title: Automated synthesis of a 184-member library of thiadiazepan-1,1-dioxide-4-ones.
abstract: The construction of a 225-member (3 × 5 × 15) library of thiadiazepan-1,1-dioxide-4-ones was performed on a Chemspeed Accelerator (SLT-100) automated parallel synthesis platform, culminating in the successful preparation of 184/225 sultams. Three sultam core scaffolds were prepared based upon the utilization of an aza-Michael reaction on a multifunctional vinyl sulfonamide linchpin. The library exploits peripheral diversity in the form of a sequential, two-step [3 + 2] Huisgen cycloaddition/Pd-catalyzed Suzuki-Miyaura coupling sequence.
authors.affiliation: Center for Chemical Methodologies and Library Development at the University of Kansas, Delbert M. Shankel Structural Biology Center, Lawrence, Kansas 66047, United States.
authors.forename: Erik
authors.initials: E
authors.lastname: Fenster
authors.forename: Toby R
authors.initials: TR
authors.lastname: Long
authors.forename: Qin
authors.initials: Q
authors.lastname: Zang
authors.forename: David
authors.initials: D
authors.lastname: Hill
authors.forename: Benjamin
authors.initials: B
authors.lastname: Neuenswander
authors.forename: Gerald H
authors.initials: GH
authors.lastname: Lushington
authors.forename: Aihua
authors.initials: A
authors.lastname: Zhou
authors.forename: Conrad
authors.initials: C
authors.lastname: Santini
authors.forename: Paul R
authors.initials: PR
authors.lastname: Hanson
mesh_terms: D001381:Azepines / Q000737:chemistry*; D020650:Combinatorial Chemistry Techniques
chemical_list: D001381:Azepines