| 摘要 |
PURPOSE: A process for preparing alpha-amino acids, derivatives thereof including phenylalanine and homophenylalanine and intermediates thereof are provided to maintain the stereochemistry of an optically pure aziridine used as starting material. CONSTITUTION: The process for preparing a compound having formula(7) comprises the steps of: reducing (2R)-or (2S)-£N-R3|aziridine-2-carboxylic acid ester of formula(5) to produce aldehyde of formula(6); and adding aryl alkali metal (ArM+) or aryl alkali earth metal (ArM++) thereto, wherein R3 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, phenyl, 4-chlorophenyl, 4-methoxyphenyl, 3-triazinyl or pyridinyl acyl, benzyl, hydrocarbon residue which may be substituted by a substituent selected from the group consisting of hydroxy, alkoxy, dialkylamino, phenyl, 4-chlorophenyl and 4-methoxyphenyl, 2,4-dimethoxyphenyl, substituted phenyl including (1R)-phenylethyl or (1S)-phenylethyl; Ar is phenyl, 4-methoxyphenyl, 2,4-dimethoxyphenyl, 4-chlorophenyl, 2,4-dichlorophenyl, 2-fluorophenyl, 4-fluorophenyl, 2,3,4,5,6-pentafluorophenyl, 4-cyanophenyl, 2-cyanophenyl, 1-naphthyl or 2-naphthyl; R4 is methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, isopentyl, neopentyl, n-hexyl, n-heptyl, isoheptyl, n-octyl or isooctyl; M+ is alkali metal; and M++ is alkali earth metal.
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