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公开(公告)号：EP3567040B1
公开(公告)日：2020-09-09
申请号：EP19181689.1
申请日：2014-06-24
申请人： Amgen, Inc
IPC分类号： C07D471/04
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公开(公告)号：EP3805232A1
公开(公告)日：2021-04-14
申请号：EP20197741.0
申请日：2014-06-09
申请人： Amgen Inc.
发明人： Bio, Matthew , Caille, Sebastian , Cochran, Brian , Fang, Yuanqing , Fox, Brian Matthew , Lucas, Brian , McGee, Lawrence R. , Vounatsos, Filisaty , Wiedemann, Sean , Wortman, Sarah
IPC分类号： C07D498/04 , C07C309/35
摘要： The present invention provides the crystalline form of an intermediate useful in processes for making 2-((3R,5R,6S)-5-(3-chlorophenyl)-6-(4-chlorophenyl)-1-((S)-1-(isopropylsulfonyl)-3-methylbutan-2-yl)-3-methyl-2-oxopiperidin-3-yl)acetic acid as well as processes for making the intermediate.
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3.发明公开
公开(公告)号：EP3567040A1
公开(公告)日：2019-11-13
申请号：EP19181689.1
申请日：2014-06-24
申请人： Amgen, Inc
IPC分类号： C07D471/04
摘要： The present application discloses a method comprising: (A)
(i) admixing a methylnicotinate of Formula (I):
wherein R3 is Cl, Br, or I, and R4 is alkyl;
with 1,3,5-triazine, and a base, under conditions sufficient to form a naphthyridinone of Formula (II):
(ii) admixing the naphthyridinone of Formula (II) with methoxyethanol, a base, and a copper (I) catalyst, under conditions sufficient to form 3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one ("NAPH"):
or (B):
(i) admixing protected 2-alkoxypyridin-4-ylamine with a lithium reagent, under conditions sufficient to form the protected N-(3-formyl-4-amino-2-alkoxy)pyridine:
wherein PG is a protecting group
wherein R 8 is an alkyl group;
(ii) admixing the protected N-(3-formyl-4-amino-2-alkoxy)pyridine with 1-hydroxy-2-(2-methoxyethoxy)ethane-1 -sulfonate:
and base, under conditions sufficient to form a naphthyridine of Formula (III):
; and
(iii) acidifying the naphthyridine of Formula (III), under conditions sufficient to form 3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one ("NAPH"):
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