发明授权
US07960558B2 Pharmaceutical intermediate for synthesizing ACE inhibitors and the use thereof
有权
用于合成ACE抑制剂的药物中间体及其用途
- 专利标题: Pharmaceutical intermediate for synthesizing ACE inhibitors and the use thereof
- 专利标题(中): 用于合成ACE抑制剂的药物中间体及其用途
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申请号: US12300545申请日: 2007-05-11
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公开(公告)号: US07960558B2公开(公告)日: 2011-06-14
- 发明人: Márta Porcs-Makkay , Gyula Simig , Tibor Mezei , Angéla Veressné Pandur , Gyula Lukács
- 申请人: Márta Porcs-Makkay , Gyula Simig , Tibor Mezei , Angéla Veressné Pandur , Gyula Lukács
- 申请人地址: HU Budapest
- 专利权人: Egis Gyogyszergyar Nyilvanosan Mukodo Reszvenytarsasag
- 当前专利权人: Egis Gyogyszergyar Nyilvanosan Mukodo Reszvenytarsasag
- 当前专利权人地址: HU Budapest
- 代理商 Jonathan Myers; Andrew Wilford
- 优先权: HU0600403 20060512; HU0600404 20060512
- 国际申请: PCT/HU2007/000039 WO 20070511
- 国际公布: WO2007/132277 WO 20071122
- 主分类号: C07D263/44
- IPC分类号: C07D263/44 ; C07D209/52 ; C07D209/42 ; C07C69/96
摘要:
The compounds of the general Formula (I), wherein R1 is aryl or alkyl; R2 represents alkyl; R3 represents alkyl or aralkyl, are valuable pharmaceutical intermediates, which can be prepared by reacting a compound of the general Formula (IV) (wherein the definitions of R1 and R2 are as above), with at least 2 molar equivalents of the compound of the general Formula (VI) (wherein X represents halogen or tertiary butyloxycarbonyloxy group and R3 is as defined above). The known compounds of the general Formula (II) (wherein R1 and R2 are as defined above) are prepared by reacting the compounds of the general Formula (I) with thionyl chloride. The compounds of the general Formula (I) are new intermediates useful in the synthesis of pharmaceutically active ingredients, particularly in the preparation of ACE-inhibitors, e.g. enalapril, perindopril or ramipril.
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