公开(公告)号：US20180319816A1

公开(公告)日：2018-11-08

申请号：US16034002

申请日：2018-07-12

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Kazuhiro MIWA ,  Tsuyoshi SASAKI ,  Fumiya KOMURA

IPC: C07D495/04 ,  C07D409/12 ,  C07D333/38

Abstract: The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrimidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1′-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.

公开(公告)号：US20220204525A1

公开(公告)日：2022-06-30

申请号：US17694635

申请日：2022-03-14

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Koichiro FUKUOKA ,  Kazuhiro MIWA ,  Tsuyoshi SASAKI ,  Fumiya KOMURA

IPC: C07D495/04 ,  C07D333/38 ,  C07D409/12

Abstract: The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrirnidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1′-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.

公开(公告)号：US20180297980A1

公开(公告)日：2018-10-18

申请号：US15768037

申请日：2016-10-14

Applicant: Takeda Pharmaceutical Company Limited

Inventor： Fumiya KOMURA ,  Yoshihiro HIGUGHI

IPC: C07D401/06 ,  C07D401/14 ,  B01J31/22

CPC classification number: C07D401/06 ,  B01J31/2208 ,  B01J2531/824 ,  C07B61/00 ,  C07D401/14

Abstract: The present invention provides a production method of heterocyclic compound having an excellent CH24H inhibitory action, which is suitable for industrial production.In the present invention, a 2-halogenonicotinic acid or a reactive derivative thereof or a salt thereof is reacted with 4-benzyl-4-hydroxypiperidine acid addition salt to give a (4-benzyl-4-hydroxypiperidin-1-yl) (2-halogenopyridin-3-yl)methanone or a salt thereof, and then the obtained compound is reacted with pyridine-4-boronic acid or a reactive derivative thereof or a salt thereof in the presence of a metal catalyst and a base to give (4-benzyl-4-hydroxypiperidin-1-yl) (2,4′-bipyridin-3-yl)methanone or a salt thereof.

公开(公告)号：US20170210753A1

公开(公告)日：2017-07-27

申请号：US15481505

申请日：2017-04-07

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

Inventor： Koichiro FUKUOKA ,  Kazuhiro MIWA ,  Tsuyoshi SASAKI ,  Fumiya KOMURA

IPC: C07D495/04 ,  C07D409/12 ,  C07D333/38

CPC classification number: C07D495/04 ,  C07D333/38 ,  C07D409/12

Abstract: The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrimidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1′-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.