The preparation method of bazedoxifene acetate polymorph a

A technology of bazedoxifene acetate and bazedoxifene, applied in the direction of organic chemistry, to achieve the effects of high product yield, high crystal purity and convenient operation
CN107628982BActive Publication Date: 2021-03-23SUZHOU LIXIN PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SUZHOU LIXIN PHARMA
Publication Date
2021-03-23

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Abstract

The present invention discloses a Bazedoxifene Acetate polymorphism A preparation method, wherein a raw material Bazedoxifene free alkali is dissolved in a single solvent methanol, and salt forming and crystallization are performed to directly obtain the high-purity Bazedoxifene Acetate polymorphism A. According to the present invention, the preparation method has characteristics of simple process, economy and environmental protection, and is suitable for industrial production.
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Description

technical field

[0001] The invention belongs to the technical field of preparation of raw materials and intermediates, and in particular relates to a preparation method of polymorphic form A of bazedoxifene acetate, a new generation of selective estrogen receptor modulator. Background technique

[0002] Bazedoxifene Acetate is a small molecule drug originally developed by Wyeth and later acquired by Pfizer. Bazedoxifene acetate was first launched in Italy and Spain with the approval of the European Medicines and Drug Administration (EMEA) in April 2009, with the product name Conbriza; in July 2010, it was launched in Japan with the product name Viviant; in October 2013, it was launched in the United States. Approved by the Food and Drug Administration (FDA), it is marketed in the United States under the trade name Duavee for the treatment of moderate to severe menopause-related vasomotor symptoms (hot flashes) and the prevention of postmenopausal osteoporosis in postmenopaus...

Claims

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