The enantioselective organocatalytic reduction of trifluoromethyl aryl and alkyl ketoimines afforded the corresponding fluorinated amines with high chemical and stereochemical efficiency. The Lewis base catalyzed reaction with trichlorosilane led to chiral products with a trifluoromethyl group directly linked to the newly generated stereocenter typically in >90% yield and up to 98% e.e.

The incorporation of the (trifluoromethyl)thio group into the benzo[e][1,2]thiazine 1,1-dioxide scaffold via a reaction of trifluoromethanesulfanylamide with 2-(2-alkynyl)benzenesulfonamide is reported. The transformation proceeds under mild conditions to afford the 4-((trifluoromethyl)thio)-2H-benzo[e][1,2]thiazine 1,1-dioxides in moderate to good yields.

Trifluoromethyl propargylamines react with various azide derivatives to afford 1,4-disubstituted 1,2,3-triazoles through a Huisgen 1,3-dipolar cycloaddition. The reaction is catalyzed by a Cu(I) species in acetonitrile, and the corresponding products are obtained in good yields. This process thus offers an entry to new trifluoromethyl peptidomimetics as interesting scaffolds.

An enantioselective organocatalytic alpha-trifluoromethylation of aldehydes has been accomplished using a commercially available, electrophilic trifluoromethyl source. The merging of Lewis acid and organocatalysis provides a new strategy for the enantioselective construction of trifluoromethyl stereogenicity, an important chiral synthon for pharmaceutical, materials, and agrochemical applicatio...

It has been demonstrated previously that several 3-trifluoromethyl-3-(4-alkoxyphenyl)diaziridines inhibit the 7-ethoxy-4-(trifluoroethyl)coumarin (7-EFC) O-deethylation activity of P450 2B6 in a mechanism-based manner. In contrast, 3-trifluoromethyl-3-(4-methylthio)phenyl)diaziridine did not have any effect on the activity of P450 2B6. It is interesting that both the alkoxy and the thiophenyl c...

Phosphonated derivatives of trifluoromethyl aziridine were obtained with good yield from aziridine-2-carbaldehyde by two distinct methods, which resulted in different diastereoselectivities. Using thiols as nucleophiles ring opening reactions of trifluoromethylated derivatives of aziridine-2-phosphonates proceeded regio- and diastereoselectively, giving rise to γ-amino-γ-trifluoromethyl phospho...

An efficient method for highly diastereoselective synthesis of quaternary α-trifluoromethyl α-amino acids was developed via indium mediated allylation of (R)-phenylglycinol methyl ether based imines of trifluoropyruvate in good yields with high diastereoselectivities at room temperature; to illustrate the application of this method in organic synthesis, 2-allyl-2-(trifluoromethyl) aziridine was...

4-methylaniline in chlorobenzene reacted with sulphuric acid, sodium thiocyanate and sulfuryl chloride to give 2-amino-6-methyl benzothiazole. This 2-amino-6methyl benzothiazole was later further reacted with 2-(2,2difluoroethoxy)-6-(trifluoromethyl)benzene-1-sulfonyl chloride in the presence of Dichloromethane and anhydrous Pyridine to afford 2-(2,2-difluoroethoxy)-N-(6methylbenzo[d]thiazole-2...