公开(公告)号：US20090259045A1

公开(公告)日：2009-10-15

申请号：US12311016

申请日：2007-10-10

申请人： Hirohito Oooka ,  Shinya Fukuhara

发明人： Hirohito Oooka ,  Shinya Fukuhara

IPC分类号： C07D221/02

CPC分类号： C07D221/22 ,  C07D221/24

摘要： The object is to produce an azabicycloalkanol derivative, particularly a cis-3-substituted-3-azabicyclo[3.2.1]octan-8-ol derivative which is a useful intermediate for agricultural chemicals or pharmaceutical agents, with a good yield and at an industrially low cost. A diastereomer of an azabicyclo-C6-10-alkanol derivative having a methyne substituted a hydroxyl group as an asymmetric carbon (e.g., a trans-3-substituted-3-azabicyclo[3.2.1]-8-ol derivative) is isomerized in the presence of a transition metal complex, thereby producing an excess amount of a thermodynamically more stable one of diastereomers (e.g., a cis-3-substituted-3-azabicyclo[3.2.1]-8-ol derivative). In this manner, a thermodynamically more stable one of diastereomers of the azabicyclo-C6-10-alkanol derivatives can be produced.

摘要翻译： 本发明的目的是制备氮杂双链烷醇衍生物，特别是作为农药或药剂的有用中间体的顺式-3-取代-3-氮杂双环[3.2.1]辛-8-醇衍生物，其产率高， 工业成本低。 具有取代羟基作为不对称碳的甲炔的氮杂双环C 6-10链烷醇衍生物的非对映体（例如，反式-3-取代-3-氮杂双环[3.2.1] -8-醇衍生物）异构化为 过渡金属络合物的存在，从而产生过量的热力学上更稳定的非对映异构体（例如，顺式-3-取代-3-氮杂双环[3.2.1] -8-醇衍生物）。 以这种方式，可以制备氮杂双环C 6-10链烷醇衍生物的非对映异构体的热力学上更稳定的一种。

公开(公告)号：US20120209004A1

公开(公告)日：2012-08-16

申请号：US13454558

申请日：2012-04-24

申请人： Hirohito Oooka ,  Shinya Fukuhara

发明人： Hirohito Oooka ,  Shinya Fukuhara

IPC分类号： C07D221/22

CPC分类号： C07D221/22 ,  C07D221/24

摘要： The object is to produce an azabicycloalkanol derivative, particularly a cis-3-substituted-3-azabicyclo[3.2.1]octan-8-ol derivative which is a useful intermediate for agricultural chemicals or pharmaceutical agents, with a good yield and at an industrially low cost. A diastereomer of an azabicyclo-C6-10-alkanol derivative having a methyne substituted a hydroxyl group as an asymmetric carbon (e.g., a trans-3-substituted-3-azabicyclo[3.2.1]-8-ol derivative) is isomerized in the presence of a transition metal complex, thereby producing an excess amount of a thermodynamically more stable one of diastereomers (e.g., a cis-3-substituted-3-azabicyclo[3.2.1]-8-ol derivative). In this manner, a thermodynamically more stable one of diastereomers of the azabicyclo-C6-10-alkanol derivatives can be produced.

摘要翻译： 本发明的目的是制备氮杂双链烷醇衍生物，特别是作为农药或药剂的有用中间体的顺式-3-取代-3-氮杂双环[3.2.1]辛-8-醇衍生物，其产率高， 工业成本低。 具有取代羟基作为不对称碳的甲炔的氮杂双环C 6-10链烷醇衍生物的非对映体（例如，反式-3-取代-3-氮杂双环[3.2.1] -8-醇衍生物）异构化为 过渡金属络合物的存在，从而产生过量的热力学上更稳定的非对映异构体（例如，顺式-3-取代-3-氮杂双环[3.2.1] -8-醇衍生物）。 以这种方式，可以制备氮杂双环C 6-10链烷醇衍生物的非对映异构体的热力学上更稳定的一种。

