Process for the preparation of estetrol
AssigneeCrystal Pharma, S.A.U.
InventorsJuan José Ferreiro Gil, Jesús Miguel Iglesias Retuerto, Francisco Javier Gallo Nieto
Life of this patent
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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.
Claims16
A compound of formula (IV)
- or a salt or solvate thereof, wherein
- R1O is a protected hydroxyl group selected from the group consisting of a silyl ether, an ether, an ester, a carbamate and a carbonate,
- R2O is a protected hydroxyl group which is an ether,
- with the proviso that the ether in R2O does not include silyl ether;
- with the proviso that if R1O is a methyl ether, then R2O is neither a 2-propynyl ether nor a 2- tetrahydropyranyl ether.
A process for the preparation of Estetrol or a salt or solvate thereof, the process comprising:
- a) reacting a compound of formula (IV)
- or a salt or solvate thereof, wherein
- R1O at position C3 is a protected hydroxyl group selected from the group consisting of a silyl ether, an ether, an ester, a carbamate and a carbonate,
- R2O at position C17 is a protected hydroxyl group which is an ether,
- with the proviso that the ether in R2O does not include silyl ether;
- with an oxidizing agent selected from OsO4or 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.
Dependencies are inferred from the claim text.