| 摘要 |
Prepn. of N-formyl -L-alpha-aspartyl -L-phenylalanine (I) or its methyl ester (II) involves (1) preparing N-formulaspartic anhydride (III), and (2) reacting (III) with phenylalanine (IV), or its salt(s), phenylalanine methyl ester (VI) or its salt(s) (VII). (III) is prepd. by treating aspartic acid with about stoichiometric amt. of formic acid and acetic anhydride in presence (or absence) of metal oxide(s), hydroxide(s) or salt(s). (IV), (V), (VI) or (VII) is added to resulting matter without isolation of (III) to prepare (I) or (II). As partic acid is pref. treated with 0.9-1.1 mol-fold formic acid and 1.9-2.1 mol-fold acetic anhydride at 45-65 deg. C to prepare (III) acetic acid soln. In this process, metal salt(s), e.g. magnesium acetate, may be used as catalyst. One of (IV), (V), (VI) or (VII) is added to (III) acetic acid soln. at minus 10 to plus 60 deg. C to obtain (I) or (II). (I) or (II) is purified and lead to L-alpha-aspartyl -L-phenylalanine methyl ester by usual manner.
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