1082208-85-2

Upstream product

• 358-23-6 trifluoromethylsulfonic anhydride 
• 69385-30-4 2,6-difluorobenzylamine 
• 1159505-61-9 C₈H₇F₄NO₂S 
• 36457-58-6 N-benzyl-1,1,1-trifluoromethanesulfonamide 
• 100-46-9 benzylamine 

Relevant academic research and scientific papers

PALLADIUM-CATALYZED ORTHO-FLUORINATION

A new method of ortho-fluorination where an aryl C—H bond is directly replaced by an aryl C-F bond in a palladium-catalyzed reaction is provided. The method includes the ortho-fluorination of a triflamide protected benzylamine, a palladium catalyst, such as Pd(OTf)2, a fluorinating reagent such as N-fluoro-2,4,6-trimethylpyridinium triflate, and a ligand to promote the reaction such as N-methylpyrrolidinone (NMP).

Versatile Pd(OTf)2·2H2O-catalyzed ortho-fluorination using NMP as a promoter

(Chemical Equation Presented) Pd(OTf)2·2H 2O-catalyzed ortho-fluorination of triflamide-protected benzylamines is reported. The use of N-fluoro-2,4,6-trimethylpyridinium triflate as the F+ source and NMP as a promoter is crucial for this reaction. The conversion of triflamide into a wide range of synthetically useful functional groups makes this fluorination protocol broadly applicable in medicinal chemistry and synthesis.

Convenient synthesis of primary sulfonamides

An efficient protocol for a one-pot synthesis of mono-sulfonamides has been developed. It features utilization of excess of sulfonylating agent followed by base mediated recovery of the primary sulfonamide.