuterated piperidone as well as preparation method and application thereof
  • Deuterated piperidone as well as preparation method and application thereof
  • Deuterated piperidone as well as preparation method and application thereof

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Embodiment Construction

[0016] In order to more clearly illustrate the purpose, technical solutions and advantages of the embodiments of the present invention, the present invention will be further described below in conjunction with the embodiments, and a clear and complete description will be made. Obviously, the described embodiments are part of the embodiments of the present invention. rather than all examples. Based on the embodiments of the present invention, all other embodiments obtained by persons of ordinary skill in the art without making creative efforts belong to the protection scope of the present invention.

[0017] The present invention provides a kind of deuterated piperidone, its general chemical structure formula is:

[0018] Wherein, at least one of R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 is deuterium.

[0019] As an example, the chemical structural formula of the deuterated piperidone is:

[0020]

[0021]

[0022]

[0023]

[0024] one o...

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Abstract

The invention discloses deuterated piperidone as well as a preparation method and application thereof, the chemical structural formula of the deuterated piperidone is shown in the specification, and at least one of R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 is deuterium. The deuterated piperidone is used as a coronary artery contrast agent or a tumor contrast agent, metabolite to which the deuterated piperidone is transferred can be tracked, the detection resolution and sensitivity are higher, dynamic exchange of a single metabolite can be detected, and by measuring the change of a 1H proton magnetic resonance spectrum, metabolites which cannot be detected by a 2H proton magnetic resonance spectrum can be detected under high spectral resolution, so that the in-vivo metaboliccycle rate is obtained, the steady-state information and metabolic rate of several metabolites can be provided by one-time collection, and no harm is caused to a human body after multiple times of detection.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a deuterated piperidone and its preparation method and application. Background technique [0002] Positron emission tomography (PET), as the most advanced medical imaging technology at present, can realize high-resolution imaging of cell metabolism and function, and conduct non-invasive, three-dimensional and dynamic research on the physiological and biochemical processes of the human body from the molecular level. The application of PET to tumors includes diagnosis of tumors, identification of benign and malignant tumors, early diagnosis and identification of malignant tumors, classification, recurrence, and metastasis, selection of treatment options, monitoring of chemotherapy effects, observation of tumor changes and prognosis. detection. PET examination is different from other examinations in that it relies on positron drugs (PET drugs), which rely on the specific concentra...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D231/32A61K49/06
CPCA61K49/06C07B2200/05C07D231/32
Inventor 杨晓军阮英恒李换锡
Owner 深圳鼎邦生物科技有限公司
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