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1.发明申请公开(公告)号：US20090326246A1
公开(公告)日：2009-12-31
申请号：US12375141
申请日：2007-07-23
IPC分类号： C07D207/04
CPC分类号： C07D207/14 , C07D207/10 , C07D207/12 , C07D207/27
摘要： Aiming at production of an optically active 3-amino nitrogen-containing compound which is useful as an intermediate in synthesis of medicines and pesticides, in particular, an optically active 1-protected-3-aminopyrrolidine derivative, from an inexpensive and readily available raw material by a process which is efficient and can be practiced industrially, an optically active 3-amino nitrogen-containing compound is produced by performing a reaction of an optically active 3-substituted nitrogen-containing compound with ammonia, methylamine, ethylamine or dimethylamine in the presence of water. In addition, a 1-protected-3-aminopyrrolidine derivative is produced by performing a reaction of an optically active 1-protected-3-(sulfonyloxy)pyrrolidine derivative with ammonia, methylamine, ethylamine, or dimethylamine in the presence of methanol, ethanol, n-propanol, or isopropanol under a pressure of less than 30 barr.
摘要翻译： 本发明涉及一种光学活性3-氨基含氮化合物的制备，其可用作药物和农药合成中的中间体，特别是光学活性的1-保护的3-氨基吡咯烷衍生物，由廉价且容易获得的原料 通过工业上有效且可以在工业上实践的方法，通过在存在下进行光学活性的3-取代的含氮化合物与氨，甲胺，乙胺或二甲胺的反应来制备光学活性的3-氨基含氮化合物 的水。 此外，通过在甲醇，乙醇，甲醇，乙醇等的存在下进行光学活性的1-保护的3-（磺酰氧基）吡咯烷衍生物与氨，甲胺，乙胺或二甲胺的反应来制备1-保护的3-氨基吡咯烷衍生物， 正丙醇或异丙醇，压力小于30巴。
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公开(公告)号：US08273883B2
公开(公告)日：2012-09-25
申请号：US12449460
申请日：2008-02-05
IPC分类号： C07D241/04 , C07D295/00
CPC分类号： C07B53/00 , C07D241/04
摘要： The objective of the present invention is to produce an optically active 2-arylpiperazine derivative useful as a synthetic intermediate for pharmaceutical products and agricultural chemicals from inexpensive and readily available starting material by an industrially practicable method. The objective can be accomplished by treating an optically active substituted aminodiol derivative produced from an optically active styrene oxide derivative with a sulfonating agent in the presence of a base, and then reacting an amine compound to obtain the 2-arylpiperazine derivative. Especially, an optically active 1-unsubstituted-2-arylpiperazine derivative can be produced by treating an optically active 1-allyl-2-arylpiperazine derivative with water in the presence of a transition metal catalyst for deallylation.
摘要翻译： 本发明的目的是通过工业上可行的方法从便宜且容易获得的原料制备用作药物产品和农药的合成中间体的光学活性2-芳基哌嗪衍生物。 该目的可以通过在碱的存在下用磺化剂处理由光学活性苯乙烯氧化物衍生物产生的光学活性取代的氨基二醇衍生物，然后使胺化合物反应得到2-芳基哌嗪衍生物来实现。 特别地，光学活性的1-未取代-2-芳基哌嗪衍生物可以通过在过渡金属催化剂的存在下用水处理光学活性的1-烯丙基-2-芳基哌嗪衍生物来进行脱气。
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公开(公告)号：US08247578B2
公开(公告)日：2012-08-21
申请号：US13115385
申请日：2011-05-25
申请人： Toshihiro Takeda , Masatoshi Ohnuki
发明人： Toshihiro Takeda , Masatoshi Ohnuki
IPC分类号： C07D207/12
CPC分类号： C07D207/12 , Y02P20/55
摘要： The present invention provides a process for producing a 3-aralkyloxypyrrolidine derivative which is important for production of pharmaceutical products and the like. In the present invention, a N-protected-3-hydroxypyrrolidine is converted into a N-protected-3-aralkyloxypyrrolidine by allowing an aralkyl halide to act in the presence of a base and at least one of a metal halide and a phase-transfer catalyst followed by deprotecting a N-protecting group to convert it to a 3-aralkyloxypyrrolidine derivative and subsequently treating the derivative in a solvent containing a polar solvent, thereby obtaining the 3-aralkyloxypyrrolidine derivative as a crystal. According to the present invention, a 3-aralkyloxypyrrolidine derivative of high purity can be produced conveniently and efficiently on an industrial scale.
