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

✍ Scribed by Noriaki Gomi; Tadaaki Ohgiya; Kimiyuki Shibuya; Jyunji Katsuyama; Masayuki Masumoto; Hitoshi Sakai

Publisher: John Wiley and Sons
Year: 2011
Weight: 42 KB
Volume: 42
Category: Article
ISSN: 0931-7597
DOI: 10.1002/chin.201148185

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✦ Synopsis

Abstract

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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