公开(公告)号：US08431707B2

公开(公告)日：2013-04-30

申请号：US13454558

申请日：2012-04-24

申请人： Hirohito Oooka ,  Shinya Fukuhara

发明人： Hirohito Oooka ,  Shinya Fukuhara

IPC分类号： C07D221/02

CPC分类号： C07D221/22 ,  C07D221/24

摘要： The object is to produce an azabicycloalkanol derivative, particularly a cis-3-substituted-3-azabicyclo[3.2.1]octan-8-ol derivative which is a useful intermediate for agricultural chemicals or pharmaceutical agents, with a good yield and at an industrially low cost. A diastereomer of an azabicyclo-C6-10-alkanol derivative having a methyne substituted a hydroxyl group as an asymmetric carbon (e.g., a trans-3-substituted-3-azabicyclo[3.2.1]-8-ol derivative) is isomerized in the presence of a transition metal complex, thereby producing an excess amount of a thermodynamically more stable one of diastereomers (e.g., a cis-3-substituted-3-azabicyclo[3.2.1]-8-ol derivative). In this manner, a thermodynamically more stable one of diastereomers of the azabicyclo-C6-10-alkanol derivatives can be produced.

公开(公告)号：US08188286B2

公开(公告)日：2012-05-29

申请号：US12311016

申请日：2007-10-10

申请人： Hirohito Oooka ,  Shinya Fukuhara

发明人： Hirohito Oooka ,  Shinya Fukuhara

IPC分类号： C07D221/02

CPC分类号： C07D221/22 ,  C07D221/24

摘要： The object is to produce an azabicycloalkanol derivative, particularly a cis-3-substituted-3-azabicyclo[3.2.1]octan-8-ol derivative which is a useful intermediate for agricultural chemicals or pharmaceutical agents, with a good yield and at an industrially low cost. A diastereomer of an azabicyclo-C6-10-alkanol derivative having a methyne substituted a hydroxyl group as an asymmetric carbon (e.g., a trans-3-substituted-3-azabicyclo[3.2.1]-8-ol derivative) is isomerized in the presence of a transition metal complex, thereby producing an excess amount of a thermodynamically more stable one of diastereomers (e.g., a cis-3-substituted-3-azabicyclo[3.2.1]-8-ol derivative). In this manner, a thermodynamically more stable one of diastereomers of the azabicyclo-C6-10-alkanol derivatives can be produced.

摘要翻译： 本发明的目的是制备氮杂双链烷醇衍生物，特别是作为农药或药剂的有用中间体的顺式-3-取代-3-氮杂双环[3.2.1]辛-8-醇衍生物，其产率高， 工业成本低。 具有取代羟基作为不对称碳的甲炔的氮杂双环C 6-10链烷醇衍生物的非对映体（例如，反式-3-取代-3-氮杂双环[3.2.1] -8-醇衍生物）异构化为 过渡金属络合物的存在，从而产生过量的热力学上更稳定的非对映异构体（例如，顺式-3-取代-3-氮杂双环[3.2.1] -8-醇衍生物）。 以这种方式，可以制备氮杂双环C 6-10链烷醇衍生物的非对映异构体的热力学上更稳定的一种。

公开(公告)号：US20100286398A1

公开(公告)日：2010-11-11

申请号：US12674326

申请日：2008-08-27

申请人： Hiroshi Hakuta ,  Tsutomu Imagawa ,  Hirohito Oooka ,  Shinya Fukuhara

发明人： Hiroshi Hakuta ,  Tsutomu Imagawa ,  Hirohito Oooka ,  Shinya Fukuhara

IPC分类号： C07D221/22

CPC分类号： C07D221/24 ,  C07B55/00

摘要： There are provided, according to the present invention, a method for producing a cis-3-substituted-3-azabicyclo[3.2.1]octan-8-ol derivative, the method characterized in that a trans-3-substituted-3-azabicyclo[3.2.1]octan-8-ol derivative or a mixture of the trans- and cis-3-substituted-3-azabicyclo[3.2.1]octan-8-ol derivatives is isomerized in the presence of an aluminum compound represented by a formula Al(OR1)3 (wherein R1 represents a hydrocarbon group in which a carbon atom having an oxygen atom bonded thereto is a secondary carbon atom). In the process, a ketone compound may be further added, in addition to the aluminum compound.

