Preparation method of levonorgestrel

Through a new preparation method, levonorgestrel is prepared through multiple-step reactions using 18-hydroxy-4-esten-3,17-dione raw materials, which solves the problems of high production costs, low conversion rates and environmental safety in the prior art, and achieves an efficient, environmentally friendly and safe production process.

CN119751532AActive Publication Date: 2025-04-04ZHEJIANG XIANJU PHARMA
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Patent Information

Application Number
CN202411965991.7
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2024-12-30
Publication Date
2025-04-04
Estimated Expiration
2044-12-30

AI Technical Summary

Technical Problem

The existing levonorgestrel synthesis method has problems such as high production costs, low conversion rates, unfriendly environment and poor safety, making it difficult to be suitable for large-scale industrial production.

Method used

levonorgestrel was prepared by iodine substitution, acetylene addition, ketal protection, methylation and hydrolyzing ketal reaction steps.

Benefits of technology

It achieves high conversion rate and high purity production of levonorgestrel, reduces production costs, improves the safety and environmental protection performance of the process, and is suitable for large-scale industrial production.

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Abstract

The invention discloses a preparation method of levonorgestrel, which comprises the following steps: carrying out iodine substitution on 18-hydroxy-4-estriene-3, 17-diketone to obtain a compound as shown in a formula 1; performing acetylene addition on the compound as shown in the formula 1 to obtain a compound as shown in a formula 2; performing ketal protection on the compound as shown in the formula 2 to obtain a compound as shown in a formula 3; methylating the compound as shown in the formula 3 to obtain a compound as shown in a formula 4; and carrying out hydrolysis ketal reaction on the compound as shown in the formula 4 to obtain levonorgestrel. The preparation method is easy and convenient to operate, high in safety and environmentally friendly, the safety, environmental protection and compliance cost in process production is greatly reduced, auxiliary materials are low in price and easy to obtain, industrial production and purchase are facilitated, and meanwhile the conversion rate is high.
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