公开(公告)号：US06187932B1

公开(公告)日：2001-02-13

申请号：US09077747

申请日：1998-08-03

申请人： Koichi Kinoshita ,  Fumihiko Kano ,  Takahiro Okubo ,  Yasuyoshi Ueda

发明人： Koichi Kinoshita ,  Fumihiko Kano ,  Takahiro Okubo ,  Yasuyoshi Ueda

IPC分类号： C07D20712

CPC分类号： C07D207/16

摘要： A process for producing captopril of the following formula (1) comprising subjecting a substrate compound of the following general formula (2) to a hydrolysis reaction in aqueous medium to remove the RCO group and isolating the product compound, said hydrolysis reaction in aqueous medium being conducted in the presence of a strong acid at pH not over 1 and a reaction temperature not below 40° C.

摘要翻译： 一种制备下式（1）的卡托普利的方法，包括使下列通式（2）的底物化合物在水性介质中进行水解反应以除去RCO基团并分离产物化合物，水介质中的所述水解反应为 在pH不超过1，反应温度不低于40℃的强酸存在下进行。

公开(公告)号：US6140527A

公开(公告)日：2000-10-31

申请号：US355529

申请日：1999-09-07

申请人： Shigeki Kunihiro ,  Fumihiko Kano ,  Natsuki Mori

发明人： Shigeki Kunihiro ,  Fumihiko Kano ,  Natsuki Mori

IPC分类号： C07C253/14 ,  C07C253/34 ,  C07C255/20 ,  C07C253/00

CPC分类号： C07C253/34 ,  C07C253/14

摘要： This invention has its objects to provide a process for producing a butyric acid ester derivative of the above general formula (2) which is capable of removing various impurity byproducts whose formation cannot be avoided by the prior art technology, particularly the compound of the above general formula (1), with good efficiency.This invention is related to a process for producing a butyric acid ester derivative of the general formula (2) which comprises treating a mixture containing a compound of the following general formula (1) with an addition reagent capable of adding itself to said ethylenic bond to thereby convert said compound of the general formula (1) to an addition product which can be easily separated from said butyric acid ester derivative of the general formula (2) and a process for producing a butyric acid ester derivative of the general formula (2) which comprises reacting a compound of the general formula (3) with a salt of prussic acid by a flow method.HOCH.sub.2 --CH.dbd.CH--COOR (1) ##STR1##

摘要翻译： PCT No.PCT / JP98 / 03686 Sec。 371 1999年9月7日第 102（e）1999年9月7日PCT PCT 1998年8月20日PCT公布。 出版物WO99 /​​ 31050 日期1999年6月24日本发明的目的是提供一种上述通式（2）的丁酸酯衍生物的制造方法，其能够除去现有技术中不能避免的各种杂质副产物，特别是 上述通式（1）的化合物，效率高。 本发明涉及一种制备通式（2）的丁酸酯衍生物的方法，该方法包括用能够将其自身加入所述烯键的加成试剂处理含有下列通式（1）的化合物的混合物 从而将所述通式（1）的化合物转化为可以容易地从通式（2）的丁酸酯衍生物分离的加成产物和通式（2）的丁酸酯衍生物的制备方法， 其包括通过流动法使通式（3）的化合物与氢氰酸的盐反应。 HOCH2-CH = CH- COOR（1）

公开(公告)号：US06864372B2

公开(公告)日：2005-03-08

申请号：US10438924

申请日：2003-05-16

申请人： Fumihiko Kano ,  Shigeki Kunihiro ,  Noritaka Yoshida ,  Natsuki Mori

发明人： Fumihiko Kano ,  Shigeki Kunihiro ,  Noritaka Yoshida ,  Natsuki Mori

IPC分类号： C07C303/28 ,  C07C309/65 ,  C07C309/66 ,  C07C309/73 ,  C07D207/12 ,  C07D207/24 ,  C07D211/40 ,  C07D223/08 ,  C07D211/06 ,  C07C303/26

CPC分类号： C07C303/28 ,  C07D207/12 ,  C07C309/65 ,  C07C309/66 ,  C07C309/73

摘要： Sulfonic acid ester derivatives represented by the general formula (4) or (5) are produced by reacting an amino alcohol derivative represented by the general formula (1) or (2) with an organic sulfonyl halide represented by the general formula (3), in a mixed solvent composed of an aprotic organic solvent and water in the presence of a non-water-prohibiting inorganic base. This procedure can be carried out in a simple, easy, safe and economical manner while reducing the load on the environment. Wherein n represents an integer of 0 to 5, A represents a phenyl group, which may be substituted, R represents a methanesulfonyl, ethanesulfonyl, p-toluenesulfonyl or p-nitrobenzenesulfonyl group and X represents a chloride, bromine or iodine atom.

