2-Fluoro-1,3-benzodithiole-1,1,3,3-tetraoxide: A Reagent for Nucleophilic Monofluoromethylation of Aldehydes

摘要

In recent years, fluorine-containing organic molecules have been identified as strong candidates for pharmaceuticals and advanced materials because of their unique properties, despite their extremely rare natural occurrence. Particularly, monofluorinated analogues of biologically active compounds are a peerless class of drug nominees, which are considered to be promising bioisosteres of the parent molecules. In this respect, compounds with monofluoro-methyl groups are particularly valuable because they can mimic the methyl or hydroxymethyl group, which are often encountered in biologically active materials. The fluoro-methyl group is best known as an effective functional group for the "Trojan horse" inhibition of vitamin B6 dependent enzymes.