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Boron-containing compound, pharmaceutical composition and preparation method and application of boron-containing compound

A boron compound and drug technology, applied in the field of boron-containing compounds and their preparation, can solve the problems of poor targeting and enrichment ability, and achieve the effects of inhibiting overexpression, good tumor targeting, and inhibiting growth

Active Publication Date: 2019-06-25
童永彭
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] The main purpose of the present invention is to provide a boron-containing compound, aiming to improve the problems that the boron agents used in boron neutron capture therapy do not have strong targeting and poor enrichment ability

Method used

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  • Boron-containing compound, pharmaceutical composition and preparation method and application of boron-containing compound
  • Boron-containing compound, pharmaceutical composition and preparation method and application of boron-containing compound
  • Boron-containing compound, pharmaceutical composition and preparation method and application of boron-containing compound

Examples

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preparation example Construction

[0041] In addition, the present invention also proposes a method for preparing a boron-containing compound, which includes the following steps: mixing the reactant and boric acid at a molar ratio of 1:15 to 1:10, adding to dimethyl sulfoxide to form a mixed solution, and Heating at 110-150° C. for 1.5-2 hours in a synthesis device, centrifugally filtering the product, recrystallizing with ethanol to obtain a precipitate, drying at 80-90° C. to obtain the boron-containing compound of the general structural formula (I) of the present invention. Wherein, the reactant is disodium adenosine triphosphate, disodium adenosine diphosphate or disodium adenosine monophosphate, and the reactant is preferably disodium adenosine triphosphate.

[0042] In addition, the present invention also proposes a pharmaceutical composition, including the above-mentioned boron-containing compound, and a pharmaceutically acceptable carrier, diluent or auxiliary agent.

[0043] Furthermore, the present in...

Embodiment 1

[0045] The synthetic route of the boron-containing compound of the present embodiment is:

[0046]

[0047] The preparation steps of the boron-containing compound in this example are as follows: mix 100 mg of adenosine triphosphate disodium with 100 mg of boric acid (the molar ratio is about 1:10), add 2000 μl of dimethyl sulfoxide to form a mixed solution, and 110-150 The reaction was heated at ℃ for 1.5 hours; the product was centrifugally filtered, recrystallized with ethanol to obtain a precipitate, and dried at 80 ℃ to finally obtain the product: adenosine triphosphate disodium borate, with a total yield of 32%. Among them, adenosine triphosphate disodium was purchased from BBI Life Science Co., Ltd., boric acid was purchased from Tianjin Damao Chemical Reagent Factory, and dimethyl sulfoxide was purchased from BBI Life Science Co., Ltd.

[0048] Infrared detection: use Nicolet 6700 Fourier infrared spectrometer, adopt tablet method to detect the infrared spectrogram o...

Embodiment 2

[0052] The synthesis route of the boron-containing compound in this example is the same as in Example 1. The preparation steps of the boron-containing compound in this example are: mix 100 mg of adenosine triphosphate disodium with 120 mg of boric acid, add 2200 μl of dimethyl sulfoxide to form a mixed solution, and Heating and reacting at 110-150°C in an organic synthesis device for 2 hours; centrifugally filtering the product, recrystallizing with ethanol to obtain a precipitate, and drying at 90°C to finally obtain the product: adenosine triphosphate disodium borate. Among them, adenosine triphosphate disodium was purchased from BBI Life Science Co., Ltd., boric acid was purchased from Tianjin Damao Chemical Reagent Factory, and dimethyl sulfoxide was purchased from BBI Life Science Co., Ltd. Using the same infrared detection, nuclear magnetic detection and mass spectrometry detection as in Example 1, the comprehensive analysis results show that the synthetic product is aden...

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Abstract

The invention discloses a boron-containing compound, a pharmaceutical composition and a preparation method and application of the boron-containing compound. The boron-containing compound has a generalstructural formula (I), and nucleotide substances serve as small molecules required by DNA synthesis and are easily taken up by rapidly proliferating tumor cells in a large amount, so that 10B atomscombined with the nucleotide substances enter the nucleus of tumor cells together, and the boron-containing compound can kill tumors more effectively after neutron irradiation. Secondly, the boron agent synthesized by the compound belongs to an epidermal growth factor receptor (EGFR) inhibitor, produces synergistic tumor growth inhibition effect with BNCT, competitively blocks ATP (adenosine triphosphate) and receptor tyrosine kinase domain to inhibit EGFR overexpression effect, prevents DNA repair of tumor cells, and further inhibits growth, migration, differentiation and survival of the tumor cells.

Description

technical field [0001] The invention relates to the field of boron-containing compounds, in particular to a boron-containing compound and its preparation method and application. Background technique [0002] At present, radiotherapy is a routine treatment for tumors, but it has poor effects on some special tumors that grow deep in the body, while Boron Neutron Capture Therapy (BNCT) has a better effect. BNCT is a 10 Unique particle radiation therapy of the B nuclear capture reaction, which in principle has significant advantages over conventional radiation therapy. The therapy mainly utilizes the high neutron capture cross-section 10 Molecules of element B react with neutrons to release particles to treat tumors. After injecting boron into the patient's body, 10 B will be selectively enriched in the tumor site, and the tumor will be irradiated with thermal neutrons, and the neutrons will interact with 10 B undergoes a neutron capture reaction, and the maximum energy of ...

Claims

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Application Information

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IPC IPC(8): C07H1/00C07H19/20A61K41/00A61P35/00
Inventor 童永彭王淼
Owner 童永彭
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