摘要翻译： 本发明提供了制备药物等的重要的3-芳烷氧基吡咯烷衍生物的制造方法。 在本发明中，通过使芳烷基卤化物在碱的存在下和金属卤化物和相转移中的至少一种作用下，将N-保护的3-羟基吡咯烷转化为N-保护的3-芳烷氧基吡咯烷 催化剂，然后脱保护N-保护基，将其转化为3-芳烷氧基吡咯烷衍生物，随后在含有极性溶剂的溶剂中处理该衍生物，从而得到作为结晶的3-芳烷氧基吡咯烷衍生物。 根据本发明，可以以工业规模方便，高效地制造高纯度的3-芳基甲氧基吡咯烷衍生物。
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公开(公告)号：US20080306283A1
公开(公告)日：2008-12-11
申请号：US11990766
申请日：2006-08-22
IPC分类号： C07D207/12
CPC分类号： C07D207/12 , Y02P20/55
摘要： The present invention provides a process for producing a 3-aralkyloxypyrrolidine derivative which is important for production of pharmaceutical products and the like. In the present invention, a N-protected-3-hydroxypyrrolidine is converted into a N-protected-3-aralkyloxypyrrolidine by allowing an aralkyl halide to act in the presence of a base and at least one of a metal halide and a phase-transfer catalyst followed by deprotecting a N-protecting group to convert it to a 3-aralkyloxypyrrolidine derivative and subsequently treating the derivative in a solvent containing a polar solvent, thereby obtaining the 3-aralkyloxypyrrolidine derivative as a crystal. According to the present invention, a 3-aralkyloxypyrrolidine derivative of high purity can be produced conveniently and efficiently on an industrial scale.
摘要翻译： 本发明提供了制备药物等的重要的3-芳烷氧基吡咯烷衍生物的制造方法。 在本发明中，通过使芳烷基卤化物在碱的存在下和金属卤化物和相转移中的至少一种作用下，将N-保护的3-羟基吡咯烷转化为N-保护的3-芳烷氧基吡咯烷 催化剂，然后脱保护N-保护基，将其转化为3-芳烷氧基吡咯烷衍生物，随后在含有极性溶剂的溶剂中处理该衍生物，从而得到作为结晶的3-芳烷氧基吡咯烷衍生物。 根据本发明，可以以工业规模方便，高效地制造高纯度的3-芳基甲氧基吡咯烷衍生物。
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公开(公告)号：US07973176B2
公开(公告)日：2011-07-05
申请号：US11990766
申请日：2006-08-22
IPC分类号： C07D207/12
CPC分类号： C07D207/12 , Y02P20/55
摘要： The present invention provides a process for producing a 3-aralkyloxypyrrolidine derivative which is important for production of pharmaceutical products and the like. In the present invention, a N-protected-3-hydroxypyrrolidine is converted into a N-protected-3-aralkyloxypyrrolidine by allowing an aralkyl halide to act in the presence of a base and at least one of a metal halide and a phase-transfer catalyst followed by deprotecting a N-protecting group to convert it to a 3-aralkyloxypyrrolidine derivative and subsequently treating the derivative in a solvent containing a polar solvent, thereby obtaining the 3-aralkyloxypyrrolidine derivative as a crystal. According to the present invention, a 3-aralkyloxypyrrolidine derivative of high purity can be produced conveniently and efficiently on an industrial scale.
摘要翻译： 本发明提供了制备药物等的重要的3-芳烷氧基吡咯烷衍生物的制造方法。 在本发明中，通过使芳烷基卤化物在碱的存在下和金属卤化物和相转移中的至少一种作用下，将N-保护的3-羟基吡咯烷转化为N-保护的3-芳烷氧基吡咯烷 催化剂，然后脱保护N-保护基，将其转化为3-芳烷氧基吡咯烷衍生物，随后在含有极性溶剂的溶剂中处理该衍生物，从而得到作为结晶的3-芳烷氧基吡咯烷衍生物。 根据本发明，可以以工业规模方便，高效地制造高纯度的3-芳基甲氧基吡咯烷衍生物。
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公开(公告)号：US20100087643A1
公开(公告)日：2010-04-08
申请号：US12449460
申请日：2008-02-05
IPC分类号： C07D241/04
CPC分类号： C07B53/00 , C07D241/04
摘要： The objective of the present invention is to produce an optically active 2-arylpiperazine derivative useful as a synthetic intermediate for pharmaceutical products and agricultural chemicals from inexpensive and readily available starting material by an industrially practicable method. The objective can be accomplished by treating an optically active substituted aminodiol derivative produced from an optically active styrene oxide derivative with a sulfonating agent in the presence of a base, and then reacting an amine compound to obtain the 2-arylpiperazine derivative. Especially, an optically active 1-unsubstituted-2-arylpiperazine derivative can be produced by treating an optically active 1-allyl-2-arylpiperazine derivative with water in the presence of a transition metal catalyst for deallylation.