摘要翻译： 根据本发明，提供顺式-3-取代-3-氮杂双环[3.2.1]辛-8-醇衍生物的制备方法，其特征在于反式-3-取代-3-氮杂双环[3.2.1] 氮杂双环[3.2.1]辛-8-醇衍生物或反式和顺式-3-取代-3-氮杂双环[3.2.1]辛-8-醇衍生物的混合物在代表的铝化合物存在下异构化 通过式Al（OR1）3（其中R1表示其中键合有氧原子的碳原子是仲碳原子的烃基）。 在该方法中，除了铝化合物之外，还可以加入酮化合物。

公开(公告)号：US08461340B2

公开(公告)日：2013-06-11

申请号：US12674326

申请日：2008-08-27

申请人： Hiroshi Hakuta ,  Tsutomu Imagawa ,  Hirohito Oooka ,  Shinya Fukuhara

发明人： Hiroshi Hakuta ,  Tsutomu Imagawa ,  Hirohito Oooka ,  Shinya Fukuhara

IPC分类号： C07D221/22

CPC分类号： C07D221/24 ,  C07B55/00

摘要： There are provided, according to the present invention, a method for producing a cis-3-substituted-3-azabicyclo[3.2.1]octan-8-ol derivative, the method characterized in that a trans-3-substituted-3-azabicyclo[3.2.1]octan-8-ol derivative or a mixture of the trans- and cis-3-substituted-3-azabicyclo[3.2.1]octan-8-ol derivatives is isomerized in the presence of an aluminum compound represented by a formula Al(OR1)3 (wherein R1 represents a hydrocarbon group in which a carbon atom having an oxygen atom bonded thereto is a secondary carbon atom). In the process, a ketone compound may be further added, in addition to the aluminum compound.

摘要翻译： 根据本发明，提供顺式-3-取代-3-氮杂双环[3.2.1]辛-8-醇衍生物的制备方法，其特征在于反式-3-取代-3-氮杂双环[3.2.1] 氮杂双环[3.2.1]辛-8-醇衍生物或反式和顺式-3-取代-3-氮杂双环[3.2.1]辛-8-醇衍生物的混合物在代表的铝化合物存在下异构化 通过式Al（OR1）3（其中R1表示其中键合有氧原子的碳原子是仲碳原子的烃基）。 在该方法中，除了铝化合物之外，还可以加入酮化合物。

公开(公告)号：US20110117157A1

公开(公告)日：2011-05-19

申请号：US13002689

申请日：2009-07-07

申请人： Yoshihisa Endo ,  Yoshio Nakamura ,  Shinya Fukuhara

发明人： Yoshihisa Endo ,  Yoshio Nakamura ,  Shinya Fukuhara

IPC分类号： A01N43/40 ,  A01N25/10 ,  A01P7/04 ,  B29B9/00

CPC分类号： A01N47/40 ,  A01N25/10 ,  A01N2300/00

摘要： The present invention offers a method of manufacture of sustained-release formulation composition which includes a step of spray drying a composition that contains (1) an active ingredient, (2) a resin ingredient, and (3) a solvent, using a spray dryer and controlling the exit temperature of the spray dryer, wherein solvent content in the composition after spray drying is 5 mass % or less, and the composition after the aforementioned spray drying does not substantially contain decomposed matter of the aforementioned active ingredient.

摘要翻译： 本发明提供一种制备缓释制剂组合物的方法，其包括使用喷雾干燥器喷雾干燥含有（1）活性成分，（2）树脂成分和（3）溶剂）的组合物的步骤 并控制喷雾干燥器的出口温度，其中喷雾干燥后组合物中的溶剂含量为5质量％以下，上述喷雾干燥后的组成基本上不含有上述活性成分的分解物。