发明申请
- 专利标题: Ccr-2 antagonist salt
- 专利标题(中): Ccr-2拮抗剂盐
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申请号: US10577584申请日: 2004-10-25
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公开(公告)号: US20070135474A1公开(公告)日: 2007-06-14
- 发明人: Mark Jensen , Robert Larsen , Daniel Sidler
- 申请人: Mark Jensen , Robert Larsen , Daniel Sidler
- 国际申请: PCT/US04/35069 WO 20041025
- 主分类号: A61K31/4745
- IPC分类号: A61K31/4745 ; 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-methoxytetrahydro-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; (1 S ,4 S )-4-(2,5-dimethyl-1 H -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-(trifluoromethyl)-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-{[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
- US07473696B2 CCR-2 antagonist salt 公开/授权日:2009-01-06
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