title: Instant ligand libraries. Parallel synthesis of monodentate phosphoramidites and in situ screening in asymmetric hydrogenation.
abstract: Chiral phosphoramidites have been identified as excellent ligands for various metal-catalyzed enantioselective transformations. Taking advantage of their easy preparation and modular nature, we designed a fully automated protocol for the parallel preparation of a library of 32 phosphoramidites and its screening in asymmetric hydrogenation of amino acid precursors. This initial study led to the discovery of a new ligand for the preparation of an enantiopure beta(3)-homoalanine precursor. [structure--see text]
authors.affiliation: DSM Pharma Chemicals-Advanced Synthesis, Catalysis and Development, P.O. Box 18, 6160 MD Geleen, The Netherlands.
authors.forename: Laurent
authors.initials: L
authors.lastname: Lefort
authors.forename: Jeroen A F
authors.initials: JA
authors.lastname: Boogers
authors.forename: André H M
authors.initials: AH
authors.lastname: de Vries
authors.forename: Johannes G
authors.initials: JG
authors.lastname: de Vries
mesh_terms: D000577:Amides / Q000138:chemical synthesis* / Q000737:chemistry; D000588:Amines / Q000737:chemistry; D000596:Amino Acids / Q000737:chemistry*; D002384:Catalysis; D006865:Hydrogenation; D008024:Ligands; D015394:Molecular Structure; D010756:Phosphoric Acids / Q000138:chemical synthesis* / Q000737:chemistry; D013237:Stereoisomerism
chemical_list: D000577:Amides; D000588:Amines; D000596:Amino Acids; D008024:Ligands; D010756:Phosphoric Acids; C011067:phosphoramidic acid