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Sorafenib-ruthenium complex as well as preparation method and application thereof

A ruthenium complex, sorafenib technology, applied in the field of organic targeted drugs and synthesis, can solve the problems of unsatisfactory drug efficacy, unsatisfactory active drug release effect, etc., and achieve high efficiency, low toxicity, drug resistance, good cell light The effect of less toxicity and by-products

Active Publication Date: 2021-10-19
SHENZHEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to provide a Sorafenib-ruthenium complex and its preparation method, aiming to solve the technical problem that the existing active complexes have unsatisfactory release effect on the coupled active drug and lead to unsatisfactory drug efficacy

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  • Sorafenib-ruthenium complex as well as preparation method and application thereof
  • Sorafenib-ruthenium complex as well as preparation method and application thereof
  • Sorafenib-ruthenium complex as well as preparation method and application thereof

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preparation example Construction

[0030] Correspondingly, the embodiment of the present invention also provides a preparation method of the above-mentioned sorafenib-ruthenium complex. The process flow of the preparation method of the embodiment of the present invention Sorafenib-ruthenium complex is shown in the figure, the above structural formula 1 0 The preparation method of shown Sorafenib-ruthenium complex comprises the steps:

[0031] S01: dissolving Sorafenib and the ruthenium complex in the reaction solvent to prepare a mixed solution;

[0032] S02: In a dark and protective atmosphere, the mixed solution is subjected to a coordination reaction to generate a Sorafenib-ruthenium complex containing a cation shown in the following structural formula 1:

[0033] Wherein, the reactant ruthenium complex in step S01 can be a ruthenium complex commonly used in the art, such as the following chemical structural formula is the following structural formula 1 A Shown ruthenium complex; The chemical structural fo...

Embodiment 1

[0051] This embodiment provides a Sorafenib-ruthenium complex and its preparation method. The structural formula of the Sorafenib-ruthenium complex in this embodiment is the structural formula 1 in the following chemical reaction formula 1 1 shown.

[0052] The preparation method of the present embodiment Sorafenib-ruthenium complex comprises the following steps:

[0053] S1: Add ruthenium precursor ([Ru(bpy) 2 (Cl) 2 ]) (96.87mg, 0.20mmol) and Sorafenib (Sorafenib) (111.56mg, 0.24mmol) were added in a 1:4 volume ratio of water: ethanol mixed solvent (10mL);

[0054] S2: Purify by column chromatography after reflux reaction at 80°C for 6 hours in the dark to obtain the structural formula 1 1 The sorafenib-ruthenium complex shown.

[0055] After purification, structural formula 1 1 The yield of the sorafenib-ruthenium complex shown was 76%. Characterized by mass spectrometry and NMR, the ruthenium complex was successfully prepared. The molecular formula is: C 41 h 32 C...

Embodiment 2

[0059] This embodiment provides a Sorafenib-ruthenium complex and its preparation method. The structural formula of the Sorafenib-ruthenium complex in this embodiment is the structural formula 1 in the following chemical reaction formula 2 2 shown.

[0060] The preparation method of the present embodiment Sorafenib-ruthenium complex comprises the following steps:

[0061] The mixed solution after the reflux reaction in step S2 of Example 1 was cooled to room temperature and filtered to remove unreacted substances, the filtrate was collected, and a 10-fold excess saturated ammonium hexafluorophosphate aqueous solution (NH 4 PF 6 ), a dark red precipitate was precipitated, and the liquid was placed at a low temperature to precipitate more precipitates, filtered and washed twice with ice-deionized water and ether, respectively, to obtain a dark red solid with a yield of 76%.

[0062] Characterized by mass spectrometry and NMR, the ruthenium complex was successfully prepared. T...

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Abstract

The invention discloses a sorafenib-ruthenium complex as well as a preparation method and application thereof. The sorafenib-ruthenium complex contains cations as shown in a chemical structural formula 1. The preparation method of the sorafenib-ruthenium complex comprises the following steps: dissolving sorafenib and a ruthenium complex in a reaction solvent to prepare a mixed solution; and carrying out a coordination reaction on the mixed solution in a dark and protective atmosphere to generate the sorafenib-ruthenium complex, and the like. The sorafenib-ruthenium complex disclosed by the invention shows low toxicity to Hep-G2 liver tumor cells and normal liver cells in a dark environment; and the toxicity to liver tumor cells is enhanced under the illumination condition, and the compound can be used for photoactivation chemotherapy of tumors and can be applied to preparation of liver cancer targeted drugs.

Description

technical field [0001] The invention belongs to the technical field of organic targeted drugs and synthesis, and in particular relates to a sorafenib-ruthenium complex and its preparation method and application. Background technique [0002] With the in-depth study of cancer, researchers have found that tumor drug resistance has become a major limiting factor in cancer treatment. The underlying mechanisms of drug resistance are numerous, and each tumor has a unique set of features that determine tumor development and ultimately death. According to the latest global cancer data in 2020, liver cancer is the third most fatal malignant tumor in the world. Liver cirrhosis is its main risk factor, which is mainly caused by viral infection (mostly HBV or HCV) or alcoholic liver disease. The recurrence rate of liver cancer is high, 5 The annual survival rate is low. Although early-stage liver cancer can be treated with tumor resection and liver transplantation, and the prognosis i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07F15/00A61K31/44A61K41/00A61P1/16A61P35/00
CPCC07F15/0053A61P35/00A61P1/16A61K31/44A61K41/0057A61K41/0042A61K2300/00
Inventor 张平玉赖艺丹
Owner SHENZHEN UNIV
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