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Novel estriol preparing method

A technology for estriol and dimethoxyestradiol, which is applied in the new field of estriol preparation, can solve the problems of large consumption of reagents, expensive reagents, low yield and content, etc., and achieves short reaction time and reagent consumption. Small, cheap reagents

Inactive Publication Date: 2015-12-02
湖北三晶生物科技股份有限公司
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Problems solved by technology

[0006] The purpose of the present invention is to overcome the defect of prior art, provide a kind of new preparation method of estriol, it can effectively solve the problem that the reagent used in the prior art is expensive, the reaction route time is long, the consumption of reagent is big, can not effectively control The production of impurity epiestriol, and the problem of low yield and content, is more suitable for industrial production

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preparation example Construction

[0016] The embodiment of the present invention provides a new preparation method of estriol, comprising the following steps:

[0017] Step 1: Using estrone 1 to react with isopropenyl acetate (IsopropenylAcetate) to prepare estrone diacetate compound 2; in the step 1, using p-toluenesulfonic acid as a catalyst. The following is the chemical reaction equation:

[0018]

[0019] Step 2: reacting the estrone diacetate compound 2 with N-bromosuccinimide (NBS) to prepare 16-bromoestrolone acetate 3; wherein, the reaction temperature of the step 2 is - 20°C to -10°C. The following is the chemical reaction equation:

[0020]

[0021] Step 3: The 16-bromoestrolone acetate 3 is reacted in the environment of sodium hydroxide (NaOH) and methanol to prepare 17,17-dimethoxyestradiol 4; the chemical reaction equation is as follows:

[0022]

[0023] Step 4: The 17,17-dimethoxyestradiol 4 is hydrolyzed with hydrochloric acid (HCL) to obtain 16α-hydroxyestradiol 5; the reaction te...

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Abstract

The invention relates to a novel estriol preparing method. The novel estriol preparing method includes the following steps: 1, estrone is reacted with isopropenyl acetate to prepare an estraene diacetate compound; 2, the estraene diacetate compound is reacted with N-bromosuccinimide to prepare 16-bromo-acetic-acid estrone; 3, the 16-bromo-acetic-acid estrone is reacted in the environment of sodium hydroxide and methyl alcohol to prepare 17,17-dimethoxy-estradiol; 4, a hydrolysis reaction is carried out on the 17,17-dimethoxy-estradiol and hydrochloric acid, and 16alpha-hydroxy-estrone is obtained; 5, a reduction reaction is carried out on the 16alpha-hydroxy-estrone, and estriol can be obtained. When the estriol is prepared with the novel estriol preparing method, the reagents used for preparing are low in price, the reaction time is short, consumption of the reagents required by the reaction is small, and the content of the prepared estriol is high; meanwhile, epiestriol serving as impurities is effectively controlled, and the novel estriol preparing method is suitable for industrial production.

Description

technical field [0001] The invention relates to a new method for preparing estriol, which belongs to the field of medicinal chemistry. Background technique [0002] Estriol is a metabolite of estradiol in the body and is a natural estrogen mainly found in urine. Its oral estrogenic activity is about 6 times that of estrone, but weaker than estradiol. It is made into a variety of dosage forms with pharmaceutical excipients, and is clinically used for the treatment of various gynecological diseases and menopausal diseases. [0003] Estriol has the effect of rapidly increasing peripheral leukocytes, and is effective for leukopenia caused by chemotherapy or radiotherapy. It can also reduce the permeability and fragility of blood vessels, and can be used for the treatment of various bleedings. [0004] The synthesis technique of estriol mainly has the following defects at present: 1. use peroxyacid in the reaction, the time is longer, and part of the reactant is converted into...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J1/00
Inventor 尹宏
Owner 湖北三晶生物科技股份有限公司
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