title: Synthesis of optically active alpha-aminoalkyl alpha'-halomethyl ketone: a cross-Claisen condensation approach.
abstract: A simple and versatile method was developed for the synthesis of alpha-aminoalkyl alpha'-halomethyl ketone derivatives, which are useful intermediates of protease inhibitors. It involves selective halogenation of the alpha-position on a beta-ketoester, which is prepared by cross-Claisen condensation using N-protected amino acid ester. The title compound is obtained in high yield after decarboxylation of the alpha-halo-beta-ketoester.
authors.affiliation: AminoScience Laboratories, Ajinomoto Co. Inc., Suzuki-cho, Kawasaki-ku, Kawasaki-shi 210-8681, Japan.
authors.forename: Yutaka
authors.initials: Y
authors.lastname: Honda
authors.forename: Satoshi
authors.initials: S
authors.lastname: Katayama
authors.forename: Mitsuhiko
authors.initials: M
authors.lastname: Kojima
authors.forename: Takayuki
authors.initials: T
authors.lastname: Suzuki
authors.forename: Kunisuke
authors.initials: K
authors.lastname: Izawa