摘要翻译： 由通式（4）或（5）表示的磺酸酯衍生物通过使由通式（1）或（2）表示的氨基醇衍生物与通式（3）表示的有机磺酰卤反应， 在由非水性阻止无机碱存在下由非质子有机溶剂和水组成的混合溶剂中。 该方法可以简单，容易，安全和经济地进行，同时减少环境负荷。其中n表示0至5的整数，A表示可被取代的苯基，R表示甲磺酰基， 乙磺酰基，对甲苯磺酰基或对硝基苯磺酰基，X表示氯，溴或碘原子。

公开(公告)号：US07268236B2

公开(公告)日：2007-09-11

申请号：US10490267

申请日：2003-03-28

申请人： Fumihiko Kano ,  Natsuki Mori

发明人： Fumihiko Kano ,  Natsuki Mori

IPC分类号： C07D207/14

CPC分类号： C07D207/14

摘要： The present invention provides a method to improve the optical purity of 1-benzyl-3-aminopyrrolidine having a low optical purity using an inexpensive agent via a simple procedure. The present invention provides a method for improving the optical purity of 1-benzyl-3-aminopyrrolidine including the steps of converting 1-benzyl-3-aminopyrrolidine into an equimolar salt with an optically inactive acid, and recovering the salt as crystals. The present invention also provides a salt of 1-benzyl-3-aminopyrrolidine that is used in the method.

摘要翻译： 本发明提供了通过简单的方法使用廉价的试剂提高具有低光学纯度的1-苄基-3-氨基吡咯烷酮的光学纯度的方法。 本发明提供了提高1-苄基-3-氨基吡咯烷的光学纯度的方法，包括以下步骤：将1-苄基-3-氨基吡咯烷转化成等摩尔盐与光学惰性的酸反应，并回收盐晶体。 本发明还提供了用于该方法的1-苄基-3-氨基吡咯烷的盐。

公开(公告)号：US20080255371A1

公开(公告)日：2008-10-16

申请号：US11882653

申请日：2007-08-03

申请人： Fumihiko Kano ,  Natsuki Mori

发明人： Fumihiko Kano ,  Natsuki Mori

IPC分类号： C07D207/14

CPC分类号： C07D207/14

摘要： The present invention provides a method to improve the optical purity of 1-benzyl-3-aminopyrrolidine having a low optical purity using an inexpensive agent via a simple procedure. The present invention provides a method for improving the optical purity of 1-benzyl-3-aminopyrrolidine including the steps of converting 1-benzyl-3-aminopyrrolidine into an equimolar salt with an optically inactive acid, and recovering the salt as crystals. The present invention also provides a salt of 1-benzyl-3-aminopyrrolidine that is used in the method.

摘要翻译： 本发明提供了通过简单的方法使用廉价的试剂提高具有低光学纯度的1-苄基-3-氨基吡咯烷酮的光学纯度的方法。 本发明提供了提高1-苄基-3-氨基吡咯烷的光学纯度的方法，包括以下步骤：将1-苄基-3-氨基吡咯烷转化成等摩尔盐与光学惰性的酸反应，并回收盐晶体。 本发明还提供了用于该方法的1-苄基-3-氨基吡咯烷的盐。

