Process optimizations for the synthesis of an intermediate of dydrogesterone.

ABSTRACT: Dydrogesterone (DG) is a potent progesterone drug that can be used to treat almost all progesterone-deficiency in women. However, there are few reports on DG process studies, and the by-products are unclear, which make the process optimization challenging. In this paper, we report the process optimization studies for the synthesis of 9α,10β-pregest-5,7-diene-3,20-diethylene glycol ketone (1), an intermediate of DG. Starting from the natural raw progesterone, the intermediate 1 was synthesised via a three-step process involving ketal protection, allylic bromination and elimination. We synthesised and characterised the main by-products in the process route, and explored the effects of conditions such as feed amount, temperature and types of bases on the yield and selectivity. Compared

SUBMITTER: Wang Z 

PROVIDER: S-EPMC11891995 | biostudies-literature | 2025 Mar

REPOSITORIES: biostudies-literature