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Novel berberine derivative as well as synthesis method and application thereof

A technology of berberine and its derivatives, applied in the direction of organic chemical methods, chemical instruments and methods, isotope introduction into organic compounds, etc., can solve the problems of difficult synthesis of raw materials, difficult clinical transformation, low yield, etc., to achieve clinical transformation , Raw materials are easy to get, and the effect of reducing costs

Active Publication Date: 2021-01-22
WEST CHINA HOSPITAL SICHUAN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, the synthesis of raw materials for this series of compounds is difficult, the yield is very low, and it is difficult to achieve clinical transformation

Method used

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  • Novel berberine derivative as well as synthesis method and application thereof
  • Novel berberine derivative as well as synthesis method and application thereof
  • Novel berberine derivative as well as synthesis method and application thereof

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Embodiment Construction

[0043] In order to further illustrate the technical effect of the present invention, the present invention is specifically described below through examples.

[0044] 18 The specific preparation method of the novel berberine derivatives marked by F is as follows:

[0045]

[0046]Compound 1, (1 g, 2.69 mmol) was placed in a round bottom flask and connected to a water pump using a vacuum adapter. Turn on the water pump to evacuate, and when the vacuum is stable at 0.1Mpa, heat the oil bath to 170 degrees. Heat at this temperature for 1h, take out the vacuum bottle, cool to room temperature, and remove the water pump. The crude product was separated by column chromatography to obtain 0.85 g of compound 2 which was selectively demethylated at the 9-position, with a yield of 88.3%. 1H NMR()10.20(S,1H),8.66(S,1H),7.95(S,1H),7.14(S,1H),7.02(d,1H),6.82(d,1H),6.07(s, 2H), 5.35(S,1H), 4.45(dd,2H), 3.83(S,3H), 3.12(dd,2H).

[0047]

[0048] Compound 2 (300mg, 0.83mmol) was dis...

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Abstract

The invention discloses a novel berberine derivative as well as a synthesis method and application thereof, belongs to the field of imaging agents, and aims to derive the structure of isoquinoline alkaloid berberine, optimize derived sites on the basis of an early stage and introduce an F-containing side chain to prepare a series of probes with a myocardial targeting property. A 18F marker of theseries of compounds is successfully prepared through a marking experiment of positron nuclide 18F; the 18F-labeled novel berberine derivative is higher in myocardial uptake, raw materials are easy toobtain, the synthesis cost of a molecular probe is reduced, and clinical transformation is facilitated.

Description

technical field [0001] The invention belongs to the field of imaging agents, and in particular relates to a novel berberine derivative and its synthesis method and application. Background technique [0002] Although the diagnosis and treatment of coronary heart disease have made great progress in recent years, coronary heart disease is still one of the major diseases that seriously threaten human health worldwide (especially in European and American countries). In my country, the incidence and mortality of coronary heart disease and heart-related diseases are also on the rise. According to the latest data from the World Health Organization (WHO), my country will usher in the peak of cardiovascular diseases in the next five years or so. Therefore, early diagnosis, early intervention and prognosis evaluation of coronary heart disease and other heart-related diseases are particularly important. [0003] As a non-invasive diagnostic technique, myocardial perfusion imaging is pa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D455/03C07B59/00A61K51/04A61K101/02
CPCC07D455/03C07B59/002A61K51/0455C07B2200/05
Inventor 范成中吴小艾潘立立
Owner WEST CHINA HOSPITAL SICHUAN UNIV
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