| 摘要 |
PURPOSE: An intermediate of an optically active diarylalanine and derivatives thereof and a process for preparing the same are provided, thereby requiring no protection of serine by using aziridine-2-carboxylic acid ester and (L)-diphenylalanine as well as (D)-diphenylalanine by stereo-specifically selecting aziridine-2-carboxylic acid ester. CONSTITUTION: The intermediate of an optically active diarylalanine and derivatives thereof represented by formula (2) are provided, wherein Ar is phenyl, phenyl substituted with 1 to 3 substituents selected from C1-C8 alkyl, halogen such as F, Cl and I, C1-C8 alkoxy, C1-C8 thioalkoxy, NO2, OH and CF3, naphthalene, N, O or S containing C1-C14 hetero aromatic ring compounds; R1 is hydrogen, C1-C8 alkyl, C1-C8 cycloalkyl, phenyl, 4-chlorophenyl, 4-methoxyphenyl, s-triazinyl or pyridinyl acyl, benzyl, C1-C8 carbohydrate residue substituted with hydroxy, alkoxy, dialkylamino, phenyl, 4-chlorophenyl or 4-methoxyphenyl, 2,4-methoxyphenyl, or (R)-phenylethyl, or (S)-phenylethyl. The method for preparing the intermediate of an optically active diarylalanine and derivatives thereof of formula (2) comprises reacting aziridine-2-carboxylic acid ester of formula (1) with arylmagnesium halide, wherein the halide X of arylmagnesium halide is Cl or Br; the arylmagnesium halide is phenylmagnesium chloride or phenylmagnesium bromide; and R2 is C1-C10 alkyl.
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