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US 9,540,413 B2Granted
Method for monofluoromethylation of organic substrates to prepare biologically active organic compounds
AssigneeHovione Inter Ltd.
InventorEmilia Perpetua Tavares Leitao
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Abstract
Described herein is a process for the preparation of monofluoromethylated organic biologically active compounds using monofluoromethylated reagents. Fluticasone Propionate and Fluticasone Furoate can be prepared using, for example, S-monofluoromethyl-S-phenyl-2,3,4,5-tetramethylphenylsulfonium tetrafluoroborate as monofluoromethylating reagent instead of bromofluoromethane.
Claims12
A method of preparing a pharmaceutically active compound containing a “CH2F” moiety on a sulphur atom, which method comprises the use of a monofluoromethylating reagent characterized by formula I:
- wherein:
- R4 is an anion suitable to form a salt of the reagent presented above, selected from the group consisting of tetrafluoroborate, triflate and halogen;
- by reacting with a compound of formula A:
- wherein R is selected from the group consisting of hydroxyl, furoate and propionate;
- wherein the pharmaceutically active is a compound of Formula IV:
- wherein R is selected from the group consisting of hydroxyl, furoate and propionate.
3 more elements
Dependencies are inferred from the claim text.