公开(公告)号：EP2123769B1

公开(公告)日：2016-05-18

申请号：EP08711442.7

申请日：2008-02-18

申请人： Kaneka Corporation

发明人： MORI, Kohei ,  NOJIRI, Masutoshi ,  NISHIYAMA, Akira ,  TAOKA, Naoaki

IPC分类号： C12P41/00 ,  C07D211/56 ,  C07D211/60 ,  C07B57/00

CPC分类号： C07D211/60 ,  C07B57/00 ,  C07D211/56 ,  C12P17/12 ,  C12P41/006

公开(公告)号：EP3124470A1

公开(公告)日：2017-02-01

申请号：EP15769421.7

申请日：2015-03-23

申请人： Kaneka Corporation

发明人： MACHIDA, Koji ,  MORI, Kohei ,  KISHIMOTO, Narumi ,  TAKEDA, Toshihiro

IPC分类号： C07C277/08 ,  C07C279/24

摘要： A tri-carbobenzoxy-arginine represented by the following formula (2):

is produced by carbobenzoxylating the arginine or arginine derivative (1) represented by the following formula (1), or a salt thereof:

by adding carbobenzoxy chloride and a base in a water/organic solvent bilayer system to an arginine or arginine derivative (1) represented by the formula (1), or a salt thereof.

摘要翻译： 由下式（2）表示的三碳代苯甲酰氧基 - 精氨酸：通过对由下式（1）表示的精氨酸或精氨酸衍生物（1）或其盐进行苄氧羰基化生产：通过加入苄氧苯甲酰氯和碱 水/有机溶剂双层体系转化为式（1）表示的精氨酸或精氨酸衍生物（1）或其盐。

公开(公告)号：EP2039689A1

公开(公告)日：2009-03-25

申请号：EP07743869.5

申请日：2007-05-22

申请人： Kaneka Corporation

发明人： MORI, Kohei ,  NISHIYAMA, Akira ,  TAOKA, Naoaki ,  MORIYAMA, Daisuke ,  NAGASHIMA, Nobuo

IPC分类号： C07D263/16 ,  C07C67/31 ,  C07C69/675 ,  C07C231/12 ,  C07C231/16 ,  C07C237/04 ,  C07C237/22 ,  C07D301/24 ,  C07D303/16 ,  C07D303/48 ,  C12P7/42 ,  C12P7/62 ,  C07B53/00 ,  C07B61/00

CPC分类号： C07B53/00 ,  C07B2200/07 ,  C07C67/31 ,  C07C231/18 ,  C07C237/04 ,  C07C237/22 ,  C07C2601/02 ,  C07D263/16 ,  C07D301/24 ,  C07D303/16 ,  C07D303/48 ,  C12P7/42 ,  C12P13/02 ,  C12P41/002 ,  C07C69/675

摘要： An objective of the present application is to provide an industrially practicable method for producing an optically-active 3-amino-2-hydroxypropionic cyclopropylamide derivative or salt thereof from an inexpensive easily-available starting material. The derivative or salt thereof is useful as an intermediate for a medicine. It is also intended by the present application to provide a useful intermediate of the derivative. The objective is attained by the following method. First, an easily-available 2-halo-3-oxopropionic acid derivative is asymmetrically reduced, and then epoxidated to produce an optically-active epoxycarboxylic acid derivative. Next, the derivative is converted into an optically-active epoxyamide derivative by reaction with cyclopropylamine, and then reacted with a nitrile to obtain an optically-active oxazolinamide derivative. Subsequently, selective acid solvolysis of the oxazoline skeleton gives the optically-active 3-amino-2-hydroxypropionic cyclopropylamide derivative or salt thereof.

摘要翻译： 本申请的目的是提供从便宜的廉价起始材料制备光学活性3-氨基-2-羟基丙基环丙基酰胺衍生物或其盐的工业上可行的方法。 其衍生物或其盐可用作药物的中间体。 本申请还希望提供衍生物的有用中间体。 目的是通过以下方法实现。 首先，将易于获得的2-卤代-3-氧代丙酸衍生物不对称地还原，然后环氧化以产生光学活性的环氧羧酸衍生物。 接下来，通过与环丙胺反应将衍生物转化为光学活性环氧酰胺衍生物，然后与腈反应，得到光学活性的恶唑啉酰胺衍生物。 随后，恶唑啉骨架的选择性酸溶解分解得到光学活性3-氨基-2-羟基丙基环丙基酰胺衍生物或其盐。

公开(公告)号：EP3124470B1

公开(公告)日：2020-01-08

申请号：EP15769421.7

申请日：2015-03-23

申请人： Kaneka Corporation

发明人： MACHIDA, Koji ,  MORI, Kohei ,  KISHIMOTO, Narumi ,  TAKEDA, Toshihiro

IPC分类号： C07C277/08 ,  C07C279/24

公开(公告)号：EP2123769A1

公开(公告)日：2009-11-25

申请号：EP08711442.7

申请日：2008-02-18

申请人： Kaneka Corporation

发明人： MORI, Kohei ,  NOJIRI, Masutoshi ,  NISHIYAMA, Akira ,  TAOKA, Naoaki

IPC分类号： C12P41/00 ,  C07D211/56 ,  C07D211/60 ,  C07B57/00

CPC分类号： C07D211/60 ,  C07B57/00 ,  C07D211/56 ,  C12P17/12 ,  C12P41/006

摘要： The present invention relates to a method for producing an optically active 3-aminopiperidine or salt thereof. In the method, a racemic nipecotamide is stereoselectively hydrolyzed to obtain an optically active nipecotamide and an optically active nipecotic acid in the presence of an enzyme source derived from an organism, and then the optically active nipecotamide is derived into an optically active aminopiperidine or salt thereof by aroylation, Hofmann rearrangement, deprotection of the amino group and further deprotection; or the optically active nipecotamide is derived into an optically active aminopiperidine or salt thereof by selective protection with BOC, Hofmann rearrangement and further deprotection. It is possible by the present invention to produce an optically active 3-aminopiperidine or salt thereof useful as a pharmaceutical intermediate from an inexpensive and easily available starting material by easy method applicable to industrial manufacturing.

摘要翻译： 本发明涉及一种用于在光学活性的3-氨基哌啶或其盐的制造。 在该方法中，外消旋哌啶甲酰胺是立体选择性地水解，以获得光学活性的哌啶甲酰胺，并在从生物来源的酶源的存在下，以光学活性哌啶酸，然后将光学活性的哌啶甲酰胺推断为对光学活性的氨基哌啶或它们的盐 由芳酰化，霍夫曼重排，氨基和脱保护。此外脱保护; 或光学活性哌啶甲酰胺通过用BOC，霍夫曼重排和脱保护。此外选择性保护衍生插入光学活性氨基哌啶或其盐。 有可能通过本发明，以产生在3-氨基哌啶或其盐如从廉价且容易获得的起始原料的药物中间体通过适用于工业制造容易的方法及其有用的光学活性。