Targeted malignant tumor resistance medicament and preparation method thereof
A malignant tumor and targeted technology, applied in the field of medicine, can solve the problems of high toxic and side effects, poor treatment effect, and patient pain, and achieve the effect of simple preparation method, low toxic and side effects, and easy realization
Inactive Publication Date: 2012-07-25
张俏男
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- Abstract
- Description
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- Application Information
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Problems solved by technology
Traditional malignant tumor treatment methods are mainly surgery, radiotherapy and chemotherapy, but these treatment methods not only bring great pain to patients, but also are prone to recurrence and metastasis after operation
At present, the drugs for malignant tumors have large toxic side effects and poor therapeutic effect, resulting in low immune function of patients. So far, no drugs with significant curative effect on malignant tumors have been developed. Therefore, it is imperative to innovate drugs targeting malignant tumors
Method used
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Embodiment Construction
[0008] The specific embodiments of the present invention will be described in detail below in conjunction with the examples.
[0009] A kind of compound of the present invention prepares targeting anticancer drug, and the name is 6-boronyl-3-amino-1,2,4-benzotriazine-1,4-dioxy compound (abbreviated as 10 BABD), the molecular formula is: C 7 h 8 N 4 o 4 10 B, whose structural formula is
[0010]
[0011] Its synthetic route is:
[0012]
[0013] Concrete preparation method comprises the following steps:
[0014] (1) Synthesis of 5-boronyl-benzofurazan-1-oxide: add 22 g of potassium hydroxide and 250 ml of ethanol with a volume concentration of 95% in the reactor, stir and dissolve, then add p-boronyl-1- 41g of nitro-2-amino-benzene, stir and heat to dissolve, slowly add 359ml of sodium hypochlorite solution with a volume concentration of 12% at 0°C dropwise below 10°C, continue stirring for 30min after the addition, and filter the filter cake with distilled water ...
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Abstract
The invention relates to a targeted malignant tumor resistance medicament and a preparation method thereof and can effectively solves the problem of medicaments for treating malignant tumors. The invention adopts the technical scheme that the preparation method comprises the following steps of: adding and dissolving ethanol into potassium hydroxide; adding p-boron acyl-1- nitro-2-amino- benzene; heating; dropwise adding sodium hypochlorite solution; carrying out suction filtration; washing a filter cake by distilled water; carrying out vacuum drying; recrystallizing by ethanol to obtain 5-boron acyl- benzofuroxan-1-oxide; adding ethanol and water into the 5-boron acyl- benzofuroxan-1-oxide; emulsifying; adding sodium cyanamide; after heating to perform the reaction, cooling until solid is separated out; carrying out suction filtration; adding glacial acetic acid into filtrate; separating out a golden red product; filtering; recrystallizing the filter cake by ethanol; and drying to obtain 6- boron acyl-3-amino-1,2,4- phentriazine-1,4-dioxide. The targeted malignant tumor resistance medicament has a simple preparation method, has a targeted effect, can be combined with the specificity of tumor cells and releases active ingredients, is effectively used for treating the malignant tumor, has good curative effect and low toxic or side effects and is safe and reliable.
Description
technical field [0001] The invention relates to the field of medicine, in particular to a drug targeting anti-malignant tumors and a preparation method thereof. Background technique [0002] Malignant tumor is a disease that is difficult to treat and has a high fatality rate. The number of deaths from malignant tumors in the world exceeds 10 million every year. This disease is becoming the number one killer of human beings in the new century. Traditional malignant tumor treatment methods are mainly surgery, radiotherapy and chemotherapy, but these treatment methods not only bring great pain to patients, but also are prone to recurrence and metastasis after operation. At present, the drugs for malignant tumors have large toxic side effects and poor therapeutic effect, resulting in low immune function of patients. So far, no drugs with significant curative effect on malignant tumors have been developed. Therefore, it is imperative to innovate drugs targeting malignant tumors ...
Claims
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IPC IPC(8): C07F5/02A61K31/69A61P35/00
Inventor 张俏男
Owner 张俏男