发明授权
- 专利标题: Pd-catalyzed coupling of pyrazole amides
- 专利标题(中): 吡唑酰胺的Pd催化偶联
-
申请号: US14925544申请日: 2015-10-28
-
公开(公告)号: US09505759B2公开(公告)日: 2016-11-29
- 发明人: Serena Maria Fantasia , Kurt Puentener
- 申请人: Hoffmann-La Roche Inc.
- 申请人地址: US NJ Little Falls
- 专利权人: Hoffmann-La Roche Inc.
- 当前专利权人: Hoffmann-La Roche Inc.
- 当前专利权人地址: US NJ Little Falls
- 优先权: EP13166027 20130430
- 主分类号: C07D401/14
- IPC分类号: C07D401/14 ; C07D401/02 ; C07D401/10 ; C07D471/04
摘要:
A novel process for the preparation of imidazo[1,2-a]pyridine compounds of the formula wherein R1 is C1-4-alkoxy or NR4R5 wherein R4 and R5 are independently hydrogen or C1-4-alkyl or R4 and R5, together with the nitrogen atom to which they are attached, form a saturated 4- to 6-membered heterocyclic ring which may contain one further heteroatom selected from nitrogen or oxygen; R2 is C1-4-alkyl, C1-4-alkoxycarbonyl, halogen, phenyl which is optionally substituted with C1-4-alkyl, C1-4-alkoxy or halogen or is NR4R5 wherein R4 and R5 are independently hydrogen or C1-4-alkyl or R4 and R5, together with the nitrogen atom to which they are attached, form a saturated 4- to 6-membered heterocyclic ring which may contain one further heteroatom selected from nitrogen or oxygen; R3 is C1-4-alkyl and X is nitrogen or CH is described. The imidazo[1,2-a]pyridine compounds of the formula I are either precursors for active principles or active principles itself, acting as phosphodiesterase (PDE) inhibitors, particularly PDE10 inhibitors which have the potential to treat psychotic disorders like schizophrenia (Int. Patent Publication WO 2012/076430).
公开/授权文献
- US20160046628A1 Pd-CATALYZED COUPLING OF PYRAZOLE AMIDES 公开/授权日:2016-02-18
信息查询