title: Synthesis of novel angular spirocyclic azetidines.
abstract: The syntheses of a variety of novel angular azaspiro[3.3]heptanes are reported. gem-Difluoro and gem-dimethyl variants of the angular 1,6-diazaspiro[3.3]heptane module were prepared in high yields using efficient sequences. Additionally, a practical one-pot synthesis of 5-oxo-2-azaspiro[3.3]heptanes and subsequent conversions into functionalized derivatives are described. The methods reported are amenable to the synthesis of these building blocks for drug discovery as members of a library or individually on a preparative scale.
authors.affiliation: Laboratorium für Organische Chemie, ETH Zürich, CH-8093 Zürich, Switzerland.
authors.forename: Carine
authors.initials: C
authors.lastname: Guérot
authors.forename: Boris H
authors.initials: BH
authors.lastname: Tchitchanov
authors.forename: Henner
authors.initials: H
authors.lastname: Knust
authors.forename: Erick M
authors.initials: EM
authors.lastname: Carreira
mesh_terms: D001384:Azetidines / Q000138:chemical synthesis* / Q000737:chemistry; D006536:Heptanes / Q000138:chemical synthesis* / Q000737:chemistry; D015394:Molecular Structure; D013141:Spiro Compounds / Q000138:chemical synthesis* / Q000737:chemistry*; D013237:Stereoisomerism
chemical_list: D001384:Azetidines; D006536:Heptanes; D013141:Spiro Compounds