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Synfacts 2011(10): 1040-1040  
DOI: 10.1055/s-0030-1261044
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of Aliskiren

Contributor(s): Philip Kocienski
J. Slade, H. Liu, M. Prashad, K. Prasad*
Novartis Pharmaceuticals Corporation, East Hanover, USA
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Publication History

Publication Date:
20 September 2011 (online)

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Significance

Aliskiren (Tekturna®) was recently launched as the first orally active non-peptidic renin inhibitor. A 12-step synthesis is described that features a Curtius rearrangement to transform carboxylic acid B to the benzyl carbamate D via the isocyanate C.