A total synthesis of aliskiren

Abstract

A total synthesis of aliskiren (20) was accomplished. A key in our synthesis was to use the symmetric trans-cisoid-trans-bis-lactone 1 as a precursor. It was expediently prepared by three different routes (Scheme 2). Appending the end groups and functional group transformations completed the synthesis (Scheme 3). Copyright © 2012 Verlag Helvetica Chimica Acta AG, Zürich, Switzerland.