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Patent / 2016

Electrophilic reagents for monohalomethylation, their preparation and their uses

  • Emilia Leitao
US 9290446

The invention provides electrophilic monohalomethylating reagents, methods for their prepn. and methods for prepn. of monohalomethylated biol. active compds. using such reagents. Typical monohalomethyl groups transferred are FH2C-, CIH2C- and others. The reagents used for transferal of the groups are described by Formulas 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.