发明申请
- 专利标题: METHOD FOR MANUFACTURING HETEROCYCLE SUBSTITUTED PYRIDINE DERIVATIVES
- 专利标题(中): 制备杂环取代的吡啶衍生物的方法
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申请号: US12809011申请日: 2008-12-25
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公开(公告)号: US20110263845A1公开(公告)日: 2011-10-27
- 发明人: Jun Niijima , Kazuhiro Yoshizawa , Yuki Kosaka , Shinya Abe
- 申请人: Jun Niijima , Kazuhiro Yoshizawa , Yuki Kosaka , Shinya Abe
- 申请人地址: JP Tokyo
- 专利权人: Eisai R&D Management Co., Ltd.
- 当前专利权人: Eisai R&D Management Co., Ltd.
- 当前专利权人地址: JP Tokyo
- 国际申请: PCT/JP2008/073545 WO 20081225
- 主分类号: C07D498/04
- IPC分类号: C07D498/04 ; C07D413/04 ; C07F5/02 ; C07D213/64 ; C07D413/14 ; C07F5/04
摘要:
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.
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