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Synfacts 2011(5): 0461-0461  
DOI: 10.1055/s-0030-1259769
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of Renin Inhibitor MK-1597

Contributor(s): Philip Kocienski
C. Molinaro et al.*
Merck, Kirkland, Canada; Merck, Rahway, USA and Actelion Pharmaceuticals, Allschwil, Switzerland
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Publication History

Publication Date:
15 April 2011 (online)

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Significance

The key feature in the synthesis of MK-1597 (ACT-178882) is the highly efficient ruthenium-catalyzed asymmetric hydrogenation of the tetrasubstituted alkene J followed by a mild epimerization reaction to set both stereogenic centers in H (trans/cis > 120:1).