公开(公告)号：US06794519B2

公开(公告)日：2004-09-21

申请号：US10067784

申请日：2002-02-08

申请人： Fumihiko Kano ,  Shigeki Kunihiro ,  Noritaka Yoshida ,  Natsuki Mori

发明人： Fumihiko Kano ,  Shigeki Kunihiro ,  Noritaka Yoshida ,  Natsuki Mori

IPC分类号： C07D20704

CPC分类号： C07C303/28 ,  C07D207/12 ,  C07C309/65 ,  C07C309/66 ,  C07C309/73

摘要： Sulfonic acid ester derivatives represented by the general formula (4) or (5) are produced by reacting an amino alcohol derivative represented by the general formula (1) or (2) with an organic sulfonyl halide represented by the general formula (3), in a mixed solvent composed of an aprotic organic solvent and water in the presence of a non-water-prohibiting inorganic base. This procedure can be carried out in a simple, easy, safe and economical manner while reducing the load on the environment. Wherein n represents an integer of 0 to 5, A represents a phenyl group, which may be substituted, R represents a methanesulfonyl, ethanesulfonyl, p-toluenesulfonyl or p-nitrobenzenesulfonyl group and X represents a chloride, bromine or iodine atom.

摘要翻译： 由通式（4）或（5）表示的磺酸酯衍生物通过使由通式（1）或（2）表示的氨基醇衍生物与通式（3）表示的有机磺酰卤反应， 在由非水性阻止无机碱存在下由非质子有机溶剂和水组成的混合溶剂中。 该方法可以简单，容易，安全和经济地进行，同时减少环境负荷。其中n表示0至5的整数，A表示可被取代的苯基，R表示甲磺酰基， 乙磺酰基，对甲苯磺酰基或对硝基苯磺酰基，X表示氯，溴或碘原子。

公开(公告)号：US06992205B2

公开(公告)日：2006-01-31

申请号：US10438922

申请日：2003-05-16

申请人： Fumihiko Kano ,  Shigeki Kunihiro ,  Noritaka Yoshida ,  Natsuki Mori

发明人： Fumihiko Kano ,  Shigeki Kunihiro ,  Noritaka Yoshida ,  Natsuki Mori

IPC分类号： C07C303/26

CPC分类号： C07C303/28 ,  C07D207/12 ,  C07C309/65 ,  C07C309/66 ,  C07C309/73

摘要： Sulfonic acid ester derivatives represented by the general formula (4) or (5) are produced by reacting an amino alcohol derivative represented by the general formula (1) or (2) with an organic sulfonyl halide represented by the general formula (3), in a mixed solvent composed of an aprotic organic solvent and water in the presence of a non-water-prohibiting inorganic base. This procedure can be carried out in a simple, easy, safe and economical manner while reducing the load on the environment. Wherein n represents an integer of 0 to 5, A represents a phenyl group, which may be substituted, R represents a methanesulfonyl, ethanesulfonyl, p-toluenesulfonyl or p-nitrobenzenesulfonyl group and X represents a chloride, bromine or iodine atom.

公开(公告)号：US4859661A

公开(公告)日：1989-08-22

申请号：US75021

申请日：1987-07-13

申请人： Fumihiko Kano ,  Takehiko Yamane ,  Katsuji Yamashita ,  Kazunori Hosoe ,  Kiyoshi Watanabe

发明人： Fumihiko Kano ,  Takehiko Yamane ,  Katsuji Yamashita ,  Kazunori Hosoe ,  Kiyoshi Watanabe

IPC分类号： C07D498/18 ,  A61K31/365 ,  A61K31/535 ,  A61P31/04 ,  C07D498/14

CPC分类号： C07D498/18 ,  C07D519/00

摘要： A novel rifamycin derivative having the formula (I): ##STR1## wherein X.sup.1 is an alkyl group with 1 to 6 carbon atoms or a cycloalkyl group with 3 to 8 carbon atoms; X.sup.2 is a hydrogen atom or an alkyl group with 1 to 4 carbon atoms; R.sup.1 is hydrogen atom or acetyl group; A is a group represented by the formula: ##STR2## wherein R.sup.2 is an alkyl group with 1 to 4 carbon atoms or an alkoxyalkyl group with 2 to 6 carbon atoms and R.sup.3 is an alkyl group with 1 to 6 carbon atoms or an alkoxyalkyl group with 2 to 6 carbon atoms, or a group represented by the formula ##STR3## wherein ##STR4## is a 3 to 9 membered cyclic amino group with 2 to 8 carbon atoms, R.sup.4 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, or salts thereof, a process for preparing the same and antibacterial agents containing the same as an effective ingredient.The rifamycin derivative of the present invention having the formula (I) shows a strong antibacterial activity against the Gram-positive bacteria and the acid-fast bacteria.