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发明公开
CN103596924A 光学活性的α-取代的脯氨酸的制造方法 无效 - 撤回

光学活性的α-取代的脯氨酸的制造方法
摘要：
本发明目的是提供实际中适用于在温和条件下通过少量步骤由无环酮化合物制造光学活性的α-取代的脯氨酸的工业方法。本发明涉及光学活性的α-取代的脯氨酸(4)和/或光学活性的α-取代的脯氨酰胺(5)的制造方法，所述方法包括：(a)使无环酮化合物(1)与选自氨、铵盐、伯胺和伯胺盐的至少一种物质以及氰化剂反应得到环状含氮化合物(2)，(b)将环状含氮化合物(2)水合得到α-取代的脯氨酰胺(3)，和(c)解析α-取代的脯氨酰胺(3)，所述解析通过(d)酶促水解、(e)通过非对映体盐形成进行解析和(f)通过柱色谱分离中的一种或多种进行。
摘要（英）：

The present invention provides a practically suitable industrial method for producing an optically active alpha-substituted proline from a chain ketone compound by a short process under mild conditions. The present invention relates to a method for producing an optically active alpha-substituted proline (4) and/or an optically active alpha-substituted proline amide (5), which comprises: (a) a step for obtaining a cyclic nitrogen-containing compound (2) by reacting a chain ketone compound (1) with a cyanating agent and at least one substance selected from among ammonia, ammonium salts, primary amines and salts of primary amines; (b) a step for obtaining an a-substituted proline amide (3) by hydrating the cyclic nitrogen-containing compound (2); and (c) a step for optically resolving the alpha-substituted proline amide (3) by (d) enzymatic hydrolysis, (e) resolution by means of the formation of a diastereomeric salt and/or (f) separation by means of column chromatography.

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