1174289-22-5Relevant articles and documents
Preparation method of bazedoxifene oxide
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Paragraph 0048; 0051, (2020/05/01)
The invention belongs to the technical field of medicines, and particularly relates to a preparation method of bazedoxifene oxide, wherein the preparation method comprises the steps: by using bazedoxifene free alkali as a raw material, dissolving in a first benign solvent, adding an organic alkali, and adding a silane protecting group to protect two phenolic hydroxyl groups, and thus obtaining anintermediate 1; dissolving the intermediate 1 in a second benign solvent, and adding an oxidant for oxidation to obtain an intermediate 2; and dissolving the intermediate 2 in a third benign solvent,and adding a protecting group removing reagent to remove two molecular silane protecting groups, and thus obtaining the bazedoxifene oxide. According to the preparation method of the bazedoxifene oxide provided by the invention, a preparation method of 1-[4-[2-(azacycloheptan-1-yl)ethoxy]benzyl]-2-(4-hydroxyphenyl)-3-methyl-1H-indole-5-phenol-N-oxide is provided, and the preparation method has important significance in effectively controlling the quality of bazedoxifene.