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1. 发明专利

JP2011126828A Improved method for producing 1,3-disubstituted pyrrolidine compound or salt thereof 审中-公开
标题翻译：用于生产1,3-取代吡咯烷酮化合物或其盐的改进方法
公开(公告)号：JP2011126828A
公开(公告)日：2011-06-30
申请号：JP2009287837
申请日：2009-12-18
申请人： Kaneka Corp , 株式会社カネカ
发明人： YASUKOCHI HIROAKI , TAKEDA TOSHIHIRO
IPC分类号： C07D405/06 , A61K31/4025 , A61P13/02
摘要： PROBLEM TO BE SOLVED: To provide an industrially practicable method for efficiently producing a predetermined 1,3-disubstituted pyrrolidine compound and a salt thereof at high purity. SOLUTION: The production method comprises causing water to coexist in an organic solvent solution containing a free base of a 1,3-disubstituted pyrrolidine compound and subsequently adding a hydrohalic acid to cause crystallization. Thus, the high-purity 1,3-disubstituted pyrrolidine compound and salts thereof having been satisfactorily deprived of hardly removable impurities composed of specific analogues and discoloring components without purification by column chromatography are obtained. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：提供一种工业上可行的方法，用于有效地制备高纯度的预定的1,3-二取代的吡咯烷化合物及其盐。解决方案：制备方法包括使水在含有1,3-二取代吡咯烷化合物的游离碱的有机溶剂溶液中共存并随后加入氢卤酸以引起结晶。因此，可以得到高纯度1,3-二取代吡咯烷化合物及其盐，不需要通过柱色谱法纯化，令人满意地除去由特定类似物和变色组分组成的几乎不可除去的杂质。版权所有（C）2011，JPO＆INPIT

2. 发明专利

JP2011051896A Method for producing n-cyclopropyl-3-amino-2-hydroxyhexanoic acid amide hydrochloride 审中-公开
标题翻译：生产N-环丙基-3-氨基-2-羟基己酸酰胺盐酸盐的方法
公开(公告)号：JP2011051896A
公开(公告)日：2011-03-17
申请号：JP2007330190
申请日：2007-12-21
申请人： Kaneka Corp , 株式会社カネカ
发明人： KISHIMOTO SHIGEMI , KAMIKITA KEN , YASUKOCHI HIROAKI , TAKEDA TOSHIHIRO
IPC分类号： C07C231/24 , C07C237/04
CPC分类号： C07C237/04 , C07C231/22
摘要： PROBLEM TO BE SOLVED: To provide an industrially advantageous method for producing N-cyclopropyl-3-amino-2-hydroxyhexanoic acid amide hydrochloride, while controlling the crystal polymorphism thereof. SOLUTION: A crystal of N-cyclopropyl-3-amino-2-hydroxyhexanoic acid amide hydrochloride is subjected to a crystallization process that employs a specified organic solvent. Thereby, N-cyclopropyl-3-amino-2-hydroxyhexanoic acid amide hydrochloride with controlled crystal polymorphism can be produced. COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：待解决的问题：在控制其晶体多晶型的同时提供工业上有利的N-环丙基-3-氨基-2-羟基己酸酰胺盐酸盐的制备方法。解决方案：将N-环丙基-3-氨基-2-羟基己酸酰胺盐酸盐的晶体进行采用特定有机溶剂的结晶方法。由此，可以制备具有受控晶体多晶型物的N-环丙基-3-氨基-2-羟基己酸酰胺盐酸盐。版权所有（C）2011，JPO＆INPIT

3. 发明专利

JP2012041277A Improved method for producing 1, 3-disubstituted pyrrolidine compound or salt thereof 审中-公开
标题翻译：用于生产1,3-取代的吡咯烷酮化合物或其盐的改进方法
公开(公告)号：JP2012041277A
公开(公告)日：2012-03-01
申请号：JP2010181211
申请日：2010-08-13
申请人： Kaneka Corp , 株式会社カネカ
发明人： YASUKOCHI HIROAKI , TAKEDA TOSHIHIRO
IPC分类号： C07D405/06
摘要： PROBLEM TO BE SOLVED: To provide an industrially practicable method for efficiently producing a predetermined 1, 3-disubstituted pyrrolidine compound and a salt thereof with high purity.SOLUTION: The production method comprises making water to coexist in an organic solvent solution containing a free base of a 1, 3-disubstituted pyrrolidine compound and subsequently adding a hydrohalic acid to cause crystallization. Thereby, the high-purity 1, 3-disubstituted pyrrolidine compound and a salt thereof having been satisfactorily deprived of hardly removable impurities composed of specific analogues and coloring components without purification by column chromatography are obtained.
摘要翻译：要解决的问题：提供一种工业上可行的方法，用于有效地制备高纯度的预定的1,3-二取代的吡咯烷化合物及其盐。解决方案：制备方法包括使水共存于含有1,3-二取代吡咯烷化合物的游离碱的有机溶剂溶液中，随后加入氢卤酸以引起结晶。由此，可以得到高纯度1,3-二取代的吡咯烷化合物及其盐，不经柱色谱纯化而令人满意地除去由特定的类似物和着色成分组成的难以除去的杂质。版权所有（C）2012，JPO＆INPIT

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