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Preparation method of pure acetic acid bazedoxifene crystal form A

A technology of xifen crystal form and acetic acid, which is applied in the field of preparation of pure bazedoxifene acetate crystal form A, can solve the problems of high drug prices, complicated processes, and high production costs, and achieve easy operation, simple process, and improved production efficiency. The effect of production efficiency

Inactive Publication Date: 2017-05-31
成都归合科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The existing method for preparing bazedoxifene acetate has complicated processes and high production costs, resulting in high drug prices

Method used

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  • Preparation method of pure acetic acid bazedoxifene crystal form A
  • Preparation method of pure acetic acid bazedoxifene crystal form A
  • Preparation method of pure acetic acid bazedoxifene crystal form A

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Such as figure 1 Shown, a kind of preparation method of pure bazedoxifene acetate crystal form A comprises the following processing steps:

[0020] (1) Take 500ml of absolute ethanol as a solvent, add 50g of raw materials, 1.5g of palladium carbon, flow hydrogen, and react in a closed room at room temperature for 2h;

[0021] (2) Filter off the palladium carbon, first add 2.5g acetic acid dropwise to the filtrate at room temperature, stir for 30min, cool to -5°C ~ 0°C, then add 2.5g acetic acid dropwise, stir for 30min, warm up to room temperature, then add 2.5g dropwise Acetic acid, stirred for 30 min, filtered and dried to obtain the crude product of crystal form A.

Embodiment 2

[0023] A preparation method of pure bazedoxifene acetate crystal form A, comprising the following processing steps:

[0024] (1) Take 200ml of anhydrous methanol as a solvent, add 30g of raw materials, 1.0g of palladium carbon, flow hydrogen, and react in a closed room at room temperature for 2h;

[0025] (2) Filter out palladium carbon, first add 1.5g acetic acid dropwise to the filtrate at room temperature, stir for 30min, cool to -10°C ~ 15°C, then add 1.5g acetic acid dropwise, stir for 30min, warm up to room temperature, then add 1.5g dropwise Acetic acid, stirred for 30 min, filtered and dried to obtain the crude product of crystal form A.

Embodiment 3

[0027] A preparation method of pure bazedoxifene acetate crystal form A, comprising the following processing steps:

[0028] (1) Take 400ml of anhydrous isopropanol as a solvent, add 40g of raw materials, 1.3g of palladium carbon, flow hydrogen, and react in a closed room at room temperature for 2h;

[0029] (2) Filter out the palladium carbon, first add 2 g of acetic acid dropwise to the filtrate at room temperature, stir for 30 min, cool to -10°C to 0°C, then add 2 g of acetic acid dropwise, stir for 30 min, warm up to room temperature, then add 2 g of acetic acid dropwise, and stir After 30 minutes, it was filtered and dried to obtain the crude product of Form A.

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PUM

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Abstract

The invention discloses a preparation method of a pure acetic acid bazedoxifene crystal form A. The preparation method comprises the following process steps of firstly, under the condition of using palladium carbon as a catalyst, dissolving raw materials into a good organic solvent, and introducing hydrogen to react to a non-raw material point; after reaction is completed, filtering to remove the palladium carbon, cooling filtrate, adding acetic acid and a poor organic solvent, stirring, crystallizing, filtering, and drying, so as to obtain a crude product of the crystal form A. The preparation method has the advantages that the technology is simple, the production efficiency is high, and the preparation cost of the pure acetic acid bazedoxifene crystal form A is effectively reduced.

Description

technical field [0001] The invention relates to the field of chemical pharmacy, in particular to a preparation method of pure bazedoxifene acetate crystal form A. Background technique [0002] Bazedoxifene acetate is a new generation of selective estrogen receptor modulators. It can competitively inhibit the binding of 17α-estradiol to ERα and ERβ, has estrogen agonist activity on bones, and can improve the bone density of the spine and hip, so it can significantly reduce the vertebral bone density of postmenopausal women with osteoporosis fracture risk. It has no agonist activity against human breast cancer cell lines when used alone, and its primary indication is the treatment and prevention of postmenopausal osteoporosis. The existing method for preparing bazedoxifene acetate has complex processes and high production costs, which lead to high drug prices. Contents of the invention [0003] In order to solve the above problems, the present invention discloses a method...

Claims

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Application Information

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IPC IPC(8): C07D209/12C07C53/10C07C51/41
CPCC07B2200/13C07D209/12
Inventor 刘蓉
Owner 成都归合科技有限公司
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