Process for the preparation of estetrol

US9988417B2 · kind B2 · utility

Assignee

• CRYSTAL PHARMA, S.A.U. · ES

Inventors

• Juan José Ferreiro Gil · Laguna de Duero, ES
• Jesús Miguel Iglesias Retuerto · Laguna de Duero, ES
• Francisco Javier Gallo Nieto · Laguna de Duero, ES

Key dates

• Filing date: Sep 17, 2014
• Grant date: Jun 5, 2018
• Expiry date: Sep 17, 2034

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02P20/55
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The invention relates to a process for obtaining Estetrol or a salt or solvate thereof, the process comprising: a) reacting a compound of formula (IV) or a salt or solvate thereof, wherein R1 is a hydroxyl protecting group selected from a silyl ether, an ether, an ester, a carbamate and a carbonate, and R2 is a hydroxyl protecting group selected from an ether, with an oxidizing agent selected from OsO4 or a source of osmium tetroxide to produce Estetrol or a compound of formula (II) or a salt or solvate thereof wherein R1 is as defined previously; and b) if a compound of formula (II) is obtained in step a), deprotecting said compound to produce Estetrol.