摘要翻译： 本发明的目的是通过工业上可行的方法从便宜且容易获得的原料制备用作药物产品和农药的合成中间体的光学活性2-芳基哌嗪衍生物。 该目的可以通过在碱的存在下用磺化剂处理由光学活性苯乙烯氧化物衍生物产生的光学活性取代的氨基二醇衍生物，然后使胺化合物反应得到2-芳基哌嗪衍生物来实现。 特别地，光学活性的1-未取代-2-芳基哌嗪衍生物可以通过在过渡金属催化剂的存在下用水处理光学活性的1-烯丙基-2-芳基哌嗪衍生物来进行脱气。
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7.发明授权公开(公告)号：US08030501B2
公开(公告)日：2011-10-04
申请号：US12375141
申请日：2007-07-23
IPC分类号： C07D295/00
CPC分类号： C07D207/14 , C07D207/10 , C07D207/12 , C07D207/27
摘要： Aiming at production of an optically active 3-amino nitrogen-containing compound which is useful as an intermediate in synthesis of medicines and pesticides, in particular, an optically active 1-protected-3-aminopyrrolidine derivative, from an inexpensive and readily available raw material by a process which is efficient and can be practiced industrially, an optically active 3-amino nitrogen-containing compound is produced by performing a reaction of an optically active 3-substituted nitrogen-containing compound with ammonia, methylamine, ethylamine or dimethylamine in the presence of water. In addition, a 1-protected-3-aminopyrrolidine derivative is produced by performing a reaction of an optically active 1-protected-3-(sulfonyloxy)pyrrolidine derivative with ammonia, methylamine, ethylamine, or dimethylamine in the presence of methanol, ethanol, n-propanol, or isopropanol under a pressure of less than 30 barr.
摘要翻译： 本发明涉及一种光学活性3-氨基含氮化合物的制备，其可用作药物和农药合成中的中间体，特别是光学活性的1-保护的3-氨基吡咯烷衍生物，由廉价且容易获得的原料 通过工业上有效且可以在工业上实践的方法，通过在存在下进行光学活性的3-取代的含氮化合物与氨，甲胺，乙胺或二甲胺的反应来制备光学活性的3-氨基含氮化合物 的水。 此外，通过在甲醇，乙醇，甲醇，乙醇等的存在下进行光学活性的1-保护的3-（磺酰氧基）吡咯烷衍生物与氨，甲胺，乙胺或二甲胺的反应来制备1-保护的3-氨基吡咯烷衍生物， 正丙醇或异丙醇，压力小于30巴。
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公开(公告)号：US20110224444A1
公开(公告)日：2011-09-15
申请号：US13115385
申请日：2011-05-25
IPC分类号： C07D207/12 , C07D207/00
CPC分类号： C07D207/12 , Y02P20/55
摘要： The present invention provides a process for producing a 3-aralkyloxypyrrolidine derivative which is important for production of pharmaceutical products and the like. In the present invention, a N-protected-3-hydroxypyrrolidine is converted into a N-protected-3-aralkyloxypyrrolidine by allowing an aralkyl halide to act in the presence of a base and at least one of a metal halide and a phase-transfer catalyst followed by deprotecting a N-protecting group to convert it to a 3-aralkyloxypyrrolidine derivative and subsequently treating the derivative in a solvent containing a polar solvent, thereby obtaining the 3-aralkyloxypyrrolidine derivative as a crystal. According to the present invention, a 3-aralkyloxypyrrolidine derivative of high purity can be produced conveniently and efficiently on an industrial scale.
摘要翻译： 本发明提供了制备药物等的重要的3-芳烷氧基吡咯烷衍生物的制造方法。 在本发明中，通过使芳烷基卤化物在碱的存在下和金属卤化物和相转移中的至少一种作用下，将N-保护的3-羟基吡咯烷转化为N-保护的3-芳烷氧基吡咯烷 催化剂，然后脱保护N-保护基，将其转化为3-芳烷氧基吡咯烷衍生物，随后在含有极性溶剂的溶剂中处理该衍生物，从而得到作为结晶的3-芳烷氧基吡咯烷衍生物。 根据本发明，可以以工业规模方便，高效地制造高纯度的3-芳基甲氧基吡咯烷衍生物。
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