Electrophilic reagents for monohalomethylation, their preparation and their uses
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United States of America Patent
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Mar 22, 2016
Grant Date -
Oct 17, 2013
app pub date -
Oct 27, 2011
filing date -
Oct 27, 2010
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Abstract
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.
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