title: Synthesis of 1,4,5 trisubstituted γ-lactams via a 3-component cascade reaction.
abstract: A three component one-pot cascade reaction was developed for the synthesis of 1,4,5-trisubstituted γ-lactams. The resulting scaffold can be modified independently at three positions, two of which are conveniently accessed by changing the components of the one-pot reaction. The phases of building block generation, scaffold synthesis and subsequent appendage modification were adapted to library production, which resulted in a screening library of 500 compounds.
authors: Department of Chemistry, Technical University of Denmark, Kemitorvet 207, DK-2800 Kgs. Lyngby, Denmark.
authors: Michael Åxman
authors: MÅ
authors: Petersen
authors: Department of Chemistry, Technical University of Denmark, Kemitorvet 207, DK-2800 Kgs. Lyngby, Denmark.
authors: Michael A
authors: MA
authors: Mortensen
authors: Department of Chemistry, Technical University of Denmark, Kemitorvet 207, DK-2800 Kgs. Lyngby, Denmark.
authors: A Emil
authors: AE
authors: Cohrt
authors: Department of Chemistry, Technical University of Denmark, Kemitorvet 207, DK-2800 Kgs. Lyngby, Denmark.
authors: Rico
authors: R
authors: Petersen
authors: Department of Chemistry, Technical University of Denmark, Kemitorvet 207, DK-2800 Kgs. Lyngby, Denmark.
authors: Peng
authors: P
authors: Wu
authors: EDELRIS, 115 Avenue Lacassagne, F-69003, France.
authors: Nicolas
authors: N
authors: Fleury-Brégeot
authors: EDELRIS, 115 Avenue Lacassagne, F-69003, France.
authors: Rémy
authors: R
authors: Morgentin
authors: EDELRIS, 115 Avenue Lacassagne, F-69003, France.
authors: Claude
authors: C
authors: Lardy
authors: Department of Chemistry, Technical University of Denmark, Kemitorvet 207, DK-2800 Kgs. Lyngby, Denmark; Singapore Centre on Environmental Life Sciences Engineering, Nanyang Technological University, Singapore 637551, Singapore. Electronic address: ten@kemi.dtu.dk.
authors: Thomas E
authors: TE
authors: Nielsen
authors: Department of Chemistry, Technical University of Denmark, Kemitorvet 207, DK-2800 Kgs. Lyngby, Denmark; Center for Nanomedicine and Theranostics, Technical University of Denmark, DK-2800 Kgs. Lyngby, Denmark. Electronic address: mhc@kemi.dtu.dk.
authors: Mads H
authors: MH
authors: Clausen
mesh_terms: D002384:Catalysis; D020650:Combinatorial Chemistry Techniques / Q000379:methods; D055808:Drug Discovery; D007769:Lactams / Q000138:chemical synthesis*; D015394:Molecular Structure; D054852:Small Molecule Libraries / Q000138:chemical synthesis*; D013237:Stereoisomerism
chemical_list: D007769:Lactams; D054852:Small Molecule Libraries
keywords: Cascade reaction; Library production; Molecular diversity; One-pot reaction; γ-Lactams