ChemInform Abstract: A Practical Synthesis of Novel Rho-Kinase Inhibitor, (S)-4-Fluoro-5-(2-methyl-1,4-diazepan-1-ylsulfonyl)isoquinoline

ChemInform Abstract: A Practical Synthesis of Novel Rho-Kinase Inhibitor, (S)-4-Fluoro-5-(2-methyl-1,4-diazepan-1-ylsulfonyl)isoquinoline

The synthesis of the novel inhibitor (VII) is achieved in multi‐kilogram scale overcoming two major issues: the need of developing a regioselective chlorosulfonylation reaction at C‐5 of fluoroisoquinoline and the stereochemical purity in the asymmetric construction of the methyldiazepane moiety....

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Veröffentlicht in:ChemInform 2011-11, Vol.42 (48), p.no-no
Hauptverfasser: Gomi, Noriaki, Ohgiya, Tadaaki, Shibuya, Kimiyuki, Katsuyama, Jyunji, Masumoto, Masayuki, Sakai, Hitoshi
Format: Artikel
Sprache:eng
Schlagworte:
enzyme inhibiting activity
multi-membered N-heterocycles
ring closure reactions
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Zusammenfassung:The synthesis of the novel inhibitor (VII) is achieved in multi‐kilogram scale overcoming two major issues: the need of developing a regioselective chlorosulfonylation reaction at C‐5 of fluoroisoquinoline and the stereochemical purity in the asymmetric construction of the methyldiazepane moiety.
ISSN:0931-7597
1522-2667
DOI:10.1002/chin.201148185