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2-methoxyestramustine and derivative thereof, and preparation method and application thereof

A technology for methoxy estradiol and derivatives is applied in the field of preparation of a new compound 2-methoxy estramustine and its derivatives, which can solve the problems affecting the quality of life of patients, adverse reactions, insufficient targeting, and the like, Achieve the effect of improving bioavailability, less adverse side effects, and improving water solubility

Active Publication Date: 2020-07-14
周亚耀
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, some tumor drugs currently used clinically, while achieving significant curative effects, are often accompanied by some side effects and adverse reactions, which cause great pain to patients and seriously affect the quality of life of patients.
[0003] Nowadays, there are many kinds of antineoplastic drugs clinically used, and nitrogen mustard antineoplastic drugs are one of them, such as cyclophosphamide, ifosfamide and azamethazone; these drugs are widely used clinically, but target Insufficient performance, serious side effects and other shortcomings seriously limit the wide application of nitrogen mustards.

Method used

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  • 2-methoxyestramustine and derivative thereof, and preparation method and application thereof
  • 2-methoxyestramustine and derivative thereof, and preparation method and application thereof
  • 2-methoxyestramustine and derivative thereof, and preparation method and application thereof

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Embodiment

[0032] The synthetic route of compound shown in formula 1 and formula 2 is as follows:

[0033]

[0034] The preparation method of the compound shown in the formula 1 comprises the following steps:

[0035]Dissolve 0.906g (3.0mmol) of 2-methoxy-1,3,5(10)-triene-3,17β-estradiol (5) in 30.0mL of dichloromethane, add 0.606g (6.0mmol ) triethylamine, and 0.037g (0.3mmol) 4-dimethylaminopyridine / DMAP, stirred at room temperature for 10 minutes; Add 5.0mL of dichloromethane slowly to the above reaction solution dropwise, the dropwise addition is completed within 10 minutes, continue to stir and react for 0.5 hours, then move the reaction solution to a water bath at 40°C for 2 hours, TLC detection shows that the reaction is complete , stop the reaction, cool the reaction solution to room temperature, add 50.0mL of distilled water, adjust the pH of the reaction solution between 5-6 with 10% hydrochloric acid solution under stirring, let the layers stand, separate the organic layer...

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Abstract

The invention discloses 2-methoxyestramustine and a derivative thereof. The structural formula of the 2-methoxyestramustine is shown as a formula 1-4. According to the 2-methoxyestramustine disclosedby the invention, 2-methoxyestradiol is used as a carrier, an alkylating agent (nitrogen mustard) is connected through carbamate to form a bifunctional drug molecular compound, the whole molecule is used as an anti-mitotic agent, and after carbamate is metabolized and hydrolyzed in vivo, 2-methoxyestradiol released by metabolite mediation can still continue to play an anti-tumor role. The derivative of the 2-methoxyestradiol can be used as the prodrug of the 2-methoxyestradiol. The invention also discloses a preparation method of the 2-methoxyestramustine and the derivative thereof, the preparation method can be used for preparing the 2-methoxyestramustine and the derivative thereof, and the yield is relatively high. The invention further discloses application of the 2-methoxyestramustineand the derivative thereof in a medicine for treating tumors or multiple myeloma.

Description

technical field [0001] The invention relates to the technical field of organic synthesis, in particular to a class of novel compound 2-methoxyestramustine and its derivatives, preparation method and application. Background technique [0002] At present, with the improvement of medical level, great progress has been made in tumor treatment. The survival period of cancer patients has been significantly prolonged and the quality of life has been significantly improved, mainly due to the invention and clinical application of various high-efficiency anti-cancer and anti-tumor drugs. . However, some tumor drugs currently used clinically, while achieving remarkable curative effects, are often accompanied by some side effects and adverse reactions, which cause great pain to patients and seriously affect the quality of life of patients. [0003] Nowadays, there are many kinds of antineoplastic drugs clinically used, and nitrogen mustard antineoplastic drugs are one of them, such as ...

Claims

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Application Information

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IPC IPC(8): C07J41/00C07J43/00C07J51/00A61K31/565A61K31/58A61P35/00
CPCC07J41/0072C07J43/003C07J51/00A61P35/00Y02P20/55
Inventor 周亚耀
Owner 周亚耀
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