Electrophilic reagents for monohalomethylation, their preparation and their uses

摘要

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—, CIH2C— 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.;

主权项

1. A compound of formula A wherein X represents F; R1-R5, R6, R9 and R10 represent H; R7 and R8 represent alkyl; and R11 represents tetrafluoroborate.