title: Versatile solid-phase synthesis of s-arylisothioureas.
abstract: Resin-bound amines 4a-m condense with di(benzotriazol-1-yl)methanimine 6 to give 1H-benzotriazole-1-carboximidamide resins 7a-m, which subsequently react with thiols 9a'-g' followed by cleavage affording nonprotected isothioureas 1aa'-mg' in high yields and with good purities. Analogous reactions with secondary amines activated with EtMgBr lead to guanidines 2a,b,e-g in moderate yields. Resin-bound isothioureas 1 are converted by acyl chlorides or carboxylic acids into acyl derivatives 12a-n in high yields and with good purities.
authors.affiliation: Center for Heterocyclic Compounds, Department of Chemistry, University of Florida, Gainesville, Florida 32611-7200, USA. katrizky@chem.ufl.edu
authors.forename: Alan R
authors.initials: AR
authors.lastname: Katritzky
authors.forename: Boris V
authors.initials: BV
authors.lastname: Rogovoy
authors.forename: Vladimir
authors.initials: V
authors.lastname: Vvedensky
authors.forename: Katherine
authors.initials: K
authors.lastname: Kovalenko
authors.forename: Behrouz
authors.initials: B
authors.lastname: Forood