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    • 6. 发明授权
    • Process for the preparation of l-proline derivatives
    • 制备脯氨酸衍生物的方法
    • US5473081A
    • 1995-12-05
    • US181168
    • 1994-01-13
    • Yoshimasa KobayashiKaori TosaAkihiro SakimaeRyozo Numazawa
    • Yoshimasa KobayashiKaori TosaAkihiro SakimaeRyozo Numazawa
    • C07D207/16C07D207/12
    • C07D207/16
    • An L-proline derivative represented by: ##STR1## wherein R.sub.2 represents a lower alkyl group is prepared by reacting L-proline with a D-.alpha.-alkyl-.beta.-acylthiopropionic acid halide, ##STR2## wherein R.sub.1 represents an acyl group, X represents a halogen atom and R.sub.2 has the same meaning as defined above. The halide is added to an aqueous medium containing L-proline and a condensation agent for deacidification. The halide and L-proline are reacted while the reaction temperature and pH are maintained at 12.degree. C. or lower and within a range of 10.5-11.5, whereby a compound represented by: ##STR3## wherein R.sub.1 and R.sub.2 have the same meanings as defined above is obtained. The resulting compound is then subjected to deacylation under strong alkaline conditions without being isolated from the reaction mixture, thereby yielding the target L-proline derivative.
    • 由下式表示的L-脯氨酸衍生物:其中R2表示低级烷基,其通过L-脯氨酸与D-α-烷基-β-酰基硫代丙酰卤反应来制备,其中R1表示酰基,X 表示卤素原子,R2表示与上述相同的含义。 将卤化物加入到含有L-脯氨酸和用于脱酸的缩合剂的水性介质中。 使卤化物和L-脯氨酸反应,同时将反应温度和pH保持在12℃或更低并且在10.5-11.5的范围内,由此得到由下式表示的化合物:其中R1和R2具有相同的含义 获得上述定义。 然后将所得化合物在强碱性条件下进行脱酰基,而不从反应混合物中分离,从而得到目标L-脯氨酸衍生物。