发明授权
- 专利标题: Process for the preparation of CCR-2 antagonists
- 专利标题(中): 制备CCR-2拮抗剂的方法
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申请号: US10577587申请日: 2004-10-25
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公开(公告)号: US07361765B2公开(公告)日: 2008-04-22
- 发明人: Dongwei Cai , Fred Fleitz , Min Ge , Scott Hoerrner , Gary Javadi , Mark Jensen , Robert Larsen , Wenjie Li , Dorian Nelson , Elizabeth Szumigala , Lihu Yang , Changyou Zhou
- 申请人: Dongwei Cai , Fred Fleitz , Min Ge , Scott Hoerrner , Gary Javadi , Mark Jensen , Robert Larsen , Wenjie Li , Dorian Nelson , Elizabeth Szumigala , Lihu Yang , Changyou Zhou
- 申请人地址: US NJ Rahway
- 专利权人: Merck & Co., Inc.
- 当前专利权人: Merck & Co., Inc.
- 当前专利权人地址: US NJ Rahway
- 代理商 James L. McGinnis; Mark Daniel
- 国际申请: PCT/US2004/035294 WO 20041025
- 国际公布: WO2005/044795 WO 20050519
- 主分类号: C07D471/02
- IPC分类号: C07D471/02
摘要:
The present invention provides an efficient synthesis for the preparation of ((1R,3S)-3-isopropyl-3-{[3-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopentyl)[(3S,4S)-3-m ethoxytetrahydro-2H-pyran-4-yl]amine and its succinate salt. The present invention additionally provides an efficient syntheses for the preparation of intermediates (3R)-3-methoxytetrahydro-4H-pyran-4-one; (1S,4S)-4-(2,5-dimethyl-1H-pyrrol-1-yl)-1-isopropylcyclopent-2-ene-1-carboxylic acid; and 3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,6-naphthyridine; and for the preparation of the precursor (3S,4S)-N-((1S,4S)-4-isopropyl-4-{[3-(tri-fluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopent-2-en-1-yl)-3-methoxytetrahydro-2H-pyran-4-amine. The invention additionally resides in the superior properties of the succinate salt of ((1R,3S)-3-isopropyl-3-1{[3-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl]carbonyl}cyclopentyl)[(3S,4S)-3-methoxytetrahydro-2H-pyran-4-yl]amine
公开/授权文献
- US20070135475A1 Process for the preparation of ccr-2 antagonists 公开/授权日:2007-06-14
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