- Method for synthesizing equilin
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The invention relates to a synthesis method of a steroid drug, namely equilin. The method comprises the following steps: starting from estrone, performing phenolic hydroxyl group and C17-position ketal protection, and then performing oxidation and further dehydrogenation to obtain an intermediate II; reducing and deoxidizing the intermediate II to obtain an intermediate III; and finally, performing deprotection to obtain a final product, namely an equilin bulk drug. The method is few in steps and comprises four conversion steps; total yield is as high as 50%; the used raw materials are relatively cheap and easy to obtain; the whole process route is green and safe; and the bulk drug is high in quality, has purity of 99.8% or above, and is suitable for industrial production.
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Paragraph 0014; 0022
(2021/05/26)
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