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    • 4. 发明申请
    • Ccr-2 antagonist salt
    • Ccr-2拮抗剂盐
    • US20070135474A1
    • 2007-06-14
    • US10577584
    • 2004-10-25
    • Mark JensenRobert LarsenDaniel Sidler
    • Mark JensenRobert LarsenDaniel Sidler
    • A61K31/4745C07D471/02
    • C07D471/04
    • 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.
    • 本发明提供了制备((1R,3S)-3-异丙基-3 - {[3-(三氟甲基)-7,8-二氢-1,6-二氮杂萘-6(5H) ]羰基}环戊基)[(3S,4S)-3-甲氧基四氢-2H-吡喃-4-基]胺及其琥珀酸盐。 本发明另外提供了制备中间体(3R)-3-甲氧基四氢-4H-吡喃-4-酮的有效合成方法; (1S,4S)-4-(2,5-二甲基-1H - 吡咯-1-基)-1- 异丙基环戊-2-烯-1-羧酸; 和3-(三氟甲基)-5,6,7,8-四氢-1,6-萘啶; 制备前体(3S,4S)-N - ((1S,4S)-4-异丙基-4 - {[3-(三氟甲基)-7,8-二氢-1,6-萘啶-6( 5H) - 基]羰基}环戊-2-烯-1-基)-3-甲氧基四氢-2H-吡喃-4-胺。 本发明还涉及((1R,3S)-3-异丙基-3 - {[3-(三氟甲基)-7,8-二氢-1,6-二氮杂萘-6(5H))的琥珀酸盐的优异性能, - 基]羰基}环戊基)[(3S,4S)-3-甲氧基四氢-2H-吡喃-4-基]胺。