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1. 发明申请

WO2009011551A2 PROCESS FOR THE EFFICIENT PREPARATION OF 3-HYDROXY PYRROLIDINE AND DERIVATIVES THEREOF 审中-公开
标题翻译：有效制备3-羟基吡咯烷酮及其衍生物的方法
公开(公告)号：WO2009011551A2
公开(公告)日：2009-01-22
申请号：PCT/KR2008/004193
申请日：2008-07-17
申请人： RSTECH CORPORATION , QUAN, Long Guo , LEE, Jae Kwan , HONG, Mei Hua , KIM, Kwang Sub , PARK, Kwang Sik
发明人： QUAN, Long Guo , LEE, Jae Kwan , HONG, Mei Hua , KIM, Kwang Sub , PARK, Kwang Sik
IPC分类号： C07D207/12
CPC分类号： C07D207/12
摘要： The present invention relates to an effective process for the preparation of 3-hydroxypyrrolidine or derivatives thereof. The process comprises (a) protecting a hydroxyl group of 4-halo-3-hydroxybutyric acid, (b) reducing an ester group of the compound obtained from the step (a) to obtain a corresponding alcohol compound, (c) reacting the compound obtained from the step (b) with sulfonyl halide to produce a corresponding sulfonate compound, (d) reacting the compound obtained from the step (c) with an amine to obtain 3-hydroxy-protected pyrrolidine compound, and (e) deprotecting the compound obtained from the step (d) to produce the targeted 3-hydroxypyrrolidine or derivatives thereof. The process provides 3-hydroxypyrrolidine or derivatives thereof with high optical purity, because optical purity of the starting material is substantially retained. In the process, each of the steps is carried out in a mild condition and does not require any special purification. This means that the process is useful and adequate for industrial mass production of 3-hydroxypyrrolidine and derivatives thereof having high optical purity.
摘要翻译：本发明涉及一种制备3-羟基吡咯烷或其衍生物的有效方法。该方法包括（a）保护4-卤-3-羟基丁酸的羟基，（b）还原由步骤（a）获得的化合物的酯基，得到相应的醇化合物，（c）使化合物（b）由磺酰卤获得以产生相应的磺酸盐化合物，（d）使由步骤（c）获得的化合物与胺反应，得到3-羟基保护的吡咯烷化合物，和（e）使化合物（d）得到目标3-羟基吡咯烷或其衍生物。该方法提供具有高光学纯度的3-羟基吡咯烷酮或其衍生物，因为起始原料的光学纯度基本保持不变。在该过程中，每个步骤在温和条件下进行，并且不需要任何特殊的纯化。这意味着该方法对于具有高光学纯度的3-羟基吡咯烷及其衍生物的工业批量生产是有用和充分的。

2. 发明申请

WO2008093955A1 PROCESS FOR THE EFFICIENT PREPARATION OF 3-HYDROXYTETRAHYDROFURAN 审中-公开
标题翻译：高效制备3-羟基喹唑啉的方法
公开(公告)号：WO2008093955A1
公开(公告)日：2008-08-07
申请号：PCT/KR2008/000395
申请日：2008-01-22
申请人： RSTECH CORPORATION , QUAN, Long Guo , BOO, Chang Jin , HONG, Mei Hua , LEE, Jae Kwan , LEE, Jong Min , KIM, Seong-Jin
发明人： QUAN, Long Guo , BOO, Chang Jin , HONG, Mei Hua , LEE, Jae Kwan , LEE, Jong Min , KIM, Seong-Jin
IPC分类号： C07D307/20 , C07C29/147 , C07C31/42
CPC分类号： C07D307/20 , C07B2200/07 , C07C29/147 , C07C31/42
摘要： Disclosed is a process for the efficient preparation of 3-hydroxytetrahydrofuran. In particular, the present invention provides a process for the preparation of 3-hydroxytetrahydrofuran by performing cyclization of 4-halo-1,3-butanediol either neat or in an organic solvent by heating to 75°C to 18O°C. In the present invention, acidic solution is not used in the cyclization and, thus, the reaction environment is improved. Further, the cyclization product 3-hydroxytetrahydrofuran is purified by a simple process. In addition, according to the present invention, chirality of the starting material is substantially maintained. Consequently, chiral 3-hydroxytetrahydrofuran with a high optical purity of 99.0% ee or better can be prepared economically, in high yield.
摘要翻译：公开了一种有效制备3-羟基四氢呋喃的方法。特别地，本发明提供了一种通过加热至75℃至180℃，通过纯的或在有机溶剂中环化4-卤代-1,3-丁二醇来制备3-羟基四氢呋喃的方法。在本发明中，在环化中不使用酸性溶液，因此反应环境得到改善。此外，环化产物3-羟基四氢呋喃通过简单的方法纯化。此外，根据本发明，基本保持原料的手性。因此，可以高效率地制备光学纯度高达99.0％ee以上的手性3-羟基四氢呋喃。

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