title: O,N,N'-trialkylisoureas as mild activating reagents for N-acylsulfonamide anchors.
abstract: [chemical reaction: see text]. Prior to detachment of compounds synthesized on sulfonamide based safety-catch linkers, the molecular anchor has to be activated. This is achieved by alkylation of the nitrogen atom of the N-acylsulfonamide using different established protocols. As an addition to the existing repertoire of activating reagents, we suggest the use of O,N,N'-trialkylisoureas. Besides the demonstration of the feasibility of these mild alkylating agents for this purpose, custom-tailored novel O,N,N'-trialkylisoureas prepared from electron-deficient alcohols are reported.
authors.affiliation: Institut für Pharmazeutische Chemie, Philipps-Universität Marburg, Marbacher Weg 6, D-35032 Marburg, Germany.
authors.forename: Vida
authors.initials: V
authors.lastname: Zohrabi-Kalantari
authors.forename: Philipp
authors.initials: P
authors.lastname: Heidler
authors.forename: Tim
authors.initials: T
authors.lastname: Larsen
authors.forename: Andreas
authors.initials: A
authors.lastname: Link
mesh_terms: D000478:Alkylation; D002384:Catalysis; D007202:Indicators and Reagents; D015394:Molecular Structure; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry; D014508:Urea / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000737:chemistry
chemical_list: D007202:Indicators and Reagents; D013449:Sulfonamides; D014508:Urea