Invention Grant
- Patent Title: Method for manufacturing heterocycle substituted pyridine derivatives
- Patent Title (中): 制备杂环取代吡啶衍生物的方法
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Application No.: US12809011Application Date: 2008-12-25
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Publication No.: US08410277B2Publication Date: 2013-04-02
- Inventor: Jun Niijima , Kazuhiro Yoshizawa , Yuki Kosaka , Shinya Abe
- Applicant: Jun Niijima , Kazuhiro Yoshizawa , Yuki Kosaka , Shinya Abe
- Applicant Address: JP Tokyo
- Assignee: Eisai R&D Managment Co., Ltd.
- Current Assignee: Eisai R&D Managment Co., Ltd.
- Current Assignee Address: JP Tokyo
- Agency: Birch, Stewart, Kolasch & Birch, LLP
- International Application: PCT/JP2008/073545 WO 20081225
- International Announcement: WO2009/081970 WO 20090702
- Main IPC: C07D413/14
- IPC: C07D413/14

Abstract:
It is an object of the present invention to provide an efficient method for manufacturing heterocycle-substituted pyridine derivatives. The present invention provides a method for manufacturing a compound represented by the following formula (I): the method including reacting a compound represented by the following formula (III): and a compound represented by the following formula (II): in a solvent and in the presence of a palladium catalyst and a base, wherein R1 represents a hydrogen atom, etc.; R2 represents a hydrogen atom, a C1-6 alkyl group, an amino group that may be protected with a protective group, etc.; one of X and Y represents a nitrogen atom and the other represents a nitrogen atom or an oxygen atom; Q represents a leaving group; the ring A represents a 5- or 6-member heteroaryl ring or a benzene ring, which may have one or two halogen atoms or C1-6 alkyl groups; Z represents a single bond, a methylene group, an ethylene group, an oxygen atom, etc.; R represents a hydrogen atom or a C1-6 alkyl group, etc.; R3 represents a hydrogen atom or a halogen atom, etc.; and R4 represents a hydrogen atom or a halogen atom; provided that when Z represents a single bond, or when R3 represents a hydrogen atom, then R1, R2, and R4 cannot all be a hydrogen atom at the same time.
Public/Granted literature
- US20110263845A1 METHOD FOR MANUFACTURING HETEROCYCLE SUBSTITUTED PYRIDINE DERIVATIVES Public/Granted day:2011-10-27
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