Synthesis of a Precursor to Sacubitril Using Enabling Technologies

An efficient preparation of a precursor to the neprilysin inhibitor sacubitril is described. The convergent synthesis features a diastereoselective Reformatsky-type carbethoxyallylation and a rhodium-catalyzed stereoselective hydrogenation for installation of the two key stereocenters. Moreover, by...

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Veröffentlicht in:	Organic letters 2015-11, Vol.17 (21), p.5436-5439
Hauptverfasser:	Lau, Shing-Hing, Bourne, Samuel L, Martin, Benjamin, Schenkel, Berthold, Penn, Gerhard, Ley, Steven V
Format:	Artikel
Sprache:	eng
Schlagworte:	Aminobutyrates - chemical synthesis Aminobutyrates - chemistry Aminobutyrates - pharmacology Catalysis Drug Combinations Hydrogenation Molecular Structure Neprilysin - antagonists & inhibitors Rhodium - chemistry Stereoisomerism Tetrazoles - chemical synthesis Tetrazoles - chemistry Tetrazoles - pharmacology
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