Review of 'Direct Nucleophilic Difluoromethylation of Aromatic Isoxazoles Activated by Electron-Withdrawing Groups Using (Difluoromethyl)trimethylsilane'

The development of new fluorination methodologies is extremely important, especially for the synthesis of drugs and many biologically active compounds bearing fluorinated moiety. In this article the authors developed a new efficient approach for the regio- and diastereoselective nucleophilic difluoromethylation of aromatic isoxazoles using TMSCF2H as a fluorinated reagent. The presence of EWGs at 4-position of aromatic isoxazoles such as nitro, triflyl and phenylsulfonyl was found as a crucial point to get moderate yielding of the corresponding products. This work is a well extension of their previous development, nevertheless the new important challenging task of introducing CF2H group was successfully realized. Additionally the nitro group can be easily cleaved, which makes this approach even more attractive. Based on that I recommend to publish this article in ScienceOpen.