TFA-sensitive arylsulfonylthiourea-assisted synthesis of N,N′-substituted guanidines

Article abstract of DOI:10.1021/jo026807m

An efficient synthesis of N,N′-substituted guanidine derivatives was developed via an aromatic sulfonyl-activated thiourea intermediate. The use of certain aromatic sulfonamides, such as PbfNH₂, as the key reagent to incorporate a TFA-labile guanidine protection group greatly facilitates solid-phase synthesis of N,N′-substituted guanidine compounds.