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Sorafenib-ruthenium complex and its preparation method and application

A technology of ruthenium complexes and sorafenib, which is applied in the field of organic targeted drugs and synthesis, can solve problems such as unsatisfactory drug efficacy and unsatisfactory release effect of active drugs, and achieve high efficiency, low toxicity, drug resistance, and good cell photoresistence. Effects of toxicity and short synthetic route

Active Publication Date: 2022-07-12
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

Method used

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  • Sorafenib-ruthenium complex and its preparation method and application
  • Sorafenib-ruthenium complex and its preparation method and application
  • Sorafenib-ruthenium complex and its preparation method and application

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preparation example Construction

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

[0031] S01: dissolving sorafenib and 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 represented by 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 The ruthenium complex sh...

Embodiment 1

[0051] This embodiment provides a sorafenib-ruthenium complex and a preparation method thereof. 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 Sorafenib-ruthenium complex of the present embodiment comprises the following steps:

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

[0054] S2: Reflux reaction at 80°C in the dark for 6 hours, and then carry out column chromatography purification to obtain structural formula 1 1 Sorafenib-ruthenium complex shown.

[0055] After purification, structural formula 1 1 The yield of the Sorafenib-ruthenium complex shown was 76%. The ruthenium complex was successfully prepared by mass spectrometry and NMR characterization. The molecular formula i...

Embodiment 2

[0059] This embodiment provides a sorafenib-ruthenium complex and a preparation method thereof. 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 Sorafenib-ruthenium complex of the present embodiment comprises the following steps:

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

[0062] The ruthenium complex was successfully prepared by mass spectrometry and NMR ch...

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Abstract

The invention discloses a sorafenib-ruthenium complex and its preparation method and application. The sorafenib-ruthenium complex contains a cation represented by chemical structural formula 1. The preparation method of sorafenib-ruthenium complex includes: dissolving sorafenib and ruthenium complex in a reaction solvent to prepare a mixed solution; in a light-proof and protective atmosphere, performing a coordination reaction on the mixed solution to generate sorafenib Rafenib-ruthenium complex and other steps. The sorafenib-ruthenium complex of the present invention exhibits low toxicity to Hep-G2 liver tumor cells and normal liver cells in a dark environment; and enhances the toxicity to liver tumor cells under light conditions, and can be used for tumor light therapy Activation chemotherapy can be used in the 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 a preparation method and application thereof. Background technique [0002] As the study of cancer intensifies, researchers have discovered that tumor resistance has become a major limiting factor for cancer treatment. The underlying mechanisms of drug resistance are numerous, and each tumor has a unique set of characteristics that determine tumor development and ultimately death. The latest global cancer data in 2020 shows that liver cancer is the third malignant tumor with a global mortality rate, and 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 by tumor resection, liver transplantation and o...

Claims

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Application Information

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Patent Type & Authority Patents(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