title: Branching cascades provide access to two amino-oxazoline compound libraries.
abstract: An efficient synthetic access to two amino-oxazoline compound libraries was developed employing the branching cascades approach. A common precursor, that is, chromonylidene β-ketoester was transformed into two different ring-systems, that is, the pyridine and the benzopyrane substituted hydroxyphenones. In further two steps, the ketone moiety in two ring-systems was transformed into an amino-oxazoline ring. The functional groups on the two amino-oxazoline scaffolds were exploited further to generate, a compound collection of ca. 600 amino-oxazolines which are being exposed to various biological screenings within the European Lead Factory consortium.
authors.affiliation: Max-Planck-Institut für molekulare Physiologie, Otto-Hahn-Strasse 11, 44227 Dortmund, Germany.
authors.forename: Annamalai
authors.initials: A
authors.lastname: Murali
authors.affiliation: Medicinal Chemistry, Taros Chemicals GmbH & Co. KG, Emil-Figge-Str. 76a, 44227 Dortmund, Germany.
authors.forename: Federico
authors.initials: F
authors.lastname: Medda
authors.affiliation: Medicinal Chemistry, Taros Chemicals GmbH & Co. KG, Emil-Figge-Str. 76a, 44227 Dortmund, Germany.
authors.forename: Matthias
authors.initials: M
authors.lastname: Winkler
authors.affiliation: Medicinal Chemistry, Taros Chemicals GmbH & Co. KG, Emil-Figge-Str. 76a, 44227 Dortmund, Germany.
authors.forename: Fabrizio
authors.initials: F
authors.lastname: Giordanetto
authors.affiliation: Max-Planck-Institut für molekulare Physiologie, Otto-Hahn-Strasse 11, 44227 Dortmund, Germany. Electronic address: kamal.kumar@mpi-dortmund.mpg.de.
authors.forename: Kamal
authors.initials: K
authors.lastname: Kumar
mesh_terms: D055808:Drug Discovery; D057166:High-Throughput Screening Assays; D015394:Molecular Structure; D010080:Oxazoles / Q000737:chemistry*; D054852:Small Molecule Libraries / Q000138:chemical synthesis*
chemical_list: D010080:Oxazoles; D054852:Small Molecule Libraries
keywords: Amino-oxazolines; Branching cascades; Compound libraries; Dipolar cycloadditions; Heterocycles