Process for the production of estetrol intermediates
EP4771029A1Pending Publication Date: 2026-07-08ESTETRA SRL
Patent Information
- Authority / Receiving Office
- EP · EP
- Patent Type
- Applications
- Current Assignee / Owner
- ESTETRA SRL
- Filing Date
- 2024-08-30
- Publication Date
- 2026-07-08
AI Technical Summary
Technical Problem
Existing processes for synthesizing estetrol intermediates face challenges such as the need for protecting the 3-OH function with benzyl groups, which are difficult to remove, and the generation of impurities that complicate industrial-scale production.
Method used
A new process involving the sulfinylation of a specific compound followed by protection, using optimized reaction conditions and solvents, to produce 3-protected-oxy-estra-1,3,5(10),15-tetraene-17-ol with improved yield and purity.
Benefits of technology
The new process achieves high yield and purity of the estetrol intermediate, reduces solvent usage and reaction time, and minimizes environmental impact, making it more suitable for industrial production.
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Smart Images
Figure EP2024074283_06032025_PF_FP_ABST
Abstract
The present invention relates to a process for the preparation of a compound of formula (I), a stereoisomer, a salt, a hydrate or a solvate thereof, (II) comprising the step of sulfinylation of a compound of formula (IV) to produce compound of formula (II); (IV) wherein: R1 and R2 are as defined in the claims, wherein said sulfinylation step is performed in the presence of a solvent selected from the group comprising benzene, toluene, ethylbenzene, xylene, chlorobenzene, bromobenzene, fluorobenzene, anisole, nitrobenzene, tetralin, dichlorobenzene, trimethylbenzene, ethylacetate, propylacetate, butylacetate, propanol, butanol, 2- methyltetrahydrofuran, diethylether, methyltertbutylether, cyclopentyl methyl ether, dichloromethane, tetrachloromethane, pentane, hexane, heptane, cyclohexane, decaline and mixtures thereof.
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