Hovione Inter Limited

Emilia Perpetua Tavares Leitao

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.

Method for monofluoromethylation of organic substrates to prepare biologically active organic compounds

The invention provides a compound of formula A, B, C or D, methods for making them, intermediates therefor, and their use in making organic biologically active compounds: Wherein: Wherein: Wherein: 

Electrophilic reagents for monohalomethylation, their preparation and their uses

The invention provides electrophilic monohalomethylating reagents, methods for their preparation and methods for preparation of monohalomethylated biologically active compounds using such reagents. Typical monohalomethyl groups transferred are FH2C&#x2014;, CIH2C&#x2014; and others. The reagents used for transferal of the groups are described by Formulae A-D: wherein: X=F, Cl, Br, I, sulfonate esters, phosphate esters or another leaving group; R11=tetrafluoroborates, inflates, halogen, perchlorate, sulfates, phosphates or carbonates The other variables are as defined in the claims. 

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Sao Marcos, Portugal

Emilia Perpetua Tavares Leitao