C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 471/04 (2006.01) C07D 309/30 (2006.01)
Patent
CA 2543250
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-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin- 6(5H)-yl]carbonyl}cyclopent-2-e n-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.
L'invention concerne une synthèse efficace pour l'élaboration de ((1R,3S)-3-isopropyle-3-{[3-(trifluorométhyle)-7,8-dihydro-1,6-naphthyridine-6(5H)-yle]carbonyle}cyclopentyle)[(3S,4S)-3-méthoxytétrahydro-2H-pyrane-4-yle]amine et son succinate correspondant, mais aussi une synthèse efficace pour l'élaboration d'intermédiaires (3R)-3-méthoxytétrahydro-4H-pyrane-4-one; (1<I>S</I>,4<I>S</I>)-4-(2,5-diméthyle-1<I>H</I>-pyrrole-1-yle)-1-isopropylcyclopent-2-ène-1-acide carboxylique; et 3-(trifluorométhyle)-5,6,7,8-tétrahydro-1,6-naphthyridine; ainsi que pour l'élaboration du précurseur (3S,4S)-N-((1S,4S)-4-isopropyle-4-{[3-(trifluorométhyle)-7,8-dihydro-1,6-naphthyridine-6(5H)-yle]carbonyle}cyclopent-2-èn-1-yle)-3-méthoxytétrahydro-2H-pyrane-4-amine. Enfin, l'invention concerne les propriétés supérieures du succinate de ((1R,3S)-3-isopropyle-3-{[3-(trifluorométhyle)-7,8-dihydro-1,6-naphthyridine-6(5H)-yle]carbonyle}cyclopentyle)[(3S,4S)-3-méthoxytétrahydro-2H-pyrane-4-yle]amine.
Cai Dong-Wei
Fleitz Fred
Ge Min
Hoerrner Scott
Javadi Gary
Merck & Co. Inc.
Merck Sharp & Dohme Corp.
Norton Rose Or S.e.n.c.r.l. S.r.l./llp
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