公开(公告)号：EP3394042A1

公开(公告)日：2018-10-31

申请号：EP16826192.3

申请日：2016-12-22

申请人： Shionogi & Co., Ltd

发明人： ONODERA, Naohiro ,  NOGUCHI, Kouichi ,  ANDO, Shigeru ,  NAGAMATSU, Daiki ,  ISHIBASHI, Kenichi ,  OCHI, Shunsuke ,  HASEGAWA, Aiko ,  ODA, Katsuo

IPC分类号： C07D279/06 ,  C07D417/12

CPC分类号： C07D279/06 ,  C07D417/12

摘要： The present invention provides a process for preparation of the compound of formula (VI), wherein each symbol is as defined in the specification, without using any intermediate compound showing mutagenicity. The process comprises salt formation of the intermediate compound of formula (I) with acid to enable optical resolution to isolate the intermediate compound of formula (II) in a stereo-selective manner.

公开(公告)号：EP2505584A1

公开(公告)日：2012-10-03

申请号：EP10833197.6

申请日：2010-11-24

申请人： Shionogi & Co., Ltd.

发明人： KUNITANI, Ryosuke ,  TAKAYA, Kenji ,  IMAMURA, Yoshiaki ,  HASEGAWA, Aiko

IPC分类号： C07D263/58 ,  C07D277/82

CPC分类号： C07D263/58 ,  C07D277/82

摘要： A process for the preparation of a compound of formula (I):

wherein R 1 is each independently halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl, C1-C6 haloalkoxy or C1-C6 alkylcarbonyl,
R 3 is C1-C6 alkyl; C3-C8 cycloalkyl; or phenyl optionally substituted with one or more substituents selected from the group consisting of halogen, C1-C6 alkyl; C1-C6 alkoxy, C1-C6 haloalkyl and C1-C6 haloalkoxy,
n is an integer of 0 to 2,
X is S atom or O atom,

its salt or solvate thereof characterized by reacting a compound of formula (IV):

wherein R 1 , n and X have the same meaning as defined above, and
R 2 is C1-C6 alkyl; C1-C6 haloalkyl; or phenyl optionally substituted with one or more substituents selected from the group consisting of halogen, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 haloalkyl, C1-C6 haloalkoxy and nitro,

with a compound of formula (V):

wherein R 3 has the same meaning as defined above.

摘要翻译： 一种制备式（I）化合物的方法：其中R 1各自独立地为卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，C 1 -C 6卤代烷基，C 1 -C 6卤代烷氧基或C 1 -C 6烷基羰基，R 3为 C1-C6烷基; C3-C8环烷基; 或任选被一个或多个选自以下的取代基取代的苯基：卤素，C 1 -C 6烷基; C1-C6烷氧基，C1-C6卤代烷基和C1-C6卤代烷氧基，n是0-2的整数，X是S原子或O原子，其盐或溶剂合物的特征在于使式（Ⅳ）化合物：其中R 1，n和X具有与上述相同的含义，R 2是C 1 -C 6烷基; C1-C6卤代烷基; 或任选被一个或多个选自卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，C 1 -C 6卤代烷基，C 1 -C 6卤代烷氧基和硝基的取代基取代的苯基与式（Ⅴ）化合物反应：其中R 3具有与上述相